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