the purpose of this study was to design and optimize an oral controlled release acyclovir mucoadhesive tablet, in term of its drug release and mucoadhesive strength. a 32 full factorial design was employed to study the effect of independent variables like carbopol-934p and hydroxypropyl methylcellulose k100m, which significantly influence characteristics like swelling index, ex-vivo mucoadhesiv...

in recent years, great efforts have been devoted to the design of drug delivery systems. many polymeric excipients have been studied in order to make drug release fit the desired profiles. the aim of this work was to design a theophylline oral suspension, as sustained release pharmaceutical preparation in order to decrease the plasma level fluctuations and adverse effects of theophylline. micro...

in order to enhance in vitro dissolution and content uniformity of poorly soluble drug glimepiride by preparing solid dispersions using modified solvent fusion method, solid dispersions of drug were prepared by modified fusion solvent method using peg 6000 and pvp k25 (as carrier). eight batches (f1-f8) were prepared by factorial design (23) by taking three factors i.e. the concentration of: dr...

The process of preclinical drug discovery consists of two steps: finding of initial hits (binding ligands to a medicinal relevant target, usually a protein) and lead optimization. Nuclear magnetic resonance spectroscopy is a powerful tool that can provide valuable information to every step of drug development. NMR is commonly used for characterizing the structure and molecular dynamics of targe...

Biotechnology is often presented as if progress in the past two decades represented a major success, but the reality is quite different. For example, ten major classes of antibiotics were discovered between 1935 and 1963, but after 1963 there has been just one, the oxazolidones. To illustrate the possibilities of doing better by taking account of the real behaviour of metabolic systems, we can ...

A common step in drug design is the formation of a quantitative structure-activity relationship (QSAR) to model an exploratory series of compounds. A QSAR generalizes how the structure of a compound relates to its biological activity. There is growing interest in the application of machine learning techniques in QSAR modeling research. However, no single technique can claim to be uniformly supe...

Molecular dynamics (MD) simulations are useful tools for structure-based drug design. We review recent publications in which explicit solvent MD was used at the initial or final stages of high-throughput docking campaigns. In some cases, MD simulations of the protein target have been carried out before docking to generate a conformer of the protein which differs from the available crystal struc...

In the past few decades there has been a hiatus in the momentum of research and discovery of ‘novel’ medicinal compounds. This particular trend in drug development perhaps is augmented due to two vital factors, namely : first, strict empirical and rational approach to drug design ; and secondly, high standards of safety and therapeutic efficacy together with tremendous increased costs of resear...

The poly (ADP-ribose) polymerase 1 (PARP1) enzyme is one of the promising molecular targets for the discovery of antitumor drugs. PARP1 is a common nuclear protein (1-2 million molecules per cell) serving as a "sensor" for DNA strand breaks. Increased PARP1 expression is sometimes observed in melanomas, breast cancer, lung cancer, and other neoplastic diseases. The PARP1 expression level is a p...

Drug design may be considered as an integrated whole approach which essentially involves various steps, namely : chemical synthesis, evaluation for activity-spectrum, toxicological studies, metabolism of the drug, i.e., biotransformation and the study of the various metabolites formed, assay procedures, and lastly galenical formulation and biopharmaceutics. The ‘drug design’ in a broader sense ...