Pharmacology, General Pharmacology, Toxicology and Pharmaceutics
46
Scopus Publications
Scopus Publications
Oral solid self-emulsifying system containing non-oncology drug combination for repurposing in melanoma treatment: In vitro cytotoxicity, and in vivo hematotoxicity and pharmacokinetic study Rameshwar Ardad, Shashikant Dhawale, Arehalli Manjappa, Sunil T. Galatage, Ahmad Salawi Journal of Research in Pharmacy, 2025 The goal of the current research was to identify a safe and effective non-oncology drug combination as a substitute to existing toxic chemotherapeutics for the treatment melanoma. Further intend was to develop an oral solid self-emulsifying drug delivery system (S-SEDDS) for concurrent delivery of identified combination. The drug containing S-SEDDS was prepared and characterized for flowability, compressibility, drug content, particle size and zeta potential, and in vitro cytotoxicity against melanoma cells. In silico molecular docking for drug with excipients interaction shows compatibility with each other. Moreover, the formulations were characterized in vivo for hepatotoxicity and pharmacokinetic study in rats. The S-SEDDS showed good flowability and compressibility. The particle size of S-SEDDS upon dilution was found in nanometer range. Furthermore, the in vitro cytotoxicity of S-SEDDS containing non-oncology drug (NOD) combination [ketoconazole (KCZ), tadalafil (TLF), disulfiram (DSR)] and docetaxel (DTX) was observed to be higher than S-SEDDS containing only NOD combination against mouse melanoma cells. No significant change in the hematological parameters, animal vital organs weights, and body weights were observed after oral administration of S SEDDS containing non-oncology drug combination with DTX indicating their safety. In addition, significant (p< 0.05) improvement in the oral bioavailability of DTX was observed following its administration in the form of S-SEDDS when compared to the Taxotere in the rats. The developed S-SEDDS containing non-oncology drug combination alone and in combination with docetaxel could be a promising and safe approach in the effective treatment of melanoma.
Preparation and Characterization of Quercetin Phytosome School of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded-431606, India, S D Pande, S C Dhawale, School of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded-431606, India International Journal of Drug Delivery Technology, 2025 The goal of this work is to improve quercetin's solubility and bioavailability by creating and characterizing quercetinphytosomes using the solvent evaporation technique. After obtaining phospholipids from ghee leftovers a quercetin-phosphatidylcholine complex was synthesized and its physicochemical characteristics were assessed. Analytical tools suchas Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (IR), X-ray Diffraction (XRD),Scanning Electron Microscopy (SEM), and Transmission Electron Microscopy (TEM) were used to conduct thecharacterization. Quercetin and phosphatidylcholine have formed a stable combination, as shown by DSC and IR studies.XRD, on the other hand, showed a change to a less crystalline state, suggesting improved solubility. SEM and TEM imagesshowed uniform, nanoscale spherical particles, supporting the successful encapsulation of quercetin. Thus, the 1:2 ratio isidentified as the optimal formulation for maximizing practical yield, underscoring the importance of phospholipidconcentration in achieving higher efficiency. The results indicate that the phytosome formulation enhances the stability,solubility, and bioavailability of quercetin, providing a promising strategy for its therapeutic applications
Citric acid crosslinked hydroxyethyl tamarind gum-based hydrogel films: A promising biomaterial for drug delivery Vishwajeet Sampatrao Ghorpade, Kailas Krishnat Mali, Remeth Jacky Dias, Shashikant Chhaburao Dhawale, Rohit Ramesh Digole, et al. International Journal of Biological Macromolecules, 2024 This investigation explored citric acid crosslinked hydroxyethyl tamarind gum hydrogel films as a potential biomaterial for drug delivery. Hydroxyethylation of tamarind gum aimed to improve its solubility, swelling, and crosslinking potential. The synthesized hydroxyethylated tamarind gum (HETG) was comprehensively characterized, revealing the presence of hydroxyethyl groups and increased viscosity in comparison to unmodified tamarind gum. The citric acid crosslinked HETG hydrogel films were developed by esterification-crosslinking mechanism. The films were characterized using instrumental techniques and evaluated for total carboxyl content, mechanical properties, swelling behavior, drug loading, drug release, antibacterial activity, hemocompatibility and in vitro wound healing activity. The presence of ester crosslinks and extent of crosslinking was confirmed through total carboxyl content and instrumental analysis. Varying HETG (2-2.5%w/v) and citric acid (1-1.4 %w/v) concentrations resulted in films with tunable mechanical strength, swelling, and drug loading. The films effectively controlled the release of a water-soluble drug (80.87-99.70 % in 24 h) through a non-Fickian diffusion mechanism. The optimized HETG hydrogel film showed antimicrobial activity, hemocompatibility, and support for cell growth, confirming its biocompatibility and potential for wound healing. Citric acid-crosslinked HETG films appear promising for drug delivery to wounds, meriting further in vivo study.
