title: The pharmacokinetics and pharmacodynamics of lidocaine- loaded biodegradable poly(lactic-co-glycolic acid) microspheres.
abstract: The purpose of this study was to develop novel lidocaine microspheres. Microspheres were prepared by the oil-in-water (o/w) emulsion technique using poly(D,L-lactide-co-glycolide acid) (PLGA) for the controlled delivery of lidocaine. The average diameter of lidocaine PLGA microspheres was 2.34±0.3 μm. The poly disperse index was 0.21±0.03, and the zeta potential was +0.34±0.02 mV. The encapsulation efficiency and drug loading of the prepared microspheres were 90.5%±4.3% and 11.2%±1.4%. In vitro release indicated that the lidocaine microspheres had a well-sustained release efficacy, and in vivo studies showed that the area under the curve of lidocaine in microspheres was 2.02-2.06-fold that of lidocaine injection (p<0.05). The pharmacodynamics results showed that lidocaine microspheres showed a significant release effect in rats, that the process to achieve efficacy was calm and lasting and that the analgesic effect had a significant dose-dependency.
authors.affiliation: Department of Anesthesiology, Shanghai Pulmonary Hospital, Tongji University School of Medicine, 507 Zhengmin Road, Yangpu District, Shanghai 200433, China. liujianming@126.com.
authors.forename: Jianming
authors.initials: J
authors.lastname: Liu
authors.affiliation: Department of Anesthesiology, Shanghai Pulmonary Hospital, Tongji University School of Medicine, 507 Zhengmin Road, Yangpu District, Shanghai 200433, China. xinlvph@163.com.
authors.forename: Xin
authors.initials: X
authors.lastname: Lv
mesh_terms: D000779:Anesthetics, Local / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry; D006207:Half-Life; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008012:Lidocaine / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D008863:Microspheres; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D012709:Serum Albumin / Q000737:chemistry / Q000378:metabolism
chemical_list: D000779:Anesthetics, Local; D004337:Drug Carriers; D012709:Serum Albumin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D008012:Lidocaine