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Geraniol, a natural monoterpene, is a component of many plant essential oils. It contains many medicinal and pharmacological properties. Doxorubicin is an anticancer drug; however, its clinical usage is limited due to its cumulative and dose-dependent cardiotoxicity. This study investigates geraniol as a protective agent against doxorubicin-induced cardiotoxicity and explores possible underlying mechanisms of action. Methods: Male Sprague-Dawley rats were allocated into five groups. Groups 1 and 2 were administered saline and geraniol 200 mg/kg/day/orally, respectively, for 15 days. Group 3 was administered intraperitoneal doxorubicin (5 mg/kg/IP on the 5th, 10th and 15th days to achieve a cumulative dose of 15 mg/kg) to induce cardiotoxicity. The fourth and fifth groups were treated with either geraniol 100 mg/kg or 200 mg/kg orally and doxorubicin to equal the doxorubicin dose administered to Group 3. Results: Treatment with geraniol significantly ameliorated cardiac damage and restored serum cardiac injury marker levels in doxorubicin treated animals. Geraniol upregulated Nrf2 and HO-1 expression, elevated total antioxidant capacity, decreased the nuclear accumulation of kappa-light-chain enhancer of activated B cells (NF-κB), decreased the phosphorylation and degradation of nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor, alpha (IκBα), suppressed tumor necrosis factor-alpha (TNF-α), interleukin 1 beta (IL-1β), and interleukin-18 (IL-18) levels, and restored the levels of Bax and caspase-3 and 9 in heart tissue. Conclusion: Geraniol may function as a potential activator of nuclear factor erythroid 2-related factor 2 (Nrf2), which subsequently improves Nrf2-dependent antioxidative signaling, diminishes apoptosis and subdues the inflammatory response. The downstream result is protection of the heart from doxorubicin-induced cardiotoxicity.
Nancy S. Younis; Heba S. Elsewedy; Wafaa E. Soliman; Tamer M. Shehata; Maged E. Mohamed. Geraniol isolated from lemon grass to mitigate doxorubicin-induced cardiotoxicity through Nrf2 and NF-κB signaling. Chemico-Biological Interactions 2021, 347, 109599 .
AMA StyleNancy S. Younis, Heba S. Elsewedy, Wafaa E. Soliman, Tamer M. Shehata, Maged E. Mohamed. Geraniol isolated from lemon grass to mitigate doxorubicin-induced cardiotoxicity through Nrf2 and NF-κB signaling. Chemico-Biological Interactions. 2021; 347 ():109599.
Chicago/Turabian StyleNancy S. Younis; Heba S. Elsewedy; Wafaa E. Soliman; Tamer M. Shehata; Maged E. Mohamed. 2021. "Geraniol isolated from lemon grass to mitigate doxorubicin-induced cardiotoxicity through Nrf2 and NF-κB signaling." Chemico-Biological Interactions 347, no. : 109599.
Natural products have been extensively used for treating a wide variety of disorders. In recent times, Brucine (BRU) as one of the natural medications extracted from seeds of nux vomica, was investigated for its anticancer activity. As far as we know, this is the first study on BRU anticancer activity against skin cancer. Thus, the rational of this work was implemented to develop, optimize and characterize the anticancer activity of BRU loaded ethosomal gel. Basically, thin film hydration method was used to formulate BRU ethosomal preparations, by means of Central composite design (CCD), which were operated to construct (32) factorial design. Two independent variables were designated (phospholipid percentage and ethanol percentage) with three responses (vesicular size, encapsulation efficiency and flux). Based on the desirability function, one formula was selected and incorporated into HPMC gel base to develop BRU loaded ethosomal gel. The fabricated gel was assessed for all physical characterization. In-vitro release investigation, ex-vivo permeation and MTT calorimetric assay were performed. BRU loaded ethosomal gel exhibited acceptable values for the characterization parameters which stand proper for topical application. In-vitro release investigation was efficiently prolonged for 6 h. The flux from BRU loaded ethosome was enhanced screening optimum SSTF value. Finally, in-vitro cytotoxicity study proved that BRU loaded ethosomal gel significantly improved the anticancer activity of the drug against A375 human melanoma cell lines. Substantially, the investigation proposed a strong motivation for further study of the lately developed BRU loaded ethosomal gel as a prospective therapeutic strategy for melanoma treatment.
Tamer Ismail; Tamer Shehata; Dalia Mohamed; Heba Elsewedy; Wafaa Soliman. Quality by Design for Development, Optimization and Characterization of Brucine Ethosomal Gel for Skin Cancer Delivery. Molecules 2021, 26, 3454 .
AMA StyleTamer Ismail, Tamer Shehata, Dalia Mohamed, Heba Elsewedy, Wafaa Soliman. Quality by Design for Development, Optimization and Characterization of Brucine Ethosomal Gel for Skin Cancer Delivery. Molecules. 2021; 26 (11):3454.
Chicago/Turabian StyleTamer Ismail; Tamer Shehata; Dalia Mohamed; Heba Elsewedy; Wafaa Soliman. 2021. "Quality by Design for Development, Optimization and Characterization of Brucine Ethosomal Gel for Skin Cancer Delivery." Molecules 26, no. 11: 3454.
Date palm fruit (Phoenix dactylifera) is reputed to have numerous biological activities, including anticancer properties. To utilize the great fortune of this fruit, the current study aimed to maximize its pharmacological activity. Date palm extract (DPE) of Khalas cultivar was obtained in powder form and then was formulated into nanoemulsion (NE). The optimized DPE-NE was formulated along with its naked counterpart followed by studying their physical and chemical properties. A qualitative assessment of total serum protein associated with the surface of formulations was implemented. Studies for the in vitro release of DPE from developed NE before and after incubation with serum were investigated. Eventually, an MTT assay was conducted. Total phenolic and flavonoid contents were 22.89 ± 0.013 mg GAE/g of dry DPE and 9.90 ± 0.03 mg QE/g of dry DPE, respectively. Homogenous NE formulations were attained with appropriate particle size and viscosity that could be administered intravenously. The optimized PEGylated NE exhibited a proper particle size, PDI, and zeta potential. Total serum protein adsorbed on PEG-NE surface was significantly low. The release of the drug through in vitro study was effectively extended for 24 h. Ultimately; PEGylated NE of DPE attained significant inhibition for cancer cell viability with IC50 values of 18.6 ± 2.4 and 13.5 ± 1.8 µg/mL for MCF-7 and HepG2 cell lines, respectively. PEGylated NE of DPE of Khalas cultivar will open the gate for future adjuvants for cancer therapy.
Hany Khalil; Nashi Alqahtani; Hossam Darrag; Hairul-Islam Ibrahim; Promise Emeka; Lorina Badger-Emeka; Katsuyoshi Matsunami; Tamer Shehata; Heba Elsewedy. Date Palm Extract (Phoenix dactylifera) PEGylated Nanoemulsion: Development, Optimization and Cytotoxicity Evaluation. Plants 2021, 10, 735 .
AMA StyleHany Khalil, Nashi Alqahtani, Hossam Darrag, Hairul-Islam Ibrahim, Promise Emeka, Lorina Badger-Emeka, Katsuyoshi Matsunami, Tamer Shehata, Heba Elsewedy. Date Palm Extract (Phoenix dactylifera) PEGylated Nanoemulsion: Development, Optimization and Cytotoxicity Evaluation. Plants. 2021; 10 (4):735.
Chicago/Turabian StyleHany Khalil; Nashi Alqahtani; Hossam Darrag; Hairul-Islam Ibrahim; Promise Emeka; Lorina Badger-Emeka; Katsuyoshi Matsunami; Tamer Shehata; Heba Elsewedy. 2021. "Date Palm Extract (Phoenix dactylifera) PEGylated Nanoemulsion: Development, Optimization and Cytotoxicity Evaluation." Plants 10, no. 4: 735.
Breast cancer is the second most common cancers among female worldwide. The current treatment strategies includes surgery, chemo-, radio- and hormone-therapy. Nevertheless, breast cancer still accounts for more than 20% of all female cancer deaths, presumably, due to the lack of specificity to target site or the development of drug resistance. Graphene nanoribbons (GNRs) are one of the promising platforms that show efficient cellular internalization and high target specificity for cancer cells. Herein, oxidized graphene nanoribbons (OGNRs), decorated with folic acid (FA) and loaded with the selective estrogen receptor modulator, tamoxifen citrate (TC), were prepared from multi-walled carbon nanotubes using the longitudinal unzipping method. The synthesized TC-loaded OGNRs-FA showed multi-layered structure with drug loading efficiency of 56%. In vitro release studies showed a pH-dependent release of TC from OGNRs. In addition, TC loaded onto OGNRs significantly reduces cell viability and induces apoptosis in MCF-7 and MDA-MB-231 breast cancer cell lines in concentration and-time dependent manner. Most importantly, cellular uptake studies revealed that surface decoration of OGNRs with FA significantly contributed to the preferential cellular internalization of TC-loaded OGRNs-FA by breast cancer cells, compared to naked OGNRs. In vivo pharmacokinetic study suggests that drug loading onto OGNRs-FA remarkably reduced the premature drug release in systemic circulation and, consequently, could enhance the availability of drug payload at the target site. Collectively, OGNRs-FA might represent a promising platform for efficient and selective delivery of tamoxifen to breast cancer cells. However, deep understanding of the in vivo fate and long-term toxicity of OGNRs-FA is crucial for further clinical application.
Amr S. Abu Lila; Mahmoud S. Soliman; H.C. Kiran; H.V. Gangadharappa; Kareem M. Younes; El-Sayed Khafagy; Tamer M. Shehata; Mahmoud M. Ibrahim; Marwa H. Abdallah. Tamoxifen-loaded functionalized graphene nanoribbons for breast cancer therapy. Journal of Drug Delivery Science and Technology 2021, 63, 102499 .
AMA StyleAmr S. Abu Lila, Mahmoud S. Soliman, H.C. Kiran, H.V. Gangadharappa, Kareem M. Younes, El-Sayed Khafagy, Tamer M. Shehata, Mahmoud M. Ibrahim, Marwa H. Abdallah. Tamoxifen-loaded functionalized graphene nanoribbons for breast cancer therapy. Journal of Drug Delivery Science and Technology. 2021; 63 ():102499.
Chicago/Turabian StyleAmr S. Abu Lila; Mahmoud S. Soliman; H.C. Kiran; H.V. Gangadharappa; Kareem M. Younes; El-Sayed Khafagy; Tamer M. Shehata; Mahmoud M. Ibrahim; Marwa H. Abdallah. 2021. "Tamoxifen-loaded functionalized graphene nanoribbons for breast cancer therapy." Journal of Drug Delivery Science and Technology 63, no. : 102499.
Curcumin is a poorly water-soluble drug that is used for the treatment of inflammations, tumors, wound healing antioxidant and other diseases. In the current manuscript, it is successfully formulated into proniosome gels. The proniosomes are readily hydrated into niosomal formulations using warm water. Proniosomes were prepared using nonionic surfactants (tween 80, span 60) either solely or in combinations with cholesterol. The produced niosomal formulations were homogenous in size with vesicular sizes >343 and <1800 nm. The encapsulation efficiency percentage “EE%” of curcumin in niosomal formulations was different according to niosomal composition. It increased up to 99.74% in formulations of tween 80/Chol of 200 μmole/mL lipid concentration. Span 60/chol niosomes showed decreased curcumin EE%. Niosomal formulations showed increased SSTF and PC with enhancement ratios of more than 20-fold compared with curcumin suspension form. Kinetically, niosomes fitted to the Korsemeyer-Peppas model with non-Fickian transport according to their calculated n-values where curcumin suspension form showed Korsemeyer-Peppas kinetics with Fickian transport. Niosomal formulations deposited higher curcumin amounts in the skin compared with the suspension form. The best niosomal formulation (F9) was used for niosomal gel and emulgel fabrication. Finally, the anti-inflammatory activity of curcumin in various formulations was evaluated using a rat hind paw edema method and the % of swelling was 17.5% following 24 h in group treated with curcumin niosomal emulgel. In conclusion, this study suggests that the developed niosomal emulgel could significantly enhance the anti-inflammatory effect of curcumin and be an efficient carrier for the transdermal delivery of the drug.
Tamer Shehata; Mahmoud Ibrahim; Heba Elsewedy. Curcumin Niosomes Prepared from Proniosomal Gels: In Vitro Skin Permeability, Kinetic and In Vivo Studies. Polymers 2021, 13, 791 .
AMA StyleTamer Shehata, Mahmoud Ibrahim, Heba Elsewedy. Curcumin Niosomes Prepared from Proniosomal Gels: In Vitro Skin Permeability, Kinetic and In Vivo Studies. Polymers. 2021; 13 (5):791.
Chicago/Turabian StyleTamer Shehata; Mahmoud Ibrahim; Heba Elsewedy. 2021. "Curcumin Niosomes Prepared from Proniosomal Gels: In Vitro Skin Permeability, Kinetic and In Vivo Studies." Polymers 13, no. 5: 791.
Background: Curcumin (Cur) possesses a variety of beneficial pharmacological properties including antioxidant, antimicrobial, anti-cancer and anti-inflammatory activities. Nevertheless, the low aqueous solubility and subsequent poor bioavailability greatly limits its effectiveness. Besides, the role of myrrh oil as an essential oil in treating inflammatory disorders has been recently demonstrated. The objective of the current investigation is to enhance Cur efficacy via developing Cur nanoemulgel, which helps to improve its solubility and permeability, for transdermal delivery. Methods: The formulated preparations (Cur gel, emulgel and nanoemulgel) were evaluated for their physical appearance, spreadability, viscosity, particle size, in vitro release and ex vivo drug permeation studies. The in vivo anti-inflammatory activity was estimated using the carrageenan-induced rat hind paw edema method. Results: The formulated Cur-loaded preparations exhibited good physical characteristics that were in the acceptable range of transdermal preparations. The release of Cur from gel, emulgel and nanoemulgel after 12 h was 72.17 ± 3.76, 51.93 ± 3.81 and 62.0 ± 3.9%, respectively. Skin permeation of Cur was significantly (p < 0.05) improved when formulated into nanoemulgel since it showed the best steady state transdermal flux (SSTF) value (108.6 ± 3.8 µg/cm2·h) with the highest enhancement ratio (ER) (7.1 ± 0.2). In vivo anti-inflammatory studies proved that Cur-loaded nanoemulgel displayed the lowest percent of swelling (26.6% after 12 h). Conclusions: The obtained data confirmed the potential of the nanoemulgel dosage form and established the synergism of myrrh oil and Cur as an advanced anti-inflammatory drug.
Wafaa E. Soliman; Tamer M. Shehata; Maged E. Mohamed; Nancy S. Younis; Heba S. Elsewedy. Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel. Polymers 2021, 13, 577 .
AMA StyleWafaa E. Soliman, Tamer M. Shehata, Maged E. Mohamed, Nancy S. Younis, Heba S. Elsewedy. Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel. Polymers. 2021; 13 (4):577.
Chicago/Turabian StyleWafaa E. Soliman; Tamer M. Shehata; Maged E. Mohamed; Nancy S. Younis; Heba S. Elsewedy. 2021. "Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel." Polymers 13, no. 4: 577.
Obesity is a growing health problem and a significant contributor to the global burden of disease. Statins have shown efficacy in modulating the mortality risk associated with obesity. Myrrh has recently been proven to reduce body weight gain and improve lipid profiles in obese hyperlipidemic rats. The aim of this study was to formulate and evaluate the anti-obesity potential of a myrrh oil-based nanoemulsion containing the hypolipidemic agent, atorvastatin. A two-factor, three-level, full factorial design was adopted to formulate and optimize the nanoemulsion formulations. The prepared formulations were characterized in terms of drug-excipient compatibility studies, physical appearance, rheological behavior, in vitro drug release, stability, and in vivo anti-obesity potential. The prepared nanoemulsion formulations showed a uniform size distribution with a droplet size within the nano-size range. The release of drug from the nanoemulsion formulations was dependent on the surfactant concentration used. Interestingly, all developed nanoemulsions were stable for up to 3 months upon storage at refrigerator and room temperature. Most importantly, in the high-fat diet-induced obesity rat model, addition of myrrh oil to oleic acid as an oily phase for nanoemulsion showed a synergistic effect to the anti-obesity potential of the hypolipidemic drug atorvastatin. In conclusion, formulating atorvastatin into a myrrh oil-based nanoemulsion might represent a promising approach for augmenting the anti-obesity action of atorvastatin, not only by enhancing its systemic bioavailability, but also by gaining the benefit of the synergistic anti-obesity effect of myrrh oil.
Tamer M. Shehata; Hany Ezzat Khalil; Heba S. Elsewedy; Wafaa E. Soliman. Myrrh essential oil-based nanolipid formulation for enhancement of the antihyperlipidemic effect of atorvastatin. Journal of Drug Delivery Science and Technology 2020, 61, 102277 .
AMA StyleTamer M. Shehata, Hany Ezzat Khalil, Heba S. Elsewedy, Wafaa E. Soliman. Myrrh essential oil-based nanolipid formulation for enhancement of the antihyperlipidemic effect of atorvastatin. Journal of Drug Delivery Science and Technology. 2020; 61 ():102277.
