Purpose: To develop a novel method of cross-linking Bovine Serum Albumin (BSA) and glycine (GLY) using Glutaraldehyde (GLUT) and to develop Resveratrol microsphere formulations using chemically modified BSA and GLY as the microsphere matrix.
Methods: 5% BSA and Glycine Solutions in deionized water were prepared and crosslinked with different concentrations of GLUT. The concentration of GLUT during crosslinking was determined at various time points for up to 24 hours using UV spectrophotometer. Resveratrol was added to the crosslinked matrices to obtain a homogenous solution. Then spray dried using Buchi 191 Mini Spray Dryer to obtain chemically stabilized Resveratrol loaded BSA and GLY microspheres. Product yields, encapsulation efficiencies, mean particle sizes and zeta potential value were determined for all the microsphere formulations prepared. Microsphere dissolution studies were performed using a modified USP type I dissolution apparatus in Phosphate Buffered Saline (PBS) to study the release of Reveratrol from the microsphere formulations.
Results: Optimum concentrations of GLUT for crosslinking of BSA and GLY suitable for spray
drying and with sufficient delayed release ability were found to be in the range of 0.5% and 1.0%. At the end of 24 hours the concentration of GLUT in the crosslinking reaction mixture was found to be 0.533 + 0.025 μg/mL. Product yields and encapsulation efficiencies were in the range of 69.00% – 78.00% and 70.60% to 81.45%, respectively. The mean particle sizes and zeta
potential values were found to be in the range of 4.55 + 1.98 μm to 5.62 + 1.13 μm and -
30.56 + 5.35 mV to -31.32 + 4.53 mV. The burst release in PBS and GLY was found to be less than 10%. The Melting points for all microspheres prepared were in the range of 254-257°C.
Conclusion: A novel method for crosslinking BSA and GLY with GLUT was established which can be used for preparation of Resveratrol loaded microspheres using the Spray Dryer. The formulations also had good encapsulation efficiencies, mean particle sizes, and zeta potential. The burst release of the drug from the microspheres was found to be significantly low and reasonable.
Ayman Shatnawi– Assistant Professor, University of Charleston, school of Pharmacy, Charleston
Tamer Fandy– Associate Professor, University of charleston, school of Pharmacy, Charleston, West Virginia
Ronaldo Ramirez– Assitant Professor, University of Charleston School of Pharmacy, Charleston, West Virginia
Kwame Yeboah– Associate Professor, Harding University, Searcy, Arkansas