title: Exenatide-loaded PLGA microspheres with improved glycemic control: in vitro bioactivity and in vivo pharmacokinetic profiles after subcutaneous administration to SD rats.
abstract: A subcutaneous exenatide delivery system was developed and characterized in vitro and in vivo. The results clearly showed that the exenatide loaded PLGA microspheres prepared by using a non-aqueous processing medium had low burst release and high drug encapsulation efficiency. Exenatide loaded in the microspheres preserved its bioactivity. The pharmacokinetics parameters were determined after subcutaneous administration of microspheres to SD rats. The plasma concentration of the single dose of the sustained-release microspheres attained C(max) of 108.19±14.92 ng/ml at t(max) of 1.33±0.58 h and the t(½) was 120.65±44.18 h. There was a linear correlation between the in vitro and in vivo release behavior (R²=0.888). Exenatide loaded microspheres may prove to have great potential for clinical use.
authors.affiliation: Department of Pharmaceutical Science, the Second Military Medical University School of Pharmacy, Shanghai 200433, PR China.
authors.forename: Jiming
authors.initials: J
authors.lastname: Xuan
authors.forename: Yaling
authors.initials: Y
authors.lastname: Lin
authors.forename: Jingbin
authors.initials: J
authors.lastname: Huang
authors.forename: Fei
authors.initials: F
authors.lastname: Yuan
authors.forename: Xiaoqing
authors.initials: X
authors.lastname: Li
authors.forename: Ying
authors.initials: Y
authors.lastname: Lu
authors.forename: He
authors.initials: H
authors.lastname: Zhang
authors.forename: Junjie
authors.initials: J
authors.lastname: Liu
authors.forename: Zhiguo
authors.initials: Z
authors.lastname: Sun
authors.forename: Hao
authors.initials: H
authors.lastname: Zou
authors.forename: Yan
authors.initials: Y
authors.lastname: Chen
authors.forename: Jing
authors.initials: J
authors.lastname: Gao
authors.forename: Yanqiang
authors.initials: Y
authors.lastname: Zhong
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D002460:Cell Line; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D000077270:Exenatide; D000067757:Glucagon-Like Peptide-1 Receptor; D057809:HEK293 Cells; D006801:Humans; D054795:Incretins / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D019344:Lactic Acid; D008297:Male; D008863:Microspheres; D010455:Peptides / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017207:Rats, Sprague-Dawley; D018027:Receptors, Glucagon / Q000819:agonists*; D014688:Venoms / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology
chemical_list: D001786:Blood Glucose; D003692:Delayed-Action Preparations; D004337:Drug Carriers; C000593833:GLP1R protein, human; C000593835:Glp1r protein, rat; D000067757:Glucagon-Like Peptide-1 Receptor; D054795:Incretins; D010455:Peptides; D018027:Receptors, Glucagon; D014688:Venoms; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000077270:Exenatide
keywords: Exenatide; Glycemic control; PLGA microspheres; Pharmacokinetic profile; Subcutaneous administration