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Dr. Mallesh Kurakula
Department of Biomedical Engineering, University of Memphis, Memphis, TN, USA

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0 Biomaterials
0 nanocrystals
0 Chitosan
0 Control drug delivery
0 Spinal/ dental/craniofacial Implants

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Biomaterials

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Journal article
Published: 16 July 2021 in Gels
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(1) Introduction: in recent decades, interdisciplinary research on the utilization of natural products as “active moiety carriers” was focused on due to their superior safety profile, biodegradability, biocompatibility and the ability for sustained or controlled release activity. The nano-based neuroprotective strategy is explored as an imperative treatment for diabetic neuropathy (DN). Avanafil (AV), that selectively inhibits the degradation of cGMP-specific phosphodiesterase, thereby increasing the levels of cGMP, makes a decisive mediator for cytoprotection. (2) Methods: AVnanocomplex formulations were prepared by a modified anti-solvent precipitation method and the method was optimized by Box–Behnken design. An optimized formulation was characterized and evaluated for various in vitro parameters; (3) results:based on the desirability approach, the formulation containing 2.176 g of chitosan, 7.984 g of zein and 90% v/v ethanol concentration can fulfill the prerequisites of optimum formulation (OB-AV-NC).OB-AV-NC was characterized and evaluated for various parameters. The neuroprotective mechanism of AV was evaluated by pretreatment of PC12 cells with plain AV, avanafil nanocomplex (NC) without antioxidants (AV-NC) and with antioxidants (α-Lipoic acid LP; Ellagic Acid EA), AV-LP-EA-Nanocomplex has also shown considerable attenuation in intracellular reactive oxygen species (ROS) and lipid peroxidation with a significant increase in the PC 12 viability under HG conditions in comparison to pure AV; (4) conclusion: the nanocomplex of AV prepared to utilize natural polymers and antioxidants aided for high solubility of AV and exhibited desired neuroprotective activity.This can be one of the promisingstrategy to translate the AV nanocomplex with safety and efficacy in treating DN.

ACS Style

Mallesh Kurakula; Raghavendra Naveen N.; Bhaumik Patel; Ravi Manne; Devang Patel. Preparation, Optimization and Evaluation of Chitosan-Based Avanafil Nanocomplex Utilizing Antioxidants for Enhanced Neuroprotective Effect on PC12 Cells. Gels 2021, 7, 96 .

AMA Style

Mallesh Kurakula, Raghavendra Naveen N., Bhaumik Patel, Ravi Manne, Devang Patel. Preparation, Optimization and Evaluation of Chitosan-Based Avanafil Nanocomplex Utilizing Antioxidants for Enhanced Neuroprotective Effect on PC12 Cells. Gels. 2021; 7 (3):96.

Chicago/Turabian Style

Mallesh Kurakula; Raghavendra Naveen N.; Bhaumik Patel; Ravi Manne; Devang Patel. 2021. "Preparation, Optimization and Evaluation of Chitosan-Based Avanafil Nanocomplex Utilizing Antioxidants for Enhanced Neuroprotective Effect on PC12 Cells." Gels 7, no. 3: 96.

Review
Published: 29 June 2021 in Plants
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Raspberry ketone (RK) is an aromatic phenolic compound naturally occurring in red raspberries, kiwifruit, peaches, and apples and reported for its potential therapeutic and nutraceutical properties. Studies in cells and rodents have suggested an important role for RK in hepatic/cardio/gastric protection and as an anti-hyperlipidemic, anti-obesity, depigmentation, and sexual maturation agent. Raspberry ketone-mediated activation of peroxisome proliferator-activated receptor-α (PPAR-α) stands out as one of its main modes of action. Although rodent studies have demonstrated the efficacious effects of RK, its mechanism remains largely unknown. In spite of a lack of reliable human research, RK is marketed as a health supplement, at very high doses. In this review, we provide a compilation of scientific research that has been conducted so far, assessing the therapeutic properties of RK in several disease conditions as well as inspiring future research before RK can be considered safe and efficacious with limited side effects as an alternative to modern medicines in the treatment of major lifestyle-based diseases.

