title: Comparative studies on exenatide-loaded poly (D,L-lactic-co-glycolic acid) microparticles prepared by a novel ultra-fine particle processing system and spray drying.
abstract: The purpose of this study was to compare the properties of exenatide-loaded poly (D,L-lactic-co-glycolic acid) microparticles (Ex-PLGA-MPs) prepared by a novel ultra-fine particle processing system (UPPS) and spray drying. UPPS is a proprietary technology developed by our group based on the disk rotation principle. Characteristics of the MPs including morphology, particle size distribution, drug content, encapsulation efficiency and in vitro release were comparatively studied. Cytotoxicity of the MPs was examined on A549 cells and the pharmacodynamics was investigated in vivo in type 2 diabetes Sprague-Dawley (SD) rats. Ex-PLGA-MPs prepared by UPPS showed larger particle size, denser surface, greater encapsulation efficiency, less initial burst release, and stable sustained release for more than one month in vitro as compared with the spray drying MPs. Meanwhile, the UPPS MPs effectively controlled the body growth rate and blood glucose in diabetes rats for at least three weeks after a single injection, while the spray drying MPs showed effective control period of about two weeks. UPPS technology was demonstrated to manufacture Ex-PLGA-MPs as a potential sustained release protein/polypeptide delivery system, which is an alternative method for the most commonly used spray drying. This comparative research provides a new guidance for microparticle preparation technology.
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: zhuchune1108@163.com.
authors.forename: Chune
authors.initials: C
authors.lastname: Zhu
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: 1537969972@qq.com.
authors.forename: Ying
authors.initials: Y
authors.lastname: Huang
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: 1558745493@qq.com.
authors.forename: Xiaoying
authors.initials: X
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: 1060854327@qq.com.
authors.forename: Liling
authors.initials: L
authors.lastname: Mei
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: pxin_1385@163.com.
authors.forename: Xin
authors.initials: X
authors.lastname: Pan
authors.affiliation: Guangzhou Neworld Pharm. Co. Ltd., Guangzhou 510006, China. Electronic address: ww236@hotmail.com.
authors.forename: Ge
authors.initials: G
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China; Research and Development Center of Pharmaceutical Engineering, Sun Yat-sen University, Guangzhou, China. Electronic address: chuanbin_wu@126.com.
authors.forename: Chuanbin
authors.initials: C
authors.lastname: Wu
mesh_terms: D000818:Animals; D002849:Chromatography, Gas; D002942:Circular Dichroism; D000077270:Exenatide; D005260:Female; D019344:Lactic Acid / Q000008:administration & dosage*; D008297:Male; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010455:Peptides / Q000008:administration & dosage*; D011100:Polyglycolic Acid / Q000008:administration & dosage*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017207:Rats, Sprague-Dawley; D017550:Spectroscopy, Fourier Transform Infrared; D014688:Venoms / Q000008:administration & dosage*
chemical_list: D010455:Peptides; D014688:Venoms; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000077270:Exenatide
keywords: Exenatide; Microparticles; PLGA; Spray drying; Ultra-fine particle processing system (UPPS)