Microtubules are critical components of the cytoskeleton. Perturbing their function arrests the growth of a broad spectrum of cancer cell lines, making microtubules an excellent and established target for chemotherapy. All of the U.S. Food and Drug Administration-approved antitubulin agents bind to paclitaxel or vinblastine binding sites in tubulin. Because of the complexity of their structures...

For good bioavailability, natural products must have a good balance between hydrophilicity (for dissolving into the gastro-intestinal fluids) and lipophilicity (to cross lipidic biomembranes). Many phytoconstituents like glycosilated polyphenolics have good water solubility, but are, nevertheless, poorly absorbed[1] because of their large size, incompatible with a process of passive diffusion a...

Intracellular drug exposure is influenced by cell- and tissue-dependent expression of drug-transporting proteins and metabolizing enzymes. Here, we introduce the concept of intracellular bioavailability (Fic) as the fraction of extracellular drug available to bind intracellular targets, and we assess how Fic is affected by cellular drug disposition processes. We first investigated the impact of...

Purpose: Remdesivir, a drug originally developed against Ebola virus, is currently recommended for patients hospitalized with coronavirus disease of 2019 (COVID-19). In spite United States Food and Drug Administration’s recent assent remdesivir as the only approved agent COVID-19, there limited information available about physicochemical, metabolism, transport, pharmacokinetic (PK), drug-drug i...

Transdermal patches were developed for a low oral bioavailable drug, lacidipine (LCDP) employing ethyl cellulose/Eudragit RL100 and polyvinyl pyrollidone (PVP) as polymeric matrices. The effect of binary mixtures of polymers on physicochemical properties such as thickness, moisture absorption and moisture content; in vitro release, ex vivo permeation and mechanical properties was evaluated. Ex ...

Amoxicillin/clavulanate (Co-Amox), a commonly used antibiotic for the treatment of bacterial infections, has been associated with drug-induced liver damage. Quercetin (QR), naturally occurring flavonoid pleiotropic biological activities, poor water solubility and low bioavailability. The objective this work was to produce more bioavailable formulation QR (liposomes) determine effect its intrape...

Volume 5(6) 1000e123 J Cancer Sci Ther ISSN:1948-5956 JCST, an open access journal The landmark decision to rejection of patent to anti-cancer drug ‘Glivec’ by Indian Supreme Court has catalysed range of debates around importance of innovation in research and development. The patent plea by Novartis for beta crystalline for of imanitib (i.e. glivec) was considered as an attempt to extend period...

This chapter develops a comprehensive longitudinal model for the proximate determinants of hemoglobin concentration using three repeated observations on 514 women in Bangladesh. The explanatory variables in the model were nutrient intakes, including bioavailable iron; anthropometric measurement; morbidity involving blood loss; and intake of iron tablets. Bioavailable iron, women’s height and mi...

Inappropriate platelet aggregation creates a cardiovascular risk that is largely managed with thienopyridines and aspirin. Although effective, these drugs carry risks of increased bleeding and drug 'resistance', underpinning a drive for new antiplatelet agents. To discover such drugs, one strategy is to identify a suitable druggable target and then find small molecules that modulate it. A good ...