TY - JOUR
T1 - Effects of H+ liberated from hydrolytic cleavage of polyester microcapsules on their permeability and degradability
AU - Sah, Hongkee
AU - Chien, Yie W.
PY - 1995/11
Y1 - 1995/11
N2 - Microcapsules prepared from blends of poly(d, l‐lactide‐co‐glycolide) with a lactide:glycolide ratio of 75:25 (PLGA75:25) and poly‐(d, l‐lactideactide) (PLA5000) or poly(d, l‐lactic acid‐co‐glycolic acid) (PLGA5000) were dispersed in phosphate‐buffered saline, and their hydrolytic rates were investigated. Using the Henderson–Hasselbalch equation and an L‐lactic 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 PLGA75:25 microcapsules drastically enhanced hydrolytic rates of microcapsules and resulted in controlled release of hydrogen ions generated from carboxyl end groups of both intact and degrading polymers. In contrast to microcapsules prepared with PLGA75:25 only, which liberated a negligible amount of H+ ions after a 21‐day incubation, the microcapsules prepared from polymer blends released approximately (19.2–42.0) (×10−3) mmol of H+ ions. It has been found that the amount of hydrogen 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.
AB - Microcapsules prepared from blends of poly(d, l‐lactide‐co‐glycolide) with a lactide:glycolide ratio of 75:25 (PLGA75:25) and poly‐(d, l‐lactideactide) (PLA5000) or poly(d, l‐lactic acid‐co‐glycolic acid) (PLGA5000) were dispersed in phosphate‐buffered saline, and their hydrolytic rates were investigated. Using the Henderson–Hasselbalch equation and an L‐lactic 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 PLGA75:25 microcapsules drastically enhanced hydrolytic rates of microcapsules and resulted in controlled release of hydrogen ions generated from carboxyl end groups of both intact and degrading polymers. In contrast to microcapsules prepared with PLGA75:25 only, which liberated a negligible amount of H+ ions after a 21‐day incubation, the microcapsules prepared from polymer blends released approximately (19.2–42.0) (×10−3) mmol of H+ ions. It has been found that the amount of hydrogen 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.
UR - http://www.scopus.com/inward/record.url?scp=0028808125&partnerID=8YFLogxK
U2 - 10.1002/jps.2600841117
DO - 10.1002/jps.2600841117
M3 - Article
C2 - 8587055
AN - SCOPUS:0028808125
SN - 0022-3549
VL - 84
SP - 1353
EP - 1359
JO - Journal of Pharmaceutical Sciences
JF - Journal of Pharmaceutical Sciences
IS - 11
ER -