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Heba Elsewedy
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, 31982 Al-Ahsa, Saudi Arabia

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Journal article
Published: 31 July 2021 in Chemico-Biological Interactions
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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.

ACS Style

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 Style

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.

Chicago/Turabian Style

Nancy 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.

Journal article
Published: 02 July 2021 in Molecules
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Background: Infectious diseases still affect large populations causing significant morbidity and mortality. Bacterial and fungal infections for centuries were the main factors of death and disability of millions of humans. Despite the progress in the control of infectious diseases, the appearance of resistance of microbes to existing drugs creates the need for the development of new effective antimicrobial agents. In an attempt to improve the antibacterial activity of previously synthesized compounds modifications to their structures were performed. Methods: Nineteen thiazolidinone derivatives with 6-Cl, 4-OMe, 6-CN, 6-adamantan, 4-Me, 6-adamantan substituents at benzothiazole ring were synthesized and evaluated against panel of four bacterial strains S. aureus, L. monocytogenes, E. coli and S. typhimirium and three resistant strains MRSA, E. coli and P. aeruginosa in order to improve activity of previously evaluated 6-OCF3-benzothiazole-based thiazolidinones. The evaluation of minimum inhibitory and minimum bactericidal concentration was determined by microdilution method. As reference compounds ampicillin and streptomycin were used. Results: All compounds showed antibacterial activity with MIC in range of 0.12–0.75 mg/mL and MBC at 0.25–>1.00 mg/mL The most active compound among all tested appeared to be compound 18, with MIC at 0.10 mg/mL and MBC at 0.12 mg/mL against P. aeruginosa. as well as against resistant strain P. aeruginosa with MIC at 0.06 mg/mL and MBC at 0.12 mg/mL almost equipotent with streptomycin and better than ampicillin. Docking studies predicted that the inhibition of LD-carboxypeptidase is probably the possible mechanism of antibacterial activity of tested compounds. Conclusion: The best improvement of antibacterial activity after modifications was achieved by replacement of 6-OCF3 substituent in benzothiazole moiety by 6-Cl against S. aureus, MRSA and resistant strain of E. coli by 2.5 folds, while against L. monocytogenes and S. typhimirium from 4 to 5 folds.

ACS Style

Michelyne Haroun; Christophe Tratrat; Anthi Petrou; Athina Geronikaki; Marija Ivanov; Ana Ćirić; Marina Soković; SreeHarsha Nagaraja; Katharigatta Venugopala; Anroop Balachandran Nair; Heba Elsewedy; Hafedh Kochkar. Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation. Molecules 2021, 26, 4061 .

AMA Style

Michelyne Haroun, Christophe Tratrat, Anthi Petrou, Athina Geronikaki, Marija Ivanov, Ana Ćirić, Marina Soković, SreeHarsha Nagaraja, Katharigatta Venugopala, Anroop Balachandran Nair, Heba Elsewedy, Hafedh Kochkar. Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation. Molecules. 2021; 26 (13):4061.

Chicago/Turabian Style

Michelyne Haroun; Christophe Tratrat; Anthi Petrou; Athina Geronikaki; Marija Ivanov; Ana Ćirić; Marina Soković; SreeHarsha Nagaraja; Katharigatta Venugopala; Anroop Balachandran Nair; Heba Elsewedy; Hafedh Kochkar. 2021. "Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation." Molecules 26, no. 13: 4061.

Journal article
Published: 07 June 2021 in Molecules
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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.

ACS Style

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 Style

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 (11):3454.

Chicago/Turabian Style

Tamer 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.

Journal article
Published: 09 April 2021 in Plants
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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.

ACS Style

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 Style

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 (4):735.

Chicago/Turabian Style

Hany 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.

