Synthesis and Evaluation of a New Polymeric Prodrug for Sustained and Site Specific Delivery

Abstract

This thesis deals with the investigations carried out by the writer on the synthesis and evaluation of some nonsteroidal anti-inflammatory polymeric pro-drugs for sustained and site-specific delivery. The first chapter of the thesis deals with a brief introduction to controlled drug delivery systems, role of polymeric materials in drug delivery, release characteristics of the polymeric pro-drugs, the use of NSAIDs and the problems associated with their use, targeting of the drugs to the GI tract and a literature survey on the investigations that have been carried out on sustained release formulations for the drug selected in the present investigation, namely, ibuprofen. The second chapter of the thesis explains the scope and object of the present investigation in detail. It explains, in particular, how when an NSAID linked covalently to a bicompatible polymer through an ester linkage should lead to a drug delivery system capable of releasing the drug predominantly at the lower GI tract in a sustained and site-specific manner. The third chapter of the thesis deals with the experimental procedures that are followed in the preparation of the polymeric pro-drugs, molecular weight determination, in vitro drug release studies, bioavailability studies and anti-inflammatory and ulcer inducing effects of the pro-drugs. The fourth chapter of the thesis deals with the results obtained in the present study along with a detailed discussion of the results supported by chemical equations, Tables, Figures, etc. The following are some of the important findings in the present study; (i) A polymerisable drug derivative of ibuprofen has been synthesised and characterized in terms of melting point, IR, NMR and Mass spectral analysis and this derivative has been polymerised with different ratios of HEMA to obtain five pro-drugs. (ii) The polymeric pro-drugs synthesised have been studied for their in vitro drug release behaviour at pH 1.2 and 7.2. newline