ACS Style

Shailaja Rao; Mallesh Kurakula; Nagarjuna Mamidipalli; Papireddy Tiyyagura; Bhaumik Patel; Ravi Manne. Pharmacological Exploration of Phenolic Compound: Raspberry Ketone—Update 2020. Plants 2021, 10, 1323 .

AMA Style

Shailaja Rao, Mallesh Kurakula, Nagarjuna Mamidipalli, Papireddy Tiyyagura, Bhaumik Patel, Ravi Manne. Pharmacological Exploration of Phenolic Compound: Raspberry Ketone—Update 2020. Plants. 2021; 10 (7):1323.

Chicago/Turabian Style

Shailaja Rao; Mallesh Kurakula; Nagarjuna Mamidipalli; Papireddy Tiyyagura; Bhaumik Patel; Ravi Manne. 2021. "Pharmacological Exploration of Phenolic Compound: Raspberry Ketone—Update 2020." Plants 10, no. 7: 1323.

Review
Published: 15 June 2021 in Polysaccharides
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Spinal cord injury (SCI) is one of the most complicated nervous system injuries with challenging treatment and recovery. Regenerative biomaterials such as chitosan are being reported for their wide use in filling the cavities, deliver curative drugs, and also provide adsorption sites for transplanted stem cells. Biomaterial scaffolds utilizing chitosan have shown certain therapeutic effects on spinal cord injury repair with some limitations. Chitosan-based delivery in stem cell transplantation is another strategy that has shown decent success. Stem cells can be directed to differentiate into neurons or glia in vitro. Stem cell-based therapy, biopolymer chitosan delivery strategies, and scaffold-based therapeutic strategies have been advancing as a combinatorial approach for spinal cord injury repair. In this review, we summarize the recent progress in the treatment strategies of SCI due to the use of bioactivity of chitosan-based drug delivery systems. An emphasis on the role of chitosan in neural regeneration has also been highlighted.

ACS Style

Mallesh Kurakula; Shashank Gorityala; Devang Patel; Pratap Basim; Bhaumik Patel; Saurabh Kumar Jha. Trends of Chitosan Based Delivery Systems in Neuroregeneration and Functional Recovery in Spinal Cord Injuries. Polysaccharides 2021, 2, 519 -537.

AMA Style

Mallesh Kurakula, Shashank Gorityala, Devang Patel, Pratap Basim, Bhaumik Patel, Saurabh Kumar Jha. Trends of Chitosan Based Delivery Systems in Neuroregeneration and Functional Recovery in Spinal Cord Injuries. Polysaccharides. 2021; 2 (2):519-537.

Chicago/Turabian Style

Mallesh Kurakula; Shashank Gorityala; Devang Patel; Pratap Basim; Bhaumik Patel; Saurabh Kumar Jha. 2021. "Trends of Chitosan Based Delivery Systems in Neuroregeneration and Functional Recovery in Spinal Cord Injuries." Polysaccharides 2, no. 2: 519-537.

Journal article
Published: 08 June 2021 in Pharmaceutics
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Vascular and traumatic injuries of the central nervous system are recognized as global health priorities. A polypharmacology approach that is able to simultaneously target several injury factors by the combination of agents having synergistic effects appears to be promising. Herein, we designed a polymeric delivery system loaded with two drugs, ibuprofen (Ibu) and thyroid hormone triiodothyronine (T3) to in vitro release the suitable amount of the anti-inflammation and the remyelination drug. As a production method, electrospinning technology was used. First, Ibu-loaded micro (diameter circa 0.95–1.20 µm) and nano (diameter circa 0.70 µm) fibers were produced using poly(l-lactide) PLLA and PLGA with different lactide/glycolide ratios (50:50, 75:25, and 85:15) to select the most suitable polymer and fiber diameter. Based on the in vitro release results and in-house knowledge, PLLA nanofibers (mean diameter = 580 ± 120 nm) loaded with both Ibu and T3 were then successfully produced by a co-axial electrospinning technique. The in vitro release studies demonstrated that the final Ibu/T3 PLLA system extended the release of both drugs for 14 days, providing the target sustained release. Finally, studies in cell cultures (RAW macrophages and neural stem cell-derived oligodendrocyte precursor cells—OPCs) demonstrated the anti-inflammatory and promyelinating efficacy of the dual drug-loaded delivery platform.

