title: Transdermal anaesthesia with lidocaine nano-formulation pretreated with low-frequency ultrasound in rats model.
abstract: Rapid local transdermal anaesthetic is desirable in clinic. In this paper, lidocaine loaded poly(epsilon-caprolactone)-poly(ethylene glycol)-poly(epsilon-caprolactone) (PCL-PEG-PCL) nanoparticles were prepared, and a novel transdermal lidocaine formulation: lidocaine loaded PCL-PEG-PCL nanoparticles in F127 hydrogel (Nano-Lido Gel), was demonstrated. These lidocaine loaded PCL-PEG-PCL nanoparticles with mean particle size of ca. 200 nm had drug loading of about 40%. The efficiency of transdermal anaesthesia of four treatments: EMLA cream (E), Nano-Lido Gel (N), EMLA cream with brief focal ultrasound pretreatment (EU), and Nano-Lidocaine Gel with brief focal ultrasound pretreatment (NU), was evaluated by tail-flick latency test assay in rats. Results indicated that the topical anaesthesia onset time in NU was 5 times and 2.5 times shorter than that in E and EU. The efficiency of anaesthesia in NU, expressed as maximum possible effects (MPE) value, