Faculty Publications

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Author: search.filters.author.Nayak, U.Y.Has files: No

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    Tailoring solulan C24 based niosomes for transdermal delivery of donepezil: In vitro characterization, evaluation of pH sensitivity, and microneedle-assisted Ex vivo permeation studies
    (Editions de Sante editions.de.sante@wanadoo.fr, 2020) Nayak, A.S.; Chodisetti, S.; Gadag, S.; Nayak, U.Y.; Srinikethan, S.; Raval, K.
    The present investigation aims at encapsulating donepezil (DNP) in a niosomes to avert the side effects and to deliver the intact carrier across the skin barrier by modulating its physicochemical properties. The finding conclusively demonstrated that entrapment efficiency and the alteration in the niosome size are associated with the change in the span 60: cholesterol ratio, sonication, and hydration volume. The addition of 5 mM of solulan C24 to the optimized formulation (NSV5SolC24) formed stable niosomes with a mean particle size of 180.1 ± 1.83 nm and entrapment efficiency of 82.15% ± 1.54%. The cryo-SEM image and in vitro drug release profile revealed that the NSV5SolC24 is pH-sensitive. FTIR spectral analysis of NSV5SolC24 suggested that the ether and ester group in the NSV5SolC24 complex undergoes SN2 cleavage and hydrolysis at lower pH, thus enhancing DNP release. The microneedle (MN)-assisted studies with MN1200 showed a 29-fold increase in transdermal permeation of intact NSV5SolC24 against the passive method in porcine skin. The intact NSV5SolC24 carrying DNP was translocated across the skin barrier successfully at a steady flux rate of 9.89 ± 0.923 ?g/cm2/h. Nevertheless, further in vivo studies are recommended to elucidate the pH sensitivity and clinical efficacy of the prepared drug delivery system. © 2020 Elsevier B.V.
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    Development and preclinical evaluation of microneedle-assisted resveratrol loaded nanostructured lipid carriers for localized delivery to breast cancer therapy
    (Elsevier B.V., 2021) Gadag, S.; Narayan, R.; Nayak, A.S.; Catalina Ardila, D.; Sant, S.; Yogendra, Y.; Garg, S.; Nayak, U.Y.
    Resveratrol (RVT) is one of the potent anticancer phytochemicals which has shown promising potential for breast cancer therapy. However, its short half-life and low bioavailability is a major hurdle in its effective use. In this study, we have developed nanostructured lipid carriers (NLCs) of RVT to enable localized delivery of the drug to the breast tissues using microneedle arrays to improve effectiveness. The NLCs were optimized using the Design of Experiments approach and characterized for their particle size, polydispersity index, zeta potential and entrapment efficiency. The RVT-NLCs delivered using microneedle array 1200 showed a higher permeation of RVT across the skin with lower skin retention compared to pure RVT. Further, RVT-NLCs showed higher anticancer activity on MDA-MB-231 breast cancer cell lines and enhanced internalization compared to pure RVT. Moreover, the RVT-NLCs were found to inhibit the migration of MDA-MB-231 breast cancer cell lines. Preclinical studies in rats showed that RVT-NLCs delivered via microneedles demonstrated a remarkable increase in the Cmax, Tmax and AUC0-inf, and a higher localization in breast tissue compared to pure RVT administered orally. These results suggests that the RVT-NLCs administered by microneedle array system is an effective strategy for the local delivery of RVT for breast cancer therapy. © 2021 Elsevier B.V.
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    In Silico Studies of (Z)-3-(2-Chloro-4-Nitrophenyl)-5-(4-Nitrobenzylidene)-2-Thioxothiazolidin-4-One Derivatives as PPAR-γ Agonist: Design, Molecular Docking, MM-GBSA Assay, Toxicity Predictions, DFT Calculations and MD Simulation Studies
    (World Scientific, 2024) Gowdru Srinivasa, M.G.; Naik, S.; Udayakumar, U.; Mehta, C.H.; Nayak, U.Y.; Revanasiddappa, B.C.
    Diabetes mellitus, a metabolic disorder, arises from insufficient insulin levels or increased insulin resistance. An alternative approach to address this pathogenesis involves targeting PPAR-γ, which activates glucose homeostasis and improves peripheral glucose utilization. In this study, we aimed to investigate the designed 2-thioxothiazolidin-4-one derivatives (T1-25) and assess their potential as PPAR-γ regulators by an in silico approach. Physicochemical properties and Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) profiles were evaluated. Docking studies were performed using Schrödinger software, with the protein target being PPAR-γ (PDB ID: 2ZNO). Additionally, MD simulation studies were conducted, and the key interactions in the protein-ligand complexes were identified. The results demonstrate the drug-likeness of compounds T11, T24 and T25, with docking scores of -7.953 kcal/mol, -7.973 kcal/ mol and -8.212 kcal/mol, respectively, and exhibit significant activity against PPAR-γ agonist and compared with the standard drug Pioglitazone (-7.367 kcal/mol). The density functional calculations were also performed to determine the geometrical properties, thermal parameters, chemical reactivity descriptors and molecular electrostatic potential of the compounds using the B3LYP functional and 6-31G++ basis sets. The energy difference between the highest occupied molecular orbitals and lowest unoccupied molecular orbitals for all the investigated compounds is in the range of 2.8-3.4 eV which allows for easy transfer of electrons and reactivity. Further research and development of these designed compounds could contribute to the advancement of effective antidiabetic treatments. © 2024 World Scientific Publishing Company.