ACS Style

Luisa Dolci; Rosaria Perone; Roberto Di Gesù; Mallesh Kurakula; Chiara Gualandi; Elisa Zironi; Teresa Gazzotti; Maria Tondo; Giampiero Pagliuca; Natalia Gostynska; Vito Baldassarro; Maura Cescatti; Luciana Giardino; Maria Focarete; Laura Calzà; Nadia Passerini; Maria Bolognesi. Design and In Vitro Study of a Dual Drug-Loaded Delivery System Produced by Electrospinning for the Treatment of Acute Injuries of the Central Nervous System. Pharmaceutics 2021, 13, 848 .

AMA Style

Luisa Dolci, Rosaria Perone, Roberto Di Gesù, Mallesh Kurakula, Chiara Gualandi, Elisa Zironi, Teresa Gazzotti, Maria Tondo, Giampiero Pagliuca, Natalia Gostynska, Vito Baldassarro, Maura Cescatti, Luciana Giardino, Maria Focarete, Laura Calzà, Nadia Passerini, Maria Bolognesi. Design and In Vitro Study of a Dual Drug-Loaded Delivery System Produced by Electrospinning for the Treatment of Acute Injuries of the Central Nervous System. Pharmaceutics. 2021; 13 (6):848.

Chicago/Turabian Style

Luisa Dolci; Rosaria Perone; Roberto Di Gesù; Mallesh Kurakula; Chiara Gualandi; Elisa Zironi; Teresa Gazzotti; Maria Tondo; Giampiero Pagliuca; Natalia Gostynska; Vito Baldassarro; Maura Cescatti; Luciana Giardino; Maria Focarete; Laura Calzà; Nadia Passerini; Maria Bolognesi. 2021. "Design and In Vitro Study of a Dual Drug-Loaded Delivery System Produced by Electrospinning for the Treatment of Acute Injuries of the Central Nervous System." Pharmaceutics 13, no. 6: 848.

Review article
Published: 31 May 2021 in Journal of Drug Delivery Science and Technology
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Colon-targeted drug delivery systems is an active area of research that is designed to selectively release the drug in the colonic environment to enhance the oral delivery of active drug moieties which are vulnerable to the acidic environment in the upper gastrointestinal tract. It is continuing to progress and address the needs of the diseases affecting the colon especially owing to the design and development of novel colon-targeted delivery systems based on natural biodegradable polymers. Chitosan is a key biopolymer that has been widely exploited for the delivery of drugs, peptides, protein, and genes to the colon. In the current review, the emphasis has been placed on the role of chitosan in the design of colon targeting drugs and a comprehensive overview of chitosan-based colon-specific formulations and recent developments are captured. This review will provide a brief overview of previous applications, current trends, and the recent developments that have emerged in the chitosan-based colon targeted delivery system. We anticipate the future developments and new research areas surrounding the chitosan-based delivery systems that can strengthen the applicability of this polymer in new drug modalities.

ACS Style

Mallesh Kurakula; Shashank Gorityala; Keshav Moharir. Recent trends in design and evaluation of chitosan-based colon targeted drug delivery systems: Update 2020. Journal of Drug Delivery Science and Technology 2021, 64, 102579 .

AMA Style

Mallesh Kurakula, Shashank Gorityala, Keshav Moharir. Recent trends in design and evaluation of chitosan-based colon targeted drug delivery systems: Update 2020. Journal of Drug Delivery Science and Technology. 2021; 64 ():102579.

Chicago/Turabian Style

Mallesh Kurakula; Shashank Gorityala; Keshav Moharir. 2021. "Recent trends in design and evaluation of chitosan-based colon targeted drug delivery systems: Update 2020." Journal of Drug Delivery Science and Technology 64, no. : 102579.