Chicago/Turabian StyleTamer M. Shehata; Hany Ezzat Khalil; Heba S. Elsewedy; Wafaa E. Soliman. 2020. "Myrrh essential oil-based nanolipid formulation for enhancement of the antihyperlipidemic effect of atorvastatin." Journal of Drug Delivery Science and Technology 61, no. : 102277.
The purpose of this study was to fabricate biostable inorganic silver nanoparticles (AgNPs) using fresh peel (aqueous) extract of Benincasa hispida. A fast, robust, and eco-friendly approach was used for the synthesis of AgNPs, where bioactive components of peel extract of B. hispida acted as reducing and stabilizing agents. Synthesized AgNPs were characterized using a UV–Vis spectrophotometer, Fourier-transform infrared spectroscopy (FTIR), dynamic light scattering (DLS), and electron microscopy. The synthesized nanoparticles exhibited maximum absorption at 418 nm under the typical AgNPs surface plasmon resonance band range. They depicted a mean size of 26 ± 2 nm with a spherical shape. Their therapeutic prospective was determined by evaluating their antimicrobial and anticancer potential. The bio-synthesized silver nanoparticles exhibited strong antimicrobial activity with minimum inhibitory concentration (MIC 50) values of 14.5, 8.6, 6.063, and 13.4 μg/mL against Staphylococcus aureus (ATCC 25923), Micrococcus luteus (ATCC 14593), Escherichia coli (ATCC 25922), and Klebsiella pneumonia (ATCC 13883), respectively. The biosynthesized AgNPs showed potent in vitro cytotoxicity against human cervical cancer cell line with a half maximal inhibitory concentration (IC50) value of 0.066 μg/mL; however, no cytotoxic effect was observed on normal human primary osteoblasts cell line. This study explored B. hispida extract and confirmed its effectiveness as a promising source in producing AgNPs that could be employed for several therapeutic applications.
Wafaa E. Soliman; Salman Khan; Syed Mohd Danish Rizvi; Afrasim Moin; Heba S. Elsewedy; Amr S. Abulila; Tamer M. Shehata. Therapeutic Applications of Biostable Silver Nanoparticles Synthesized Using Peel Extract of Benincasa hispida: Antibacterial and Anticancer Activities. Nanomaterials 2020, 10, 1954 .
AMA StyleWafaa E. Soliman, Salman Khan, Syed Mohd Danish Rizvi, Afrasim Moin, Heba S. Elsewedy, Amr S. Abulila, Tamer M. Shehata. Therapeutic Applications of Biostable Silver Nanoparticles Synthesized Using Peel Extract of Benincasa hispida: Antibacterial and Anticancer Activities. Nanomaterials. 2020; 10 (10):1954.
Chicago/Turabian StyleWafaa E. Soliman; Salman Khan; Syed Mohd Danish Rizvi; Afrasim Moin; Heba S. Elsewedy; Amr S. Abulila; Tamer M. Shehata. 2020. "Therapeutic Applications of Biostable Silver Nanoparticles Synthesized Using Peel Extract of Benincasa hispida: Antibacterial and Anticancer Activities." Nanomaterials 10, no. 10: 1954.
Transdermal delivery of insulin is a great challenge due to its poor permeability through the skin. The aim of the current investigation was to evaluate the prospective of insulin loaded niosome emulgel as a noninvasive delivery system for its transdermal therapy. A 23 full-factorial design was used to optimize the insulin niosome emulgel by assessing the effect of independent variables (concentration of paraffin oil, Tween 80 and sodium carboxymethyl cellulose) on dependent variables (in vitro release, viscosity and in vitro permeation). The physical characteristics of the prepared formulations were carried out by determining viscosity, particle size, entrapment efficiency, drug loading, drug release and kinetics. In vitro permeation studies were carried out using rat skin membrane. Hypoglycemic activity of prepared formulations was assessed in diabetic-induced rats. It was observed that the independent variables influenced the dependent variables. A significant difference (p < 0.05) in viscosity was noticed between the prepared gels, which in turn influenced the insulin release. The order of permeation is: insulin niosome emulgel > insulin niosome gel > insulin emulgel > insulin gel > insulin niosomes > insulin solution. The enhancement in transdermal flux in insulin niosome emulgel was 10-fold higher than the control (insulin solution). In vivo data significantly demonstrated reduction (p < 0.05) of plasma glucose level (at six hours) by insulin niosome emulgel than other formulations tested. The results suggest that the developed insulin niosome emulgel could be an efficient carrier for the transdermal delivery of insulin.
Tamer M. Shehata; Anroop B. Nair; Bandar E. Al-Dhubiab; Jigar Shah; Shery Jacob; Ibrahim A. Alhaider; Mahesh Attimarad; Heba S. Elsewedy; Mahmoud M. Ibrahim. Vesicular Emulgel Based System for Transdermal Delivery of Insulin: Factorial Design and In Vivo Evaluation. Applied Sciences 2020, 10, 5341 .
AMA StyleTamer M. Shehata, Anroop B. Nair, Bandar E. Al-Dhubiab, Jigar Shah, Shery Jacob, Ibrahim A. Alhaider, Mahesh Attimarad, Heba S. Elsewedy, Mahmoud M. Ibrahim. Vesicular Emulgel Based System for Transdermal Delivery of Insulin: Factorial Design and In Vivo Evaluation. Applied Sciences. 2020; 10 (15):5341.
Chicago/Turabian StyleTamer M. Shehata; Anroop B. Nair; Bandar E. Al-Dhubiab; Jigar Shah; Shery Jacob; Ibrahim A. Alhaider; Mahesh Attimarad; Heba S. Elsewedy; Mahmoud M. Ibrahim. 2020. "Vesicular Emulgel Based System for Transdermal Delivery of Insulin: Factorial Design and In Vivo Evaluation." Applied Sciences 10, no. 15: 5341.
