EFFECTS OF H+ LIBERATED FROM HYDROLYTIC CLEAVAGE OF POLYESTER MICROCAPSULES ON THEIR PERMEABILITY AND DEGRADABILITY

Authors
Citation
Hk. Sah et Yw. Chien, EFFECTS OF H+ LIBERATED FROM HYDROLYTIC CLEAVAGE OF POLYESTER MICROCAPSULES ON THEIR PERMEABILITY AND DEGRADABILITY, Journal of pharmaceutical sciences, 84(11), 1995, pp. 1353-1359
Citations number
22
Categorie Soggetti
Chemistry,"Pharmacology & Pharmacy
ISSN journal
00223549
Volume
84
Issue
11
Year of publication
1995
Pages
1353 - 1359
Database
ISI
SICI code
0022-3549(1995)84:11<1353:EOHLFH>2.0.ZU;2-D
Abstract
Microcapsules prepared from blends of poly(d,l-lactide-co-glycolide) w ith a lactide:glycolide ratio of 75:25 (PLGA75:25) and poly(d,l-lactid e) (PLA5000) or poly(d,l-lactic acid-co-glycolic acid) (PLGA5000) were dispersed in phosphate-buffered saline, and their hydrolytic rates we re investigated. Using the Henderson-Hasselbalch equation and an L-lac tic acid experiment, the concentration of hydrogen ions released into the bulk medium was calculated from the change in buffer pH. The rate of H+ formation was found to be dependent upon the polymer composition of the microcapsules. The incorporation of PLGA5000 or PLA5000 into P LGA75:25 microcapsules drastically enhanced hydrolytic rates of microc apsules and resulted in controlled release of hydrogen ions generated from carboxyl end groups of both intact and degrading polymers. In con trast to microcapsules prepared with PLGA75:25 only, which liberated a negligible amount of H+ ions after a 21-day incubation, the microcaps ules prepared from polymer blends released approximately (19.2-42.0) ( x10(-3)) mmol of H+ ions. It has been found that the amount of hydroge n ions liberated into the bulk can be used as a qualitative indicator to monitor the change in microcapsule permeability to protein as well as polymer degradation.