Review article
Published: 13 February 2021 in European Polymer Journal
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Chitosan (CS) a promising biopolymer has been explored for wide biomedical applications using different technologies. Electrospraying is one of the advancing liquid atomization-based techniquesrapidly merging in fields of biomedicine, especially in drug delivery and biomedical applications. Recent studies revealed that wide therapeutics such as antibiotics, anticancer, bioactives (enzymes, growth factors, genes, cells) were successfully loaded and delivered by CS using electrospraying. Apart from the exploration of CS bioactivity in drug delivery, we attempt to brief about the electrospraying technology, parameters regulating final product quality, types of polymers used, advantages, and limitations. The scrutiny highlights different conventional to controlled delivery systems fabricated by electrosprayed CS alone or in combination with other co-polymers. Further, the comprehensive addresses the different biomedical applications like wound healing, tissue engineering, coatings for antimicrobial, bone regeneration, as dental coatings, or surface modifications based on electrosprayed CS. In comparison to other methods, CS-based coating by electrospraying technique has helped to achieve desired properties for specific functions moving many processes to product commercialization. Exploration of patents filed and published from the past decade (2009–2020) based on the electrosprayed CS in the drug delivery are listed and the trends are reported. The review is concluded with an insightful outlook and future perspective of electrosprayed CS products for their broad applications, high coherence, and safe fabrication.

ACS Style

Mallesh Kurakula; N. Raghavendra Naveen. Electrospraying: A facile technology unfolding the chitosan based drug delivery and biomedical applications. European Polymer Journal 2021, 147, 110326 .

AMA Style

Mallesh Kurakula, N. Raghavendra Naveen. Electrospraying: A facile technology unfolding the chitosan based drug delivery and biomedical applications. European Polymer Journal. 2021; 147 ():110326.

Chicago/Turabian Style

Mallesh Kurakula; N. Raghavendra Naveen. 2021. "Electrospraying: A facile technology unfolding the chitosan based drug delivery and biomedical applications." European Polymer Journal 147, no. : 110326.

Chapter
Published: 14 November 2020 in Probiotic Research in Therapeutics
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Lung cancer is one of the major causes of mortality and morbidity worldwide adding a significant burden on healthcare cost. Apart from conventional and chemotherapy strategies, use of probiotics as an adjunct therapy for prevention or treatment of tumours was a game changer with scientific proofs from diverse research groups. Probiotics are the specific bacterial or fungal strains—live or dead, along with their metabolites when consumed at certain concentrations indicated proven health benefits. Probiotics are being recognized for their repurposing advantages having immunomodulatory responses and reported as alternative for cancer biotherapeutics. In this chapter, the proposed mechanisms of probiotics’ use in lung cancer therapy during proliferation, metastasis, and immunomodulation are discussed. A spolight on the elucidation of probiotics as potential candidates in the management of pulmonary tumour, highlighting relevant in vitro (cell line studies) and in vivo (animal and human trials) studies. New emerging trends using bioengineering recombinant approach of probiotic bacteria against respiratory cancer, their limitations, and future prospectus are outlined in the current chapter.

ACS Style

Mallesh Kurakula; G. S. N. Koteswara Rao. Probiotics in Lung Cancer: An Emerging Field of Multifarious Potential and Opportunities. Probiotic Research in Therapeutics 2020, 125 -158.

AMA Style

Mallesh Kurakula, G. S. N. Koteswara Rao. Probiotics in Lung Cancer: An Emerging Field of Multifarious Potential and Opportunities. Probiotic Research in Therapeutics. 2020; ():125-158.

Chicago/Turabian Style

Mallesh Kurakula; G. S. N. Koteswara Rao. 2020. "Probiotics in Lung Cancer: An Emerging Field of Multifarious Potential and Opportunities." Probiotic Research in Therapeutics , no. : 125-158.