Journal article
Published: 17 March 2021 in Antibiotics
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In this study, we report the design, synthesis, computational and experimental evaluation of the antimicrobial activity, as well as docking studies of new 5-methylthiazole based thiazolidinones. All compounds demonstrated antibacterial efficacy, some of which (1, 4, 10 and 13) exhibited good activity against E. coli and B. cereus. The evaluation of antibacterial activity against three resistant strains, MRSA, P. aeruginosa and E. coli, revealed that compound 12 showed the best activity, higher than reference drugs ampicillin and streptomycin, which were inactive or exhibited only bacteriostatic activity against MRSA, respectively. Ten out of fifteen compounds demonstrated higher potency than reference drugs against a resistant strain of E. coli, which appeared to be the most sensitive species to our compounds. Compounds 8, 13 and 14 applied in a concentration equal to MIC reduced P. aeruginosa biofilm formation by more than 50%. All compounds displayed antifungal activity, with compound 10 being the most active. The majority of compounds showed better activity than ketoconazole against almost all fungal strains. In order to elucidate the mechanism of antibacterial and antifungal activities, molecular docking studies on E. coli Mur B and C. albicans CYP51 and dihydrofolate reductase were performed. Docking analysis of E. coli MurB indicated a probable involvement of MurB inhibition in the antibacterial mechanism of tested compounds while docking to 14α-lanosterol demethylase (CYP51) and tetrahydrofolate reductase of Candida albicans suggested that probable involvement of inhibition of CYP51 reductase in the antifungal activity of the compounds. Potential toxicity toward human cells is also reported.

ACS Style

Michelyne Haroun; Christophe Tratrat; Aggeliki Kolokotroni; Anthi Petrou; Athina Geronikaki; Marija Ivanov; Marina Kostic; Marina Sokovic; Alejandro Carazo; Přemysl Mladěnka; Nagaraja Sreeharsha; Katharigatta Venugopala; Anroop Nair; Heba Elsewedy. 5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies. Antibiotics 2021, 10, 309 .

AMA Style

Michelyne Haroun, Christophe Tratrat, Aggeliki Kolokotroni, Anthi Petrou, Athina Geronikaki, Marija Ivanov, Marina Kostic, Marina Sokovic, Alejandro Carazo, Přemysl Mladěnka, Nagaraja Sreeharsha, Katharigatta Venugopala, Anroop Nair, Heba Elsewedy. 5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies. Antibiotics. 2021; 10 (3):309.

Chicago/Turabian Style

Michelyne Haroun; Christophe Tratrat; Aggeliki Kolokotroni; Anthi Petrou; Athina Geronikaki; Marija Ivanov; Marina Kostic; Marina Sokovic; Alejandro Carazo; Přemysl Mladěnka; Nagaraja Sreeharsha; Katharigatta Venugopala; Anroop Nair; Heba Elsewedy. 2021. "5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies." Antibiotics 10, no. 3: 309.

Journal article
Published: 04 March 2021 in Polymers
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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.

ACS Style

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 Style

Tamer 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 Style

Tamer 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.

Journal article
Published: 14 February 2021 in Polymers
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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.

ACS Style

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 Style

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 (4):577.

Chicago/Turabian Style

Wafaa 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.

Journal article
Published: 09 December 2020 in Journal of Drug Delivery Science and Technology
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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.

ACS Style

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 Style

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.

Chicago/Turabian Style

Tamer 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.

Journal article
Published: 30 September 2020 in Nanomaterials
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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.

ACS Style

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 Style

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 (10):1954.

Chicago/Turabian Style

Wafaa 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.