Formulation and evaluation of transdermal niosomal gel for antihyperlipidemic agent Pravin Patil, Priyanka Bhagwat, Pournima Sankpal, Sachinkumar Patil, Shashikant Dhawale Nanoscience and Nanotechnology Asia, 2024 Aims: The current study aims to create a formulation of Fluvastatin sodium (FVS) loaded niosome for the treatment of antihyperlipidemia using thin film hydration. The developed formulations were statistically optimized by two factors, three levels by 3-level factorial design and were evaluated for vesicle size, entrapment efficiency, zeta potential, transmission electron microscopy, and in-vitro drug release. Methods: The optimized FVS niosome being transformed to gel formulation was likewise analyzed for in-vitro skin permeability study, lipase action, and stability study. Results: The composition of an improved FVS niosome revealed vesicle size, entrapment effectiveness, zeta potential of 105.3 ± 12.4nm, 74.5 ± 0.86% and -36.2 ± 7mV, respectively, with spherical morphology. Conclusion: The FVS Niosomal gel demonstrated improved skin permeation compared to Orlistat. Furthermore, lipase activity showed better activity when compared with standard Orlistat drugs. Niosomal particles were discovered as a reliable nanovesicular carrier for the transdermal administration of FVS.
SULFOXIDES AND SULFONES: REVIEW Department of Pharmaceutical Chemistry, Womens College of Pharmacy, Peth-Vadgaon, Kolhapur – 416 112, Maharashtra, India, Satwashila S. Kadam, Niranjan S. Mahajan, Pankaj A. Jadhav, Shashikant C. Dhawale Indian Drugs, 2023 It has been established that sulfoxide with sulfones have distinct pharmacological effects. Commodity compounds like sulfoxide and sulfones find widespread use in many chemical disciplines. This is why organic chemists find the synthesis of sulfoxide and sulfones so interesting. In the process of oxidation, sulphides can transform into sulfoxides or sulfones. Comprehensive oxidation to the sulfones is significantly simpler than mild oxidation to the sulfoxide, but both can be achieved by the use of highly selective technologies.
Concurrent oral delivery of non-oncology drugs through solid self-emulsifying system for repurposing in hepatocellular carcinoma Rameshwar M. Ardad, Arehalli S. Manjappa, Shashikant C. Dhawale, Popat S. Kumbhar, Yogesh V. Pore Drug Development and Industrial Pharmacy, 2023 Objective The present study aimed to identify a safe and effective non-oncology drug cocktail as an alternative to toxic chemotherapeutics for hepatocellular carcinoma (HCC) treatment. The assessment of cytotoxicity of cocktail (as co-adjuvant) in combination with chemotherapeutic docetaxel (DTX) is also aimed. Further, we aimed to develop an oral solid self-emulsifying drug delivery system (S-SEDDS) for the simultaneous delivery of identified drugs.Significance The identified non-oncology drug cocktail could overcome the shortage of anticancer therapeutics and help to reduce cancer-related mortality. Moreover, the developed S-SEDDS could be an ideal system for concurrent oral delivery of non-oncology drug combinations.Methods The non-oncology drugs (alone and in combinations) were screened in vitro for anticancer effect (against HepG2 cells) using (3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide; MTT) dye assay, and cell cycle arresting and apoptotic behaviors using the fluorescence-activated cell sorting (FACS) technique. The S-SEDDS is composed of drugs such as ketoconazole (KCZ), disulfiram (DSR), tadalafil (TLF), and excipients like span-80, tween-80, soybean oil, Leciva S-95, Poloxamer F108 (PF-108), and Neusilin® US2 (adsorbent carrier), which was developed and characterized.Results The cocktail composed of KCZ, DSR, and TLF has showed substantial cytotoxicity (at the lowest concentration of 3.3 pmol), HepG2 cell arrest at G0/G1 and S phases, and substantial