Tissue repair and wound healing are complex processes that involve inflammation, granulation, and remodeling of the tissue. The potential of various statins including atorvastatin (ATR) to improve the wound healing effect was established. The aim of this study was to formulate and evaluate the efficacy of topical application of ATR-based nanoemulgel on wound healing. The prepared formulations (ATR gel, ATR emulgel, and ATR nanoemulgel) were evaluated for their physical appearance, rheological behavior, in vitro drug release and ex vivo drug permeation. The in vivo wound healing effect was evaluated in wound-induced rats. The prepared ATR gel formulations showed good physical properties and were comparable. The release profiles of drugs from gel, emulgel, and nanoemulgel were distinct. Skin permeation potential of ATR was significantly (p < 0.05) enhanced when formulated into nanoemulgel. In vivo wound healing studies showed that ATR nanoemulgel exhibited the highest percent wound contraction. Histopathological assessment showed marked improvement in the skin histological architecture after 21 days of ATR nanoemulgel treatment. In conclusion, the data demonstrated here signify the prospective of ATR nanoemulgel as an innovative therapeutic approach in wound healing.
Mohamed A. Morsy; Rania G. Abdel-Latif; Anroop B. Nair; Katharigatta N. Venugopala; Amira F. Ahmed; Heba S. Elsewedy; Tamer M. Shehata. Preparation and Evaluation of Atorvastatin-Loaded Nanoemulgel on Wound-Healing Efficacy. Pharmaceutics 2019, 11, 609 .
AMA StyleMohamed A. Morsy, Rania G. Abdel-Latif, Anroop B. Nair, Katharigatta N. Venugopala, Amira F. Ahmed, Heba S. Elsewedy, Tamer M. Shehata. Preparation and Evaluation of Atorvastatin-Loaded Nanoemulgel on Wound-Healing Efficacy. Pharmaceutics. 2019; 11 (11):609.
Chicago/Turabian StyleMohamed A. Morsy; Rania G. Abdel-Latif; Anroop B. Nair; Katharigatta N. Venugopala; Amira F. Ahmed; Heba S. Elsewedy; Tamer M. Shehata. 2019. "Preparation and Evaluation of Atorvastatin-Loaded Nanoemulgel on Wound-Healing Efficacy." Pharmaceutics 11, no. 11: 609.
The current study aimed to formulate gelatin/sodium alginate nanoparticles utilizing BÜCHI nano spray dryer B-90. Nanoparticles possess many of the advantages including new routes of drug administrations and sustained release properties. Utilizing B-90 technology, metformin hydrochloride (MET) nanoparticles were successfully developed. Preformulation studies such as atomization head mesh size, flow rate, head temperature, polymer viscosity, and surface tension, were adjusted. Additionally, post-formulation characters such as particle size, flowability, surface scan, and dissolution profiles, were evaluated. Spray head (7 µm hole), flow rate (3.5 ml/min) and head temperature (120 °C) were optimized. Polymer viscosity was less than 11.2 cP with a surface tension less than 70.1 dyne/cm. Moreover, anti-diabetic effects of MET formulations were evaluated in streptozotocin-induced diabetic rats. Here, discrete, non-aggregated free-flowing nanoparticle powders with a particle size less than 850 nm were generated. Gelatin/sodium-alginate (1:3) produced nanoparticles were successfully sustained by the in vitro release profile of the drug. In vivo evaluations of the previous formula showed a significant reduction of blood glucose level over 24 h. In conclusion, Nano Spray Dryer B-90 (Büchi Labortechnik AG, Flawil, Switzerland) offers a promising technology for nanoparticles formulation as controlled drug delivery systems enhancing compliance of type-II diabetic patients.
Tamer M. Shehata; Mahmoud M. Ibrahima. BÜCHI nano spray dryer B-90: a promising technology for the production of metformin hydrochloride-loaded alginate–gelatin nanoparticles. Drug Development and Industrial Pharmacy 2019, 45, 1907 -1914.
AMA StyleTamer M. Shehata, Mahmoud M. Ibrahima. BÜCHI nano spray dryer B-90: a promising technology for the production of metformin hydrochloride-loaded alginate–gelatin nanoparticles. Drug Development and Industrial Pharmacy. 2019; 45 (12):1907-1914.
Chicago/Turabian StyleTamer M. Shehata; Mahmoud M. Ibrahima. 2019. "BÜCHI nano spray dryer B-90: a promising technology for the production of metformin hydrochloride-loaded alginate–gelatin nanoparticles." Drug Development and Industrial Pharmacy 45, no. 12: 1907-1914.
Oral therapy of tramadol, an opiate analgesic, undergoes extensive hepatic metabolism and requires frequent administration. Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce abuse liability of tramadol. The aim of this research was to investigate the possibility of transdermal delivery of tramadol by formulating proniosome gel and evaluate its therapeutic potential in vivo. The effect of formulation composition as well as amount of drug on physicochemical characteristics of prepared proniosomes were examined. Best proniosome gel (F4) was selected and evaluated for drug release, stability and transdermal efficacy by ex vivo and in vivo experiments. The vesicles demonstrated optimal properties including spherical shape, nanosize with good entrapment efficiency, adequate zeta potential, higher stability and greater transdermal flux. The amorphization and dispersion of tramadol in the aqueous core of proniosome vesicles was confirmed by differential scanning calorimeter. Release profile of F4 was distinct (P < 0.001) from control and displayed steady and prolonged tramadol release by Fickian diffusion. Transdermal therapy of F4 showed prominent reduction of induced twitches (P < 0.005) in mice and edema (P < 0.05) in rats, as compared to oral tramadol. The improvement in clinical efficacy of tramadol in transdermal therapy is correlated with the pharmacokinetic data observed. In conclusion, the observed improvement in antinociceptive and anti-inflammatory effects from proniosome carriers signifies its potential to be a suitable alternative to oral therapy of tramadol with greater efficacy.
Jigar Shah; Anroop B. Nair; Hiral Shah; Shery Jacob; Tamer Shehata; Mohamed Aly Morsy. Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel. Asian Journal of Pharmaceutical Sciences 2019, 15, 786 -796.