Journal article
Published: 24 September 2020 in Colloids and Surfaces A: Physicochemical and Engineering Aspects
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Cancer represents one of the most life threatening disease worldwide. Poly ethylene glycol nanoemulsion (PEG-NE), a new drug delivery system (DDS) is widely utilized for encapsulating water insoluble drugs and delivering it into cancerous tissue following its intravenous injection. Brucine (BRU) is an effective anti-carcinogenic agent toward different cancer cell lines; however, its low solubility represents a great obstacle in its formulation. The objective of this investigation was to develop and evaluate BRU-PEG-NE. Physicochemical evaluation including, viscosity, particle size and entrapment efficiency investigations were performed. Quantitative and qualitative estimation of total serum protein adsorbed onto the surface of BRU-NE were performed. In vitro release studies of BRU-NE with and without serum incubation were assayed. Formulations were tested for their cytotoxic activity using MTT assay. Finally, in-vivo anticancer effect was evaluated in tumor-inoculated mice. Homogenous NEs were obtained with particle size less than 140 nm and viscosity less than 3.3 cP for BRU-PEG-NE. Total serum protein adsorbed was less than 17.33 ± 0.76 µg/µmol total lipid for BRU-PEG-NE. In vitro drug release was less than 65% over 24 h for PEG-NE. As well, PEG-NEs could achieve significant inhibition for the viability of cancer cells. Finally, significant reduction in tumor growth rate and mortality rate for BRU PEG-NE formulations were obtained. The obtained results suggested that BRU PEG NE could be considered as a potential mean for cancer therapy.

ACS Style

Heba S. Elsewedy; Bandar E. Al Dhubiab; Mahmoud A. Mahdy; Hanan M. Elnahas. Brucine PEGylated nanoemulsion: In vitro and in vivo evaluation. Colloids and Surfaces A: Physicochemical and Engineering Aspects 2020, 608, 125618 .

AMA Style

Heba S. Elsewedy, Bandar E. Al Dhubiab, Mahmoud A. Mahdy, Hanan M. Elnahas. Brucine PEGylated nanoemulsion: In vitro and in vivo evaluation. Colloids and Surfaces A: Physicochemical and Engineering Aspects. 2020; 608 ():125618.

Chicago/Turabian Style

Heba S. Elsewedy; Bandar E. Al Dhubiab; Mahmoud A. Mahdy; Hanan M. Elnahas. 2020. "Brucine PEGylated nanoemulsion: In vitro and in vivo evaluation." Colloids and Surfaces A: Physicochemical and Engineering Aspects 608, no. : 125618.

Journal article
Published: 02 August 2020 in Applied Sciences
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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.

ACS Style

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 Style

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 (15):5341.

Chicago/Turabian Style

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. 2020. "Vesicular Emulgel Based System for Transdermal Delivery of Insulin: Factorial Design and In Vivo Evaluation." Applied Sciences 10, no. 15: 5341.

Journal article
Published: 13 November 2019 in Pharmaceutics
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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.

ACS Style

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 Style

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 (11):609.

Chicago/Turabian Style

Mohamed 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.

Journal article
Published: 18 April 2019 in Current Topics in Medicinal Chemistry
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Background:Thiazole derivates as well as chalcones, are very important scaffold for medicinal chemistry. Literature survey revealed that they possess wide spectrum of biological activities among which are anti-inflammatory and antimicrobial.Objectives:The current studies describe the synthesis and evaluation of antimicrobial activity of twenty eight novel thiazole-based chalcones.Methods:The designed compounds were synthesized using classical methods of organic synthesis. The in vivo evaluation of antimicrobial activity was performed by microdilution method.Results:All compounds have shown antibacterial properties better than that of ampicillin and in many cases better than streptomycin. As far as the antifungal activity is concerned, all compounds possess much higher activity than reference drugs bifonazole and ketoconazole. The most sensitive bacterial species was B. cereus (MIC 6.5-28.4 µmol × 10-2/mL and MBC 14.2-105.0 µmol × 10-2/mL) while the most resistant ones were L. monocytogenes (MIC 21.4-113.6 µmol × 10-2/mL) and E. coli (MIC 10.7- 113.6 µmol × 10-2/mL) and MBC at 42.7-358.6 µmol × 10-2/mL and 21.4-247.2 µmol × 10-2/mL, respectively. All the compounds exhibited antibacterial activity against the three resistant strains, MRSA, P. aeruginosa and E.coli. with MIC and MBC in the range of 0.65-11.00 µmol/mL × 10-2 and 1.30-16.50 µmol/mL × 10-2. Docking studies were performed.Conclusion:Twenty-eight novel thiazole-based chalcones were designed, synthesized and evaluated for antimicrobial activity. The results showed that these derivatives could be lead compounds in search of new potent antimicrobial agents. Docking studies indicated that DNA gyrase, GyrB and MurA inhibition may explain the antibacterial activity.