Review article
Published: 15 October 2020 in International Journal of Biological Macromolecules
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Improved accuracy is one of the vital innovations in designing biopolymer-based products that are gaining momentum in diverse biomedicine arenas. The innovative devices were developed utilizing synthetic polymers but now are replaced with ‘green polymer’ such as chitosan. These bioactive polymer-based products can control release therapeutics, even greatly minimize the post-surgery inflammations, immune responses, and are biodegradable. Past decade to date, numerous proprietary technologies have been developed and protected by numerous patents. Therefore, strategical analysis of these chitosan-based process or product patent helps to identify key innovative technologies, clinically implementation, and key manufacturers behind these biomedical products. The present article analyzed the trends in patent portfolios of chitosan-based biomedical products and the number of original research papers published over a decade. A spotlight on different marketed grades, modifications for their special use, blend composites, safety profile, and regulatory concerns of chitosan use in bioengineering are covered. A scientific prospection was performed between 2009 and 2020 using the PubMed database. For technological prospection, Lens (free, open patent, and scholarly search) portal was utilized. Chitosan-originated patents were analyzed using cooperative and international patent classifications, covering their citations by patent count. Various chitosan-based patents that are approved and commercial chitosan based biomedical products are even listed. A preliminary perusal of chitosan alone or based patent portfolios can greatly benefit various stakeholders like scientists and corporate firms for new product development, government agencies for allocation of federal funds shaping up biomedicine advances by utilizing chitosan. The present analysis indicates the overall progression and unexplored corners of chitosan in a current global biomedical proposition.

ACS Style

Mallesh Kurakula; Naveen Raghavendra N.. Prospection of recent chitosan biomedical trends: Evidence from patent analysis (2009–2020). International Journal of Biological Macromolecules 2020, 165, 1924 -1938.

AMA Style

Mallesh Kurakula, Naveen Raghavendra N.. Prospection of recent chitosan biomedical trends: Evidence from patent analysis (2009–2020). International Journal of Biological Macromolecules. 2020; 165 ():1924-1938.

Chicago/Turabian Style

Mallesh Kurakula; Naveen Raghavendra N.. 2020. "Prospection of recent chitosan biomedical trends: Evidence from patent analysis (2009–2020)." International Journal of Biological Macromolecules 165, no. : 1924-1938.

Review article
Published: 02 September 2020 in Journal of Drug Delivery Science and Technology
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Polyvinylpyrrolidone (PVP) is a water-soluble polymer obtained by polymerization of monomer N-vinylpyrrolidone. PVP is an inert, non-toxic, temperature-resistant, pH-stable, biocompatible, biodegradable polymer that helps to encapsulate and cater both hydrophilic and lipophilic drugs. These advantages enable PVP a versatile excipient in the formulation development of broad conventional to novel controlled delivery systems. PVP has tunable properties and can be used as a brace component for gene delivery, orthopedic implants, and tissue engineering applications. Based on different molecular weights and modified forms, PVP can lead to exceptional beneficial features with varying chemical properties. Graft copolymerization and other techniques assist PVP to conjugate with poorly soluble drugs that can inflate bioavailability and even introduces the desired swelling tract for their control or sustained release. The present review provides chemistry, mechanical, physicochemical properties, evaluation parameters, dewy preparation methods of PVP derivatives intended for designing conventional to controlled systems for drug, gene, and cosmetic delivery. The past and growing interest in PVP establishes it as a promising polymer to enhance the trait and performance of current generation pharmaceutical dosage forms. Furthermore, the scrutiny explores existing patents, marketed products, new and futuristic approaches of PVP that have been identified and scope for future development, characterization, and its use. The exploration spotlights the importance and role of PVP in the design of Povidone-iodine (PVP–I) and clinical trials to assess therapeutic efficacy against the COVID-19 in the current pandemic scenario.

ACS Style

Mallesh Kurakula; G.S.N. Koteswara Rao. Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition. Journal of Drug Delivery Science and Technology 2020, 60, 102046 -102046.

AMA Style

Mallesh Kurakula, G.S.N. Koteswara Rao. Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition. Journal of Drug Delivery Science and Technology. 2020; 60 ():102046-102046.

Chicago/Turabian Style

Mallesh Kurakula; G.S.N. Koteswara Rao. 2020. "Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition." Journal of Drug Delivery Science and Technology 60, no. : 102046-102046.

