title: Preparation and evaluation of posaconazole-loaded enteric microparticles in rats.
abstract: OBJECTIVE
  Posaconazole (POS) is an antifungal compound which has a low oral bioavailability. The aim of this study was to prepare POS enteric microparticles to enhance its oral bioavailability.
  
  
  METHODS
  POS enteric microparticles were prepared with hypromellose acetate succinate (HPMCAS) via the spray drying method. The solvent mixtures of acetone and ethanol used in the preparation of the microparticles were optimized to produce the ideal POS enteric microparticles. Multivariate data analysis using a principal component analysis (PCA) was used to find the relationship among the HPMCAS molecular characteristics, particle properties and drug release kinetics from the spray dried microparticles.
  
  
  RESULTS
  The optimal spray solvent mixtures were critical to produce the POS microparticles with the defined polymer entanglement index, drug surface enrichment, particle size and drug loading. The HPMCAS molecular characteristics affected the microscopic connectivity and diffusivity of polymer matrix and eventually influenced the drug release behavior, and enhanced the bioavailability of POS.
  
  
  CONCLUSIONS
  These studies suggested that the selection of suitable solvent mixtures of acetone and ethanol used in the spray drying of the microparticles was quite important to produce the entangled polymer structures with preferred polymer molecular properties of polymer coiling, overlap concentration and entanglement index. Additional studies on particle size and surface drug enrichment eventually produced HPMCAS-based enteric microparticles to enhance the oral bioavailability of POS.
authors.affiliation: a School of Pharmaceutical Sciences , Shandong University , Jinan , Shandong , PR China.
authors.forename: Min
authors.initials: M
authors.lastname: Yang
authors.affiliation: a School of Pharmaceutical Sciences , Shandong University , Jinan , Shandong , PR China.
authors.forename: Zhonghua
authors.initials: Z
authors.lastname: Dong
authors.affiliation: a School of Pharmaceutical Sciences , Shandong University , Jinan , Shandong , PR China.
authors.forename: Yongchun
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: a School of Pharmaceutical Sciences , Shandong University , Jinan , Shandong , PR China.
authors.forename: Fang
authors.initials: F
authors.lastname: Zhang
authors.affiliation: a School of Pharmaceutical Sciences , Shandong University , Jinan , Shandong , PR China.
authors.forename: Yongjie
authors.initials: Y
authors.lastname: Wang
authors.affiliation: a School of Pharmaceutical Sciences , Shandong University , Jinan , Shandong , PR China.|b Shandong Engineering & Technology Research Center for Jujube Food and Drug , Jinan , Shandong , PR China.|c Shandong Provincial Key Laboratory of Mucosal and Transdermal Drug Delivery Technologies , Shandong Academy of Pharmaceutical Sciences , Jinan , Shandong , PR China.
authors.forename: Zhongxi
authors.initials: Z
authors.lastname: Zhao
mesh_terms: D000096:Acetone / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003890:Desiccation / Q000379:methods; D004339:Drug Compounding / Q000379:methods; D065546:Drug Liberation / Q000187:drug effects; D008863:Microspheres; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D014230:Triazoles / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology
chemical_list: D011108:Polymers; D012997:Solvents; D014230:Triazoles; D000096:Acetone; C101425:posaconazole
keywords: HPMCAS; PCA; Posaconazole; enteric microparticles; pharmacokinetics