Formulation Development and In vitro Evaluation of Oral Extended release Capsules Containing Biodegradable Microspheres
- *Corresponding Author:
- Duc P Do
Department of Pharmaceutical Sciences
College of Pharmacy, Chicago State University
9501 South King Drive, Douglas Hall 206, Chicago, IL 60628, USA
E-mail: [email protected]
Received Date: May 22, 2014; Accepted Date: June 14, 2014; Published Date: June 18, 2014
Citation: Enriquez GG, Orawiec BA, Rizvi SAA, Do DP (2014) Formulation Development and In vitro Evaluation of Oral Extended-release Capsules Containing Biodegradable Microspheres. J Nanomed Nanotechnol 5:208. doi:10.4172/2157-7439.1000208
Copyright: © 2014 Enriquez GG, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Oral extended-release delivery of Biopharmaceutics Classification System (BCS) class II and III compounds is desirable in order to decrease dosing frequency and potential adverse effects. Maintaining an extended-release profile of the drug is ideal to minimize fluctuations in plasma concentrations. The main objective of this research was to formulate a polymeric microsphere drug delivery system that will effectively provide extended-release characteristics via an orally administered capsule. Using acetaminophen and ibuprofen as model drugs, this drug delivery system was shown to provide extended-release characteristics of the drug for enhanced efficacy. The biodegradable polymeric matrix was formulated using bovine serum albumin (BSA) with glutaraldehyde as the crosslinker. The drug of interest was then encapsulated into the polymeric matrix and spray-dried into microspheres. Once prepared, the drug-loaded microsphere powder was placed into hard gelatin capsules. The physicochemical properties of the microsphere formulations were characterized. Additionally, differential scanning calorimetry was utilized to examine the thermal stability of the encapsulated drug. Release studies were conducted in vitro to examine the release profile of the drug. Cell uptake studies were carried out to examine the internalization capability of microsphere formulations. Drugloaded microspheres were found to be approximately 2 microns in size and exhibited a uniform size distribution. Zeta potential measurements were shown to be approximately -30 mV, which indicated that the microspheres are stable in dispersions. Release data showed a constant release of the drug from the microsphere and capsule formulations for at least 16 hours. Formulated microspheres were able to be internalized into human intestinal Caco-2 cells. These data provided evidence for the role of the microsphere delivery system in the extended-release delivery of BCS Class II and III drug substances.