Review article
Published: 01 August 2020 in European Polymer Journal
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With emerging technological advances in biomedicine, the scope of futuristic biomaterials has been limited and existing polymers are gaining momentum. Unlike other synthetic polymers, polyvinyl pyrrolidone (PVP) is bioactive, water-soluble, non-toxic, temperature-resistant, pH-stable, biodegradable, and biocompatible. Due to its versatile properties, PVP is explored and widely used in the fabrication of wide biomedical products via electrospinning, 3D/4D printing, and other technologies. PVP owes intrinsic biological and tunable properties with next-generation biomaterials as nanoscaffolds delivering wide therapeutics, supporting material in implants, as a bone spacer, in tissue regeneration, wound healing materials, in diagnostics and many more. Several modifications of PVP are reported to achieve the additional criteria for special functions and additive with other clinically approved polymers to obtain new biomedical products. This article is a literature review on the PVP use in designing multidisciplinary biomedical products via advanced approaches. The review details key research aspects and promising potentials of PVP based nanoscaffolds utilized in several biomedical implants (orthopedic, dental, vaginal, breast), regenerative engineering (neural, cardiac, and pancreatic tissue), ophthalmic, wound healing materials, theranostics and miscellaneous. A special focus on novel PVP biomedical products by emerging, sustainable, cost-effective 3D and 4D printing are highlighted. From a biomedical scientist’s viewpoint, this review presents, the current challenges, outlook, and future prospective of PVP in designing bioresorbable devices.

ACS Style

Mallesh Kurakula; G.S.N. Koteswara Rao. Moving polyvinyl pyrrolidone electrospun nanofibers and bioprinted scaffolds toward multidisciplinary biomedical applications. European Polymer Journal 2020, 136, 109919 .

AMA Style

Mallesh Kurakula, G.S.N. Koteswara Rao. Moving polyvinyl pyrrolidone electrospun nanofibers and bioprinted scaffolds toward multidisciplinary biomedical applications. European Polymer Journal. 2020; 136 ():109919.

Chicago/Turabian Style

Mallesh Kurakula; G.S.N. Koteswara Rao. 2020. "Moving polyvinyl pyrrolidone electrospun nanofibers and bioprinted scaffolds toward multidisciplinary biomedical applications." European Polymer Journal 136, no. : 109919.

Journal article
Published: 09 July 2020 in Pharmaceutics
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This study aimed at improving the targeting and cytotoxic effect of ellagic acid (EA) on colon cancer cells. EA was encapsulated in chitosan (CHIT) polymers then coated by eudragit S100 (ES100) microparticles. The release of EA double-coated microparticles (MPs) was tested at simulative pH values. Maximum release was observed at 24 h and pH 7.4. The cytotoxicity of EA MPs on HCT 116 colon cancer cells was synergistically improved as compared with raw EA. Cell-cycle analysis by flow cytometry suggested enhanced G2-M phase colon cancer cell accumulation. In addition, a significantly higher cell fraction was observed in the pre-G phase, which highlighted the enhancement of the proapoptotic activity of EA formulated in the double-coat mixture. Annexin-V staining was used for substantiation of the observed cell-death-inducing activity. Cell fractions were significantly increased in early, late, and total cell death. This was backed by high elevation in cellular content of caspase 3. Effectiveness of the double-coated EA to target colonic tissues was confirmed using real-time iohexol dye X-ray radiography. In conclusion, CHIT loaded with EA and coated with ES100 formula exhibits improved colon targeting as well as enhanced cytotoxic and proapoptotic activity against HCT 116 colon cancer when compared with the administration of raw EA.

ACS Style

Nabil Alhakamy; Osama Ahmed; Mallesh Kurakula; Giuseppe Caruso; Filippo Caraci; Hani Asfour; Anas Alfarsi; Basma Eid; Amir Mohamed; Nabil Alruwaili; Wesam Abdulaal; Usama Fahmy; Hani Alhadrami; Basmah Eldakhakhny; Ashraf Abdel-Naim. Chitosan-Based Microparticles Enhance Ellagic Acid’s Colon Targeting and Proapoptotic Activity. Pharmaceutics 2020, 12, 652 .

AMA Style

Nabil Alhakamy, Osama Ahmed, Mallesh Kurakula, Giuseppe Caruso, Filippo Caraci, Hani Asfour, Anas Alfarsi, Basma Eid, Amir Mohamed, Nabil Alruwaili, Wesam Abdulaal, Usama Fahmy, Hani Alhadrami, Basmah Eldakhakhny, Ashraf Abdel-Naim. Chitosan-Based Microparticles Enhance Ellagic Acid’s Colon Targeting and Proapoptotic Activity. Pharmaceutics. 2020; 12 (7):652.

