Preparation, evaluation and bioavailability studies of indomethacin loaded PEA polymeric microspheres for controlled drug delivery.

摘要

The goal of any drug delivery system is to provide a therapeutic amt. of drug (s) to the proper site in the body to promptly achieve and thereby to maintain the desired drug concns. during treatment. This idealized objective can be achieved by targeting the drugs to a specific organ or tissue with the help of controlling the release rate of the drug during the transit time in gastro intestinal tract. The present study aims to the prepn. of poly ester amide (PEA) microspheres contg. indomethacin (IM) as a model drug, and to compare the in vitro release and pharmacokinetics of prepd. IM formulations with com. available MicrocidSR. In the present study, water is used to prep. PEA polymer microspheres by meltable dispersed emulsified cooling induced solidification method. Surface morphol. of prepd. microspheres was evaluated using SEM. The SEM images revealed the spherical shape of microspheres with size ranges 132 μm to 796 μm. Differential scanning calorimetry (DSC) and Fourier transform IR (FTIR) spectroscopy studies indicated that the drug after encapsulation with PEA polymer was stable and compatible. A single dose randomized complete cross over study of IM (75mg) microspheres was carried out in healthy albino rabbits. Plasma IM concns. and other pharmacokinetic parameters were statistically analyzed. [on SciFinder(R)]