AMA StyleJigar Shah, Anroop B. Nair, Hiral Shah, Shery Jacob, Tamer Shehata, Mohamed Aly Morsy. Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel. Asian Journal of Pharmaceutical Sciences. 2019; 15 (6):786-796.
Chicago/Turabian StyleJigar Shah; Anroop B. Nair; Hiral Shah; Shery Jacob; Tamer Shehata; Mohamed Aly Morsy. 2019. "Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel." Asian Journal of Pharmaceutical Sciences 15, no. 6: 786-796.
Nanoemulsion is one of the potential drug delivery strategies used in topical ocular therapy. The purpose of this study was to design and optimize a nanoemulsion-based system to improve therapeutic efficacy of moxifloxacin in ophthalmic delivery. Moxifloxacin nanoemulsions were prepared by testing their solubility in oil, surfactants, and cosurfactants. A pseudoternary phase diagram was constructed by titration technique and nanoemulsions were obtained with four component mixtures of Tween 80, Soluphor® P, ethyl oleate and water. An experiment with simplex lattice design was conducted to assess the influence of formulation parameters in seven nanoemulsion formulations (MM1–MM7) containing moxifloxacin. Physicochemical characteristics and in vitro release of MM1–MM7 were examined and optimized formulation (MM3) was further evaluated for ex vivo permeation, antimicrobial activity, ocular irritation and stability. Drug pharmacokinetics in rabbit aqueous humor was assessed for MM3 and compared with conventional commercial eye drop formulation (control). MM3 exhibited complete drug release in 3 h by Higuchi diffusion controlled mechanism. Corneal steady state flux of MM3 (~32.01 µg/cm2/h) and control (~31.53 µg/cm2/h) were comparable. Ocular irritation study indicated good tolerance of MM3 and its safety for ophthalmic use. No significant changes were observed in the physicochemical properties of MM3 when stored in the refrigerator for 3 months. The greater aqueous humor concentration (Cmax; 555.73 ± 133.34 ng/mL) and delayed Tmax value (2 h) observed in MM3 suggest a reduced dosing frequency and increased therapeutic efficacy relative to control. The area under the aqueous humor concentration versus time curve (AUC0–8 h) of MM3 (1859.76 ± 424.51 ng·h/mL) was ~2 fold higher (p < 0.0005) than the control, suggesting a significant improvement in aqueous humor bioavailability. Our findings suggest that optimized nanoemulsion (MM3) enhanced the therapeutic effect of moxifloxacin and can therefore be used as a safe and effective delivery vehicle for ophthalmic therapy.
Jigar Shah; Anroop B. Nair; Shery Jacob; Rakesh K. Patel; Hiral Shah; Tamer M. Shehata; Mohamed Aly Morsy. Nanoemulsion Based Vehicle for Effective Ocular Delivery of Moxifloxacin Using Experimental Design and Pharmacokinetic Study in Rabbits. Pharmaceutics 2019, 11, 230 .
AMA StyleJigar Shah, Anroop B. Nair, Shery Jacob, Rakesh K. Patel, Hiral Shah, Tamer M. Shehata, Mohamed Aly Morsy. Nanoemulsion Based Vehicle for Effective Ocular Delivery of Moxifloxacin Using Experimental Design and Pharmacokinetic Study in Rabbits. Pharmaceutics. 2019; 11 (5):230.
Chicago/Turabian StyleJigar Shah; Anroop B. Nair; Shery Jacob; Rakesh K. Patel; Hiral Shah; Tamer M. Shehata; Mohamed Aly Morsy. 2019. "Nanoemulsion Based Vehicle for Effective Ocular Delivery of Moxifloxacin Using Experimental Design and Pharmacokinetic Study in Rabbits." Pharmaceutics 11, no. 5: 230.
Currently, proniosomes are generating a lot of interest in the field of drug delivery. They are characterized by high stability, extended drug release, ease of manufacturing, and rapid reconstitution and transformation into niosomes. The current study investigated Tramadol HCl (TH) encapsulation into niosomal vesicles using proniosome technology. Tween 80 (T80), Span 80 (S80), Tween 40 (T40), and Span 40 (S40) formed the backbones for niosome preparations. Encapsulation efficiencies (EE), vesicular sizes, in vitro release, and pharmacological activities of niosomal TH preparations were evaluated based on results from the hot plate test. Size distribution analysis showed homogenous vesicles with varied particle size that could be attributed to surfactant type and cholesterol (Chol) content. TH EE increased as a function of the increase in surfactant hydrophilic–lipophilic balance. TH release increased from all formulations as Chol% was increased from 0% to 50%. TH release from niosomal formulations with different surfactant types at 10% Chol increased in a specific order: S40 > S80 > T80 > T40. Following oral administration of TH niosomes to mice, the analgesic effects showed significantly extended effects compared to the TH solution. Oral administration of TH-encapsulated niosomes could be useful for extending the drug's analgesic effects.
Mahmoud M. Ibrahim; Tamer M. Shehata. Tramadol HCl encapsulated niosomes for extended analgesic effect following oral administration. Journal of Drug Delivery Science and Technology 2018, 46, 14 -18.
AMA StyleMahmoud M. Ibrahim, Tamer M. Shehata. Tramadol HCl encapsulated niosomes for extended analgesic effect following oral administration. Journal of Drug Delivery Science and Technology. 2018; 46 ():14-18.
Chicago/Turabian StyleMahmoud M. Ibrahim; Tamer M. Shehata. 2018. "Tramadol HCl encapsulated niosomes for extended analgesic effect following oral administration." Journal of Drug Delivery Science and Technology 46, no. : 14-18.
Tamer Shehata; Omar M.M. Mohafez; Hamza Hanieh. Pharmaceutical Formulation and Biochemical Evaluation of Atorvastatin Transdermal Patches. Indian Journal of Pharmaceutical Education and Research 2018, 52, 54 -61.