Chicago/Turabian Style

Nabil Alhakamy; Osama Ahmed; Mallesh Kurakula; Giuseppe Caruso; Filippo Caraci; Hani Asfour; Anas Alfarsi; Basma Eid; Amir Mohamed; Nabil Alruwaili; Wesam Abdulaal; Usama Fahmy; Hani Alhadrami; Basmah Eldakhakhny; Ashraf Abdel-Naim. 2020. "Chitosan-Based Microparticles Enhance Ellagic Acid’s Colon Targeting and Proapoptotic Activity." Pharmaceutics 12, no. 7: 652.

Journal article
Published: 24 April 2020 in Marine Drugs
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This work aimed at improving the targeting and cytotoxicity of simvastatin (SMV) against colon cancer cells. SMV was encapsulated in chitosan polymers, followed by eudragit S100 microparticles. The release of SMV double coated microparticles was dependent on time and pH. At pH 7.4 maximum release was observed for 6 h. The efficiency of the double coat to target colonic tissues was confirmed using real-time X-ray radiography of iohexol dye. Entrapment efficiency and particle size were used in the characterization of the formula. Cytotoxicity of SMV microparticles against HCT-116 colon cancer cells was significantly improved as compared to raw SMV. Cell cycle analysis by flow cytomeric technique indicated enhanced accumulation of colon cancer cells in the G2/M phase. Additionally, a significantly higher cell fraction was observed in the pre-G phase, which highlighted enhancement of the proapoptotic activity of SMV prepared in the double coat formula. Assessment of annexin V staining was used for confirmation. Cell fraction in early, late and total cell death were significantly elevated. This was accompanied by a significant elevation of cellular caspase 3 activity. In conclusion, SMV-loaded chitosan coated with eudragit S100 formula exhibited improved colon targeting and enhanced cytotoxicity and proapoptotic activity against HCT-116 colon cancer cells.

ACS Style

Nabil A. Alhakamy; Usama A. Fahmy; Osama A. A. Ahmed; Giuseppe Caruso; Filippo Caraci; Hani Z. Asfour; Muhammed A. Bakhrebah; Mohammad N. Alomary; Wesam H. Abdulaal; Solomon Z. Okbazghi; Ashraf B. Abdel-Naim; Basma G. Eid; Hibah M. Aldawsari; Mallesh Kurakula; Amir I. Mohamed. Chitosan Coated Microparticles Enhance Simvastatin Colon Targeting and Pro-Apoptotic Activity. Marine Drugs 2020, 18, 226 .

AMA Style

Nabil A. Alhakamy, Usama A. Fahmy, Osama A. A. Ahmed, Giuseppe Caruso, Filippo Caraci, Hani Z. Asfour, Muhammed A. Bakhrebah, Mohammad N. Alomary, Wesam H. Abdulaal, Solomon Z. Okbazghi, Ashraf B. Abdel-Naim, Basma G. Eid, Hibah M. Aldawsari, Mallesh Kurakula, Amir I. Mohamed. Chitosan Coated Microparticles Enhance Simvastatin Colon Targeting and Pro-Apoptotic Activity. Marine Drugs. 2020; 18 (4):226.

Chicago/Turabian Style

Nabil A. Alhakamy; Usama A. Fahmy; Osama A. A. Ahmed; Giuseppe Caruso; Filippo Caraci; Hani Z. Asfour; Muhammed A. Bakhrebah; Mohammad N. Alomary; Wesam H. Abdulaal; Solomon Z. Okbazghi; Ashraf B. Abdel-Naim; Basma G. Eid; Hibah M. Aldawsari; Mallesh Kurakula; Amir I. Mohamed. 2020. "Chitosan Coated Microparticles Enhance Simvastatin Colon Targeting and Pro-Apoptotic Activity." Marine Drugs 18, no. 4: 226.

