title: Development of andrographolide loaded PLGA microspheres: optimization, characterization and in vitro-in vivo correlation.
abstract: The purpose of this study was to develop a sustained-release drug delivery system based on the injectable PLGA microspheres loaded with andrographolide. The andrographolide loaded PLGA microspheres were prepared by emulsion solvent evaporation method with optimization of formulation using response surface methodology (RSM). Physicochemical characterization, in vitro release behavior and in vivo pharmacokinetics of the optimized formulation were then evaluated. The percent absorbed in vivo was determined by deconvolution using the Loo-Riegelman method, and then the in vitro-in vivo correlation (IVIVC) was established. Results showed that the microspheres were spherical with a smooth surface. Average particle size, entrapment efficiency and drug loading were found to be 53.18±2.11 μm, 75.79±3.02% and 47.06±2.18%, respectively. In vitro release study showed a low initial burst release followed by a prolonged release up to 9 days and the release kinetics followed the Korsmeyer-Peppas model. After a single intramuscular injection, the microspheres maintained relatively high plasma concentration of andrographolide over one week. A good linear relationship was observed between the in vitro and in vivo release behavior (R(2)=0.9951). These results suggest the PLGA microspheres could be developed as a potential delivery system for andrographolide with high drug loading capacity and sustained drug release.
authors.affiliation: School of Pharmacy, Yantai University, Yantai 264005, China.
authors.forename: Yunxia
authors.initials: Y
authors.lastname: Jiang
authors.affiliation: School of Pharmacy, Yantai University, Yantai 264005, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Yantai University, Yantai 264005, China. Electronic address: ytu309a@163.com.
authors.forename: Hui
authors.initials: H
authors.lastname: Xu
authors.affiliation: School of Pharmacy, Yantai University, Yantai 264005, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Yantai University, Yantai 264005, China.
authors.forename: Qingguo
authors.initials: Q
authors.lastname: Meng
authors.affiliation: School of Pharmacy, Yantai University, Yantai 264005, China.
authors.forename: Wanhui
authors.initials: W
authors.lastname: Liu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002853:Chromatography, Liquid; D003692:Delayed-Action Preparations; D004224:Diterpenes / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004655:Emulsions; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D051379:Mice; D008863:Microspheres; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013499:Surface Properties; D053719:Tandem Mass Spectrometry
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D004224:Diterpenes; D004655:Emulsions; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C030419:andrographolide
keywords: Andrographolide; Drug release; In vitro–in vivo correlation; Microspheres; PLGA; RSM