ACS Style

Christophe Tratrat; Michelyne Haroun; Iakovos Xenikakis; Konstantinos Liaras; Evangelia Tsolaki; Phaedra Eleftheriou; Anthi Petrou; Bandar Aldhubiab; Mahesh Attimarad; Katharigatta Venugopala; Nagaraja Sreeharsha; Heba Elsewedy; Athina Geronikaki; Marina Sokovic. Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones. Current Topics in Medicinal Chemistry 2019, 19, 356 -375.

AMA Style

Christophe Tratrat, Michelyne Haroun, Iakovos Xenikakis, Konstantinos Liaras, Evangelia Tsolaki, Phaedra Eleftheriou, Anthi Petrou, Bandar Aldhubiab, Mahesh Attimarad, Katharigatta Venugopala, Nagaraja Sreeharsha, Heba Elsewedy, Athina Geronikaki, Marina Sokovic. Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones. Current Topics in Medicinal Chemistry. 2019; 19 (5):356-375.

Chicago/Turabian Style

Christophe Tratrat; Michelyne Haroun; Iakovos Xenikakis; Konstantinos Liaras; Evangelia Tsolaki; Phaedra Eleftheriou; Anthi Petrou; Bandar Aldhubiab; Mahesh Attimarad; Katharigatta Venugopala; Nagaraja Sreeharsha; Heba Elsewedy; Athina Geronikaki; Marina Sokovic. 2019. "Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones." Current Topics in Medicinal Chemistry 19, no. 5: 356-375.

Journal article
Published: 22 March 2018 in Current Topics in Medicinal Chemistry
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Background: Thiazole and benzothiazole derivatives, as well as thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity. Objective: The goal of this paper is the designing of new benzothiazole based thiazolidinones and the evaluation of their biological activities. Methods: The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was evaluated using the method of microdilution. Results: The twelve newly synthesized compounds showed antimicrobial properties. All compounds appeared to be more active than ampicillin in most studied strains and in some cases, more active than streptomycin. Antifungal activity, in most cases was also better than the reference drugs ketoconazole and bifonazole. The prediction of cytotoxicity revealed that the synthesized compounds were not toxic (LD50 350-1000 mg/kg of body weight). Docking studies on the antibacterial activity confirmed the biological results. Conclusion: The twelve new compounds were synthesized and studied for their antimicrobial activity. The compounds appeared to be promising antimicrobial agents and could be the lead compounds for new, more potent drugs. According to the docking prediction, the compounds could be MurB inhibitors.

ACS Style

Michelyne Haroun; Christophe Tratrat; Katerina Kositzi; Evangelia Tsolaki; Anthi Petrou; Bandar Aldhubiab; Mahesh Attimarad; Sree Harsha; Athina Geronikaki; Katharigatta Venugopala; Heba Elsewedy; Marina Sokovic; Jasmina Glamočlija; Ana Ciric. New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation. Current Topics in Medicinal Chemistry 2018, 18, 75 -87.

AMA Style

Michelyne Haroun, Christophe Tratrat, Katerina Kositzi, Evangelia Tsolaki, Anthi Petrou, Bandar Aldhubiab, Mahesh Attimarad, Sree Harsha, Athina Geronikaki, Katharigatta Venugopala, Heba Elsewedy, Marina Sokovic, Jasmina Glamočlija, Ana Ciric. New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation. Current Topics in Medicinal Chemistry. 2018; 18 (1):75-87.

Chicago/Turabian Style

Michelyne Haroun; Christophe Tratrat; Katerina Kositzi; Evangelia Tsolaki; Anthi Petrou; Bandar Aldhubiab; Mahesh Attimarad; Sree Harsha; Athina Geronikaki; Katharigatta Venugopala; Heba Elsewedy; Marina Sokovic; Jasmina Glamočlija; Ana Ciric. 2018. "New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation." Current Topics in Medicinal Chemistry 18, no. 1: 75-87.