Effect of Stabilizers on Bioactivity of Peptide-24 in PLGA Microspheres

Mingbo      Wang; XiaoDong      Guo; Rongwei      Tan; Zhending      She; Qingling      Feng

doi:10.2174/1573406411309080014

Abstract

In the present study, Poly (D,L-lactide-co-glycolide) microspheres (PLGA MSs) were prepared for delivering a novel oligopeptide derived from rhBMP-2 (Peptide-24). Hydroxypropyl-β-cyclodextrin (HP-β-CD) and Bovine serum albumin (BSA) were used as stabilizers for retaining bioactivity of the oligopeptide. The morphology, diameter, drugloading rates and encapsulation rates of the PLGA MSs were detected and compared. The PLGA MSs were incubated for 3 and 30 days respectively to obtain the release supernatant containing Peptide-24. The structure and bioactivity of released Peptide-24 from PLGA MSs were evaluated through physicochemical detections and cell culture. The structure integrity of the Peptide-24 was confirmed by Far-UV circular dichroism and matrix-assisted laser desorption/ionization time-of-flight Mass Spectrometer (MALDI-TOF-MS) analysis. The interaction between PLGA matrix and loaded Peptide- 24 was verified through Raman. The results showed that the diameter of PLGA MSs was from 8.62 to 15.34 μm, the loading rate was 0.7-0.8%, and the encapsulation rate was 69.3-85.3%. The released Peptide-24 from PLGA MSs was proved to retain original bioactivity by the cellular activity and alkaline phosphatase (ALP) test. HP-β-CD is a kind of excellent stabilizer for retaining the bioactivity of Peptide-24 in PLGA MSs.

Keywords: Poly (D, L-lactide-co-glycolide), microencapsulation, peptides, stabilization, cell culture, bioactivity.

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