Effect of Bioresorbable Copolymers on Mesalamine Loaded Microspheres for Colon-Specific Drug Delivery

Background

Mesalamine produces many side effects through oral route such as stomach cramps, throat irritation, back ache and muscle pain. Furthermore, it failed to yield maximum drug release and also not able to produce the drug release for over a period of time at the target site. To overcome these disadvantages, the current research proposed to develop microspheres with pH-dependent bio-resorbable polymers to obtain site-specific controlled drug release at the target site.

Materials and Methods

Microspheres were prepared by two methods as ionic gelation and solvent evaporation methods using copolymers such as Eudragit S 100 and PLGA.

Results

The prepared formulations were characterized for multiple parameters and the particle size ranges were found in between 5.52 to12.56 μm whereas percentage entrapment efficiency was found in the range of 32 to 98% respectively. Apart from other formulations, PLGA microspheres showed the maximum cumulative percentage drug release through in vitro and ex vivo and the results were found as 96±0.1% and 90.8±0.8% respectively. As compared to Pentasa®, PLGA microspheres showed two folds increase in drug release. The PLGA biodegradability was observed as maximum in the caecal content than other formulations.

Conclusion

Compared to Pentasa®, the prepared PLGA microspheres showed the best results and the obtained result was verified with a p-value which is shown <0.005. Based on the results, it was concluded that the prepared PLGA microspheres showed better-controlled drug release than other test formulations.