cell death via apoptosis. The DTX inclusion into this cocktail has further resulted in increased cytotoxicity, cell arrest at the G2/M phase, and cell necrosis. The optimized blank liquid SEDDS that remains transparent without phase separation for more than 6 months is used for the preparation of drug-loaded liquid SEDDS (DL-SEDDS). The optimized DL-SEDDS with low viscosity, good dispersibility, considerable drug retention upon dilution, and smaller particle size is further converted into drug-loaded solid SEDDS (DS-SEDDS). The final DS-SEDDS demonstrated acceptable flowability and compression characteristics, significant drug retention (more than 93%), particle size in nano range (less than 500 nm), and nearly spherical morphology following dilutions. The DS-SEDDS showed substantially increased cytotoxicity and Caco-2 cell permeability than plain drugs. Furthermore, DS-SEDDS containing only non-oncology drugs caused lower in vivo toxicity (only 6% body weight loss) than DS-SEDDS containing non-oncology drugs with DTX (about 10% weight loss).Conclusion The current study revealed a non-oncology drug combination effective against HCC. Further, it is concluded that the developed S-SEDDS containing non-oncology drug combination alone and in combination with DTX could be a promising alternative to toxic chemotherapeutics for the effective oral treatment of hepatic cancer.
LC-HRMS Analysis and Antihyperlipidemic Effect of Ethanolic Leaf Extract of Momordica charantia L. Pushpa KARALE, Shashikant DHAWALE, Mahesh KARALE Hacettepe University Journal of the Faculty of Pharmacy, 2022 Momordica charantia L. (Bitter melon) has been used to treat hyperglycemia and hyperlipidemia in many parts of the world. The present study revealed antihyperlipidemic activity of ethanolic leaf extract of M. charantia L. (named as EMC). The ethanolic extract of leaves were prepared and phytochemical constituents were identified using liquid chromatography linked with mass spectrophotometry. LCMS study indicates the presence of phenolic compound (m-hydroxy benzoic acid, octyl gallate, 3-hydroxycoumarin), triterpenoids (momordicin II, momordicoside E and momordicoside K), saponin E and fatty acids were the major constituents in EMC. Whereas, Triton X-100 induced hyperlipidemic rats model was used to evaluate antihyperlipidemic activity of EMC at a dose of 50, 100 and 200 mg/kg, b.w. or atorvastatin (10 mg/kg, b.w.). The plasma total cholesterol, triglycerides, HDL, LDL and VLDL level, hepatic cholesterol and triglyceride, fecal cholesterol and triglycerides level were checked. Triton X-100 significantly (P < 0.01) increased the serum total cholesterol, triglycerides and LDL with a concomitant reduction in HDL cholesterol. These alterations were ameliorated by EMC at dose dependant manner. EMC (200 mg/kg, b.w) showed significant (P < 0.01) reduction in lipid level among three doses of extracts in comparison with the standard drug atorvastatin. Overall results findings suggest that bitter melon may have potential to use as supplementary ingredient for the prevention of hyperlipidemia and related conditions.
Design, synthesis and biological screening of N-(substituted pyridine-2-yl)-N-(quinoline-2-yl) malonamide as novel anti-HIV-I agents Indian Journal of Chemistry Section B Organic and Medicinal Chemistry, 2018
Development of vancomycin-loaded polysaccharide-based hydrogel wound dressings: In vitro and in Vivo evaluation Asian Journal of Pharmaceutics, 2018
Synthesis, Biological evaluation and docking study of 2-amino-4,6-diarylpyrimidines as novel non-nucleoside HIV-1reverse transcriptase inhibitors Journal of Chemical and Pharmaceutical Research, 2014
Development and validation of a HPLC analytical assay method for dapoxetine tablets: A medicine for premature ejaculation Journal of Chemical and Pharmaceutical Research, 2014