Polyelectrolyte complex of chondroitin sulfate and peptide with lower pI value in poly(lactide-co-glycolide) microsphere for stability and controlled release.
A polyelectrolyte complex between a therapeutic peptide and chargeable polymer was applied to prevent peptide denaturation in poly(lactide-co-glycolide) (PLGA) microspheres. Chondroitin sulfate A (CsA) was employed as a polymeric additive for the formation of an ionic complex with insulin (InS). The complex prepared at pH 3.0 evidenced a nano-size in the range of 100-400 nm with a mono distribution. The stability of InS in the complex in an organic/water (O/W) interface was verified via RP-HPLC. The insulin in the complex evidenced a retention time almost identical to native InS, whereas free insulin did not evidence such a retention time. On the basis of these studies, PLGA microspheres including a complex with various CsA/InS ratios were prepared via a double-emulsion method (PLGA/CsA MS). InS loading efficiency in the system is higher than that of the microspheres without CsA. The system evidenced a lower initial burst and, following the initial burst, continuous release kinetics for 30 days. Circular dichroism (CD) spectra demonstrated that the insulin in PLGA/CsA MS is more stable than the PLGA-only microspheres (PLGA/only MS) for 20 days. These results indicate that the complex system with CsA is useful for the long-term delivery of peptides with lower pI values.
Department of Biotechnology, The Catholic University of Korea, 43-1 Yeokkok2-dong, Wonmi-gu, Bucheon-si, Gyeonggi-do, 420-743, Republic of Korea.
Wooram
W
Park
Kun
K
Na
D002809:Chondroitin Sulfates / Q000737:chemistry*; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry; D007328:Insulin / Q000737:chemistry; D019344:Lactic Acid / Q000737:chemistry*; D008863:Microspheres; D010455:Peptides / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000138:chemical synthesis* / Q000737:chemistry*
D004337:Drug Carriers; D007328:Insulin; D010455:Peptides; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D002809:Chondroitin Sulfates