AMA StyleTamer Shehata, Omar M.M. Mohafez, Hamza Hanieh. Pharmaceutical Formulation and Biochemical Evaluation of Atorvastatin Transdermal Patches. Indian Journal of Pharmaceutical Education and Research. 2018; 52 (1):54-61.
Chicago/Turabian StyleTamer Shehata; Omar M.M. Mohafez; Hamza Hanieh. 2018. "Pharmaceutical Formulation and Biochemical Evaluation of Atorvastatin Transdermal Patches." Indian Journal of Pharmaceutical Education and Research 52, no. 1: 54-61.
Chronic inflammation in ulcerative colitis (UC) patients is the major risk factor for colitis-associated colon cancer (CAC). Recent evidences have shown that microRNAs (miRNAs) are implicated in CAC pathogenesis. However, the interaction of miRNAs with the transcription factors that alleviate CAC has not been reported. 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or 3,3'-diindolylmethane (DIM) were used to activate aryl hydrocarbon receptor (Ahr) in azoxymethane (AOM)/dextran sodium sulfate (DSS)-induced CAC in mice. Real-time PCR was used to quantify the mRNAs of miRNA and coding genes while western blot and ELISA were used to quantify protein levels. Silencing miRNA was carried out by means of electroporation and locked nucleic acid (LNA)-miRNA. Inducing CAC in mice upregulated miR-132 expression in the colon, spleen and lymph nodes at all stages of disease development. Activation of Ahr by TCDD or DIM boosted miR-132 expression and alleviated CAC severity by suppression of macrophage infiltration and pro-inflammatory cytokines. Interestingly, TCDD, but not DIM, augmented a cholinergic anti-inflammation by inducing acetylcholinesterase (AChE)-targeting miR-132. This anti-inflammation was manifested by suppressed production of TNF-α, IL-1β and IL-6. Silencing miR-132 in vivo in TCDD-treated mice abrogated the cholinergic anti-inflammation and exacerbated CAC. In addition, inhibition of miR-132 in vitro in CD4+ cells and macrophages mitigated the inhibitory effect of TCDD on AChE catalytic activity. Our findings identify miR-132 as a new molecule implicated in CAC pathogenesis, and reveal that miR-132 mediates the ameliorating effects of TCDD on CAC, suggesting miR-132 as a promising therapeutic candidate to control autoimmune inflammation and tumorigenesis in CAC patients.
Abdullah M. Alzahrani; Hamza Hanieh; Hairul-Islam Villianur Ibrahim; Omar Mohafez; Tamer Shehata; Mohammad Bani Ismail; Manal Alfwuaires. Enhancing miR-132 expression by aryl hydrocarbon receptor attenuates tumorigenesis associated with chronic colitis. International Immunopharmacology 2017, 52, 342 -351.
AMA StyleAbdullah M. Alzahrani, Hamza Hanieh, Hairul-Islam Villianur Ibrahim, Omar Mohafez, Tamer Shehata, Mohammad Bani Ismail, Manal Alfwuaires. Enhancing miR-132 expression by aryl hydrocarbon receptor attenuates tumorigenesis associated with chronic colitis. International Immunopharmacology. 2017; 52 ():342-351.
Chicago/Turabian StyleAbdullah M. Alzahrani; Hamza Hanieh; Hairul-Islam Villianur Ibrahim; Omar Mohafez; Tamer Shehata; Mohammad Bani Ismail; Manal Alfwuaires. 2017. "Enhancing miR-132 expression by aryl hydrocarbon receptor attenuates tumorigenesis associated with chronic colitis." International Immunopharmacology 52, no. : 342-351.
Polymeric networks that retain and absorb substantial amount of water or biological fluids and resemble as a biological tissue are defined as hydrogels. On the other hand, liposomes, transfersomes and niosomes are lipid carriers, which represent one of the major research and development focus areas of the pharmaceutical industry. They have great potential as lipid vehicles that are able to enhance permeation of drugs across the intact skin and can act as local depot for the drug to sustain and control its delivery. Lipid carrier and hydrogel combinations offer transdermal drug delivery of great potential to enhance systemic effects of both hydrophilic and lipophilic drugs. Also, lipid carriers can target drugs to skin appendages and improve transdermal delivery. Lipid carrier proform systems in the form of gelly liquid crystals can also be used transdermally for better drug absorption enhancement. This review highlights the potential of hydrogels and emulgels with or without lipid nanocarriers for dermal and transdermal application.
Mahmoud Ibrahim; Anroop B. Nair; Bandar E. Aldhubiab; Tamer Shehata. Hydrogels and Their Combination with Liposomes, Niosomes, or Transfersomes for Dermal and Transdermal Drug Delivery. Liposomes 2017, 1 .
AMA StyleMahmoud Ibrahim, Anroop B. Nair, Bandar E. Aldhubiab, Tamer Shehata. Hydrogels and Their Combination with Liposomes, Niosomes, or Transfersomes for Dermal and Transdermal Drug Delivery. Liposomes. 2017; ():1.
Chicago/Turabian StyleMahmoud Ibrahim; Anroop B. Nair; Bandar E. Aldhubiab; Tamer Shehata. 2017. "Hydrogels and Their Combination with Liposomes, Niosomes, or Transfersomes for Dermal and Transdermal Drug Delivery." Liposomes , no. : 1.