Journal article
Published: 09 April 2020 in Marine Drugs
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The goal of this study is to develop optimized chitosan-coated Simvastatin (SIM) nanoparticles (NPs) loaded in an in situ gel (ISG) formulation via a face-centered central composite design (FCCCD). Coated SIM-NPs were doped with Quercetin (QRC) using a modified nanoprecipitation method. The concentrations of poloxamer 188 (A) and chitosan (B) at five different levels, plus/minus alpha (+1.414 and −1.414: axial points), plus/minus 1 (factorial points) and the center point were optimized for particle size (PS-Y1), entrapment efficacy (EE-Y2) and stability index (SI-Y3). Based on the desirability approach, a formulation containing poloxamer 188 0.24% and chitosan 0.43% renders the prerequisites of optimum formulation for preparing SIM–QRC NP-loaded ISG. Scanning microscopy showed spherical SIM-NPs, indicating monodispersity in the range of 0.50 ± 0.04 nm with a charge of +32.42 mV. The optimized formulation indicated the highest EE 79.67% and better stability at 4 °C. Drug release from SIM–QRC NP-loaded ISG was slower to plateau by up to 96 h and, at the end of 168 h, only 65.12% of SIM was released in a more controlled manner in comparison to SIM–QRC NPs and plain SIM. ISG formulation showed a considerable increase in apoptosis occurrence through caspase-3 mediation and it also enhanced the tumor suppressor protein levels. Enhanced biological activity of SIM was observed due to QRC enabling promising drug and polymer synergistic interaction. The proposed formulation can provide a breakthrough in localized therapy, overcoming the potential drawbacks of systemic chemotherapy for tongue carcinoma.

ACS Style

Mallesh Kurakula; N. Raghavendra Naveen. In Situ Gel Loaded with Chitosan-Coated Simvastatin Nanoparticles: Promising Delivery for Effective Anti-Proliferative Activity against Tongue Carcinoma. Marine Drugs 2020, 18, 201 .

AMA Style

Mallesh Kurakula, N. Raghavendra Naveen. In Situ Gel Loaded with Chitosan-Coated Simvastatin Nanoparticles: Promising Delivery for Effective Anti-Proliferative Activity against Tongue Carcinoma. Marine Drugs. 2020; 18 (4):201.

Chicago/Turabian Style

Mallesh Kurakula; N. Raghavendra Naveen. 2020. "In Situ Gel Loaded with Chitosan-Coated Simvastatin Nanoparticles: Promising Delivery for Effective Anti-Proliferative Activity against Tongue Carcinoma." Marine Drugs 18, no. 4: 201.

Journal article
Published: 09 March 2020 in Processes
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The success of mucoadhesive drug delivery systems relies on the type of polymer used, which becomes adhesive naturally upon hydration. Intended polymers should be able to maintain prolonged contact with biological membranes, and to protect or cater the drug to a prolonged period. Most of the hydro polymers form weak non-covalent bonds, that hinder localization of dosage forms at specific sites resulting in therapeutic inefficiency. This can be overcome by the thiol functionalization of natural polymers. In the present study, natural okra gum (OG) was extracted, followed by thiolation (TOG) and evaluated for mucoadhesion property and its role in enhancing the efficacy of repaglinide as a model drug (short-acting Type II antidiabetic drug). The thiol functionalization of OG (TOG) was confirmed by a Fourier-transform infrared spectroscopy (FTIR) study that showed a polyhedral to a spherical shape that had a rougher surface. Differential scanning calorimetry (DSC) and X-Ray Diffraction (XRD) studies of TOG indicated a decline in endothermic transition temperature and high crystallinity, respectively, in comparison to OG. CSFR (Crushing Strength: Friability Ratio), weight and thickness variations of repaglinidetablets formulated using TOG were >80% and

ACS Style

N. Raghavendra Naveen; Chakka Gopinath; Mallesh Kurakula. Okra-Thioglycolic Acid Conjugate—Synthesis, Characterization, and Evaluation as a Mucoadhesive Polymer. Processes 2020, 8, 316 .

AMA Style

N. Raghavendra Naveen, Chakka Gopinath, Mallesh Kurakula. Okra-Thioglycolic Acid Conjugate—Synthesis, Characterization, and Evaluation as a Mucoadhesive Polymer. Processes. 2020; 8 (3):316.

Chicago/Turabian Style

N. Raghavendra Naveen; Chakka Gopinath; Mallesh Kurakula. 2020. "Okra-Thioglycolic Acid Conjugate—Synthesis, Characterization, and Evaluation as a Mucoadhesive Polymer." Processes 8, no. 3: 316.