BSA-FITC-loaded microcapsules for in vivo delivery

Here we describe the preparation of BSA-FITC-loaded microcapsules as a model protein system for in vivo delivery. BSA-FITC-loaded microcapsules were prepared using a mono-axial nozzle ultrasonic atomizer, varying a number of parameters to determine optimal conditions. The preparation method chosen resulted in a BSA-FITC encapsulation efficiency of similar to 60% and a particle size of similar to 50 mu m. An analysis of the microcapsules showed a BSA-FITC core surrounded by a poly(D,L-lactic-co-glycolic acid) (PLGA) shell. Injection of BSA-FITC-loaded microcapsules into rats resulted in a sustained release of BSA-FITC that maintained increased concentrations of BSA-FITC in plasma for up to 2 weeks. In contrast, the concentration of BSA-FITC in plasma after injection of BSA-FITC-only solution reached near-zero levels within 3 days. Fluorescence images of microcapsules removed at various times after implantation showed a gradual decrease of BSA-FITC in BSA-FITC-loaded microcapsules, confirming a sustained in vivo release of BSA-FITC. The duration of in vivo release and plasma concentration of BSA-FITC was correlated with the initial dose of BSA-FITC. BSA-FITC-loaded microcapsules maintained their structure for at least 4 weeks in the rat. The inflammatory response observed initially after injection declined over time. In conclusion, BSA-FITC-loaded microcapsules achieved sustained release of BSA-FITC, suggesting that microcapsules manufactured as described may be useful for in vivo delivery of pharmacologically active proteins. (C) 2008 Elsevier Ltd. All rights reserved.