Papers by Bharat Dhokchawle
Lipid as an Excipient for Design and Development of Formulations
Indian Drugs
Lipids are present abundantly in human body in several forms. Different types of lipids are avail... more Lipids are present abundantly in human body in several forms. Different types of lipids are available with diverse physical properties, based on which suitable lipids can be selected for development of formulations. Lipids are also available for specific purposes like lubrication, emulsification, emollientes and enhancement of bioavailability. Conventionally, many lipids are used in formulation of tablets, capsules, emulsions and cosmetics. In recent years, use of lipids for drug delivery has been extended to Solid Lipid Nanoparticles (SLN), Nanostructured Lipid Carriers (NLC), and Self-Micro Emulsifying Drug Delivery System (SEDDS), which are emerging technologies designed to address challenges like solubility and bioavailability of poorly water-soluble drugs. This paper mainly focuses on different types of formulations in which lipids are used, and parameters which are critical for selection of lipid in any dosage form development. Several examples are quoted for different uses of...
Hepatocellular carcinoma (HCC) is a serious healthcare problem worldwide because of its increasin... more Hepatocellular carcinoma (HCC) is a serious healthcare problem worldwide because of its increasing morbidity and high mortality rates. The present study aimed to investigate the chemopreventive effects of prepared sulfated oligosaccharide compounds(Maltose SO4, Raffinose SO4, Stachyose SO4, Chondroitin-6-sulfate and Maltohexaose SO4)by studying their ability to inhibit, reverse or restrict the development of cancer through inhibiting the metastasis and angiogenesis of tumor in diethylnitrosamine (DENA) induced hepatocarcinogenesis in rats. To elucidate the mechanism by which the prepared sulfated oligosaccharidesexert their antitumor activities in the animals-bearing tumor the following parameters were determined including:aspartate and alanine aminotransferases (AST & ALT), alkaline phosphatase (ALP), total bilirubinas liver function test;hepatic tyrosine kinase (TRK) and cytochrome P450 2E1 (CYP 2E1) as marker for tumor progression;vascular endothelial growth factor (VEGF) and sia...
Quantitative Structure Activity Relationship studies of Antimicrobial Compounds:A Review
Anti-Infective Agents, 2021
: With the current scenario of emerging drug-resistant microbial strains, there prevails a contin... more : With the current scenario of emerging drug-resistant microbial strains, there prevails a continuous threat to health and the development of new antimicrobial agents is a challenging task. Quantitative Structure Activity Relationship (QSAR) has proven to elevate the likelihood of finding a new pharmacophore. Intermolecular binding like hydrophobic bond, electrostatic and steric interactions helps to understand drug interaction with the receptors. Some common conclusions have been drawn after analyzing diverse case studies. Few descriptors were identified to be common in enhancing the antimicrobial activity. The structural features modifying the antimicrobial activity were analyzed using critically published results from significant QSAR studies on antimicrobial compounds. This commentary will assist the synthetic chemist to synthesize novel derivatives which could be potential antimicrobial compounds.
Translational Pharmacology: New approach of drug discovery
Increasingly, the field is recognizing the need to enable a closer collaboration of industry and ... more Increasingly, the field is recognizing the need to enable a closer collaboration of industry and academia to create a more efficient system for developing new drugs. In parallel with this, the world of drug discovery has seen the emergence of translational research as an alternative approach to the creation of new drugs, and there is growing support for the claim that this strategy may provide solutions to some of the woes of the pharmaceutical industry. Translational medicine and translational pharmacology have become terms increasingly used to describe the focus of applied pharmacological research to ultimately help patients. Yet, the number of effective medicines reaching the approval stage continues to decline. Drug discovery represents the first step in the creation of new drugs, and takes place in academic institutions, biotech companies, and large pharmaceutical corporations. With the rise of translational research these relationships are shifting and new hubs are emerging, a...
Ester Prodrugs of Ketoprofen: Synthesis, Hydrolysis Kinetics and Pharmacological Evaluation
Drug Research, 2015
The ester prodrugs of ketoprofen with various naturally available antioxidants; menthol, thymol, ... more The ester prodrugs of ketoprofen with various naturally available antioxidants; menthol, thymol, eugenol, guiacol, vanillin and sesamol have been synthesized by the dicyclohexyl carbodiimide (DCC) coupling method, purified and characterized by spectral data. Further, their, partition coefficients have been determined as well as, hydrolytic studies performed. The synthesized compounds are more lipophilic compared to the parent moieties and are stable in acidic environment, which is a prerequisite for their oral absorption. Under gastric as well as intestinal pH conditions these prodrugs showed variable susceptibility towards hydrolysis. The title compounds when evaluated for anti-inflammatory, analgesic activities and ulcerogenicity, showed improvement over the parent drug.
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Papers by Bharat Dhokchawle