Three different nonionic surfactants (Brij 72, Span 20 and Tween 60) were used to prepare various naked and PEG niosomes. In-vivo study demonstrated that PEGylation dramatically increased the AUC and decreased the affinity to the liver of Brij 72 and Span 20 niosomes in rats. Liver perfusion experiments suggested that the hepatic uptake of naked Brij 72 and Span 20 niosomes could mainly be ascribed to the receptor-mediated uptake, while PEGylation of these niosomes could diminish the receptor-mediated hepatic disposition. Evaluation of serum proteins associated with niosomes revealed that PEGylation of these niosomes significantly reduced the association of serum proteins with them, including typical opsonins such as IgG and C3. On the other hand, in the case of Tween 60 niosomes, naked Tween 60 niosome showed large AUC and its PEGylation did not show any additional effect on the in-vivo pharmacokinetics. Furthermore, PEGylation of Tween 60 niosome did not significantly affect the hepatic disposition or the association of serum proteins with Tween 60 niosome. These results demonstrated that niosomes would exhibit distinct in-vivo disposition characteristics depending on the physicochemical properties of surfactants used and that PEGylation of niosomes with adequate compositions would be a powerful tool to improve their in-vivo behavior.
Tamer Shehata; Toshikiro Kimura; Kazutaka Higaki; Ken-Ichi Ogawara. In-vivo disposition characteristics of PEG niosome and its interaction with serum proteins. International Journal of Pharmaceutics 2016, 512, 322 -328.
AMA StyleTamer Shehata, Toshikiro Kimura, Kazutaka Higaki, Ken-Ichi Ogawara. In-vivo disposition characteristics of PEG niosome and its interaction with serum proteins. International Journal of Pharmaceutics. 2016; 512 (1):322-328.
Chicago/Turabian StyleTamer Shehata; Toshikiro Kimura; Kazutaka Higaki; Ken-Ichi Ogawara. 2016. "In-vivo disposition characteristics of PEG niosome and its interaction with serum proteins." International Journal of Pharmaceutics 512, no. 1: 322-328.
Pharmaceutical development was adopted in the current study to propose a pediatric rectal formulation of sulpiride as a substitute to the available oral or parenteral formulations in the management of Tourette syndrome (TS). The goal was to formulate a product that is easy to use, stable, and highly bioavailable and to achieve a rapid clinical efficacy. Towards this aim, sulpiride solid dispersion (SD) with tartaric acid at a weight ratio of 1:0.25 was incorporated into different suppository bases, namely witepsol W25, witepsol H15, witepsol E75, suppocire NA, suppocire A, glycerogelatin, and polyethylene glycols. The formulae were evaluated in vitro using different pharmacotechnical methods such as visual, melting, weight and content uniformities, drug release, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), and X-ray diffraction (XRD) analyses. In vivo bioavailability was also assessed in rabbits to compare the bioavailability of either raw sulpiride-incorporated or its SD-incorporated witepsol H15-based suppositories to its oral suspension (reference). Sulpiride SD-incorporated witepsol H15 formulation showed acceptable in vitro characteristics with a bioavailability of 117% relative to oral dosing, which excel that in humans (27% after dosing of oral product). In addition, the proposed formula not only passed the 6-month stability study but also proposed a promising scale-up approach. Hence, it showed a great potential for pediatric product development to manage TS in rural areas.
Ahmed S. Zidan; Sherif E. Emam; Tamer Shehata; Fakhr-Eldin S. Ghazy. Pediatric Suppositories of Sulpiride Solid Dispersion for Treatment of Tourette Syndrome: In Vitro and In Vivo Investigations. AAPS PharmSciTech 2014, 16, 645 -655.
AMA StyleAhmed S. Zidan, Sherif E. Emam, Tamer Shehata, Fakhr-Eldin S. Ghazy. Pediatric Suppositories of Sulpiride Solid Dispersion for Treatment of Tourette Syndrome: In Vitro and In Vivo Investigations. AAPS PharmSciTech. 2014; 16 (3):645-655.
Chicago/Turabian StyleAhmed S. Zidan; Sherif E. Emam; Tamer Shehata; Fakhr-Eldin S. Ghazy. 2014. "Pediatric Suppositories of Sulpiride Solid Dispersion for Treatment of Tourette Syndrome: In Vitro and In Vivo Investigations." AAPS PharmSciTech 16, no. 3: 645-655.
2,4-Dichlorophenoxy acetic acid (2,4-D) is a well-known plant auxin which is widely used in plant tissue culture experiments as well as a weed killer and a herbicide. In this study, 2,4-D was rediscovered as a new anti-inflammatory agent through an in silico molecular modeling and docking studies along with drug formulation and in vivo anti-inflammatory inspection. The molecular modeling and docking studies indicated high affinity of 2,4-D toward COX-2 enzyme in a way similar to Ibuprofen, suggesting a higher anti-inflammatory activity. Molecular docking by both MOE 2013.08 and Leadit 2.1.2 revealed excellent binding pattern compared to some of well-known non-steroidal anti-inflammatory drugs. 2,4-D was formulated in different gel bases. In vitro drug release experiments were used to examine the best 2,4-D formula for in vivo studies. In vivo carrageenan-induced hind paw edema inflammatory model in rats was used to test the in silico finding. 2,4-D showed potential in vivo anti-inflammatory activity and significantly reduced the concentration of prostaglandin E2 in hind paw tissues in a way similar to Ibuprofen. These results may open the door to introduce a new anti-inflammatory molecule; especially that 2,4-D is a well-investigated regarding its toxicity and side effect.
Mohammed Khedr; Tamer Shehata; Maged Mohamed. Repositioning of 2,4-Dichlorophenoxy acetic acid as a potential anti-inflammatory agent: In Silico and Pharmaceutical Formulation study. European Journal of Pharmaceutical Sciences 2014, 65, 130 -138.
AMA StyleMohammed Khedr, Tamer Shehata, Maged Mohamed. Repositioning of 2,4-Dichlorophenoxy acetic acid as a potential anti-inflammatory agent: In Silico and Pharmaceutical Formulation study. European Journal of Pharmaceutical Sciences. 2014; 65 ():130-138.
Chicago/Turabian StyleMohammed Khedr; Tamer Shehata; Maged Mohamed. 2014. "Repositioning of 2,4-Dichlorophenoxy acetic acid as a potential anti-inflammatory agent: In Silico and Pharmaceutical Formulation study." European Journal of Pharmaceutical Sciences 65, no. : 130-138.