title: Effect of stabilizers on bioactivity of peptide-24 in PLGA microspheres.
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.
authors.affiliation: Key Laboratory of Advanced Materials, Department of Materials Science and Engineering, Tsinghua University, Beijing 100084, China. biomater@mail.tsinghua.edu.cn.
authors.forename: Mingbo
authors.initials: M
authors.lastname: Wang
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Guo
authors.forename: Rongwei
authors.initials: R
authors.lastname: Tan
authors.forename: Zhending
authors.initials: Z
authors.lastname: She
authors.forename: Qingling
authors.initials: Q
authors.lastname: Feng
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000469:Alkaline Phosphatase / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D019344:Lactic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D059630:Mesenchymal Stem Cells / Q000737:chemistry / Q000166:cytology / Q000378:metabolism*; D008863:Microspheres; D009842:Oligopeptides / Q000737:chemistry* / Q000378:metabolism*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D055550:Protein Stability / Q000187:drug effects; D011817:Rabbits; D012710:Serum Albumin, Bovine / Q000737:chemistry / Q000378:metabolism; D013499:Surface Properties; D047392:beta-Cyclodextrins / Q000737:chemistry / Q000378:metabolism
chemical_list: D009842:Oligopeptides; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D012710:Serum Albumin, Bovine; D019344:Lactic Acid; D000469:Alkaline Phosphatase