title: A novel risperidone-loaded SAIB-PLGA mixture matrix depot with a reduced burst release: effects of solvents and PLGA on drug release behaviors in vitro/in vivo.
abstract: The purpose of this study was to develop an in situ forming SAIB (sucrose acetate isobutyrate)-PLGA (poly (d, lactide-co-glycolide)) mixture matrix depot for sustained release of risperidone. The factors affecting the risperidone release kinetics were investigated to obtain further insight into the drug release mechanisms. The burst release in vitro was significantly reduced (4.95%) by using DMSO as solvent. And, increasing the PLGA content from 2 to 10% w/w decreased the initial release from 6.95 to 1.05%. The initial release in vivo decreased with increasing PLGA content (2.0% w/w PLGA, C(max) = 1161.7 ± 550.2 ng ml(-1); 10% w/w PLGA, C(max) = 280.3 ± 98.5 ng ml(-1)). The persistence (AUC(4-20 days)) over 20 days increased from 76.8 ± 20.7 to 362.8 ± 75.0 ng d ml(-1) by inclusion of 10% PLGA compared with the PLGA-free depot. These results demonstrate that the SAIB-PLGA mixture matrix depot could be useful as a sustained delivery system for risperidone.
authors.affiliation: Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang, Liaoning Province, People's Republic of China.
authors.forename: Xia
authors.initials: X
authors.lastname: Lin
authors.forename: Shenshen
authors.initials: S
authors.lastname: Yang
authors.forename: Jingxin
authors.initials: J
authors.lastname: Gou
authors.forename: Mingming
authors.initials: M
authors.lastname: Zhao
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhang
authors.forename: Na
authors.initials: N
authors.lastname: Qi
authors.forename: Haibing
authors.initials: H
authors.lastname: He
authors.forename: Cuifang
authors.initials: C
authors.lastname: Cai
authors.forename: Xing
authors.initials: X
authors.lastname: Tang
authors.forename: Penghong
authors.initials: P
authors.lastname: Guo
mesh_terms: D000818:Animals; D019540:Area Under Curve; D002845:Chromatography / Q000379:methods; D004058:Diffusion; D018492:Dopamine Antagonists / Q000008:administration & dosage* / Q000737:chemistry; D016503:Drug Delivery Systems; D005260:Female; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D008853:Microscopy / Q000379:methods; D055095:Optics and Photonics; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D016062:Porosity; D051381:Rats; D012212:Rheology; D018967:Risperidone / Q000008:administration & dosage* / Q000737:chemistry; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013997:Time Factors
chemical_list: D018492:Dopamine Antagonists; D012997:Solvents; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D018967:Risperidone