Formulation Development and Evaluation of Colonspecific Esomeprazole Microspheres

Nilima A. Thombre^*, Huzefa Ahmad Shaikh and Eknath D. Ahire

Department of Pharmaceutics, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Adgaon, Nashik, Maharashtra, India.

Corresponding Author E-mail: nilimat_iop@bkc.met.edu

DOI : http://dx.doi.org/10.13005/bbra/3020

ABSTRACT:

The development of Esomeprazole microspheres using enteric coated polymers, such as Eudragit L100, by antisolvent precipitation method has been the focus of recent research in order to achieve the best drug concentration along with improved stability and bioavailability without any adverse effects in an acidic environment. For the development of the Esomeprazole microsphere, a 3² factorial design was used, with polymer amount and rpm being the variables. According to the results of the factorial design investigation, it was found that polymer concentration has a substantial impact on drug release while stirring speed has a large impact on entrapment efficiency. Increased Eudragit L100 concentration caused the medication release to increase from 81.06 to 95.71%. The optimized formulation was then assessed for additional research on surface morphology, particle size, PDI, Zeta potential, percent entrapment efficiency, and in-vitro investigations drug release studies and stability of prepared formulation. According to the results of scanning electron microscopy for the optimised batch, developed microparticles with smooth surfaces and spherical shapes were found. 93.40% drug release and 70.63% drug entrapment efficiency were found in the optimised batch. As a result, the current study's findings indicated that microencapsulation had significant benefits for enhancing Esomeprazole's acid stability. By providing a delayed release effect for a duration of 10 hours and a higher patient compliance rate, developed microspheres were demonstrated to be efficient for protecting drugs in acidic media.

KEYWORDS: Colon Targeted Drug Delivery; Esomeprazole; Eudragit L100; Micropheres

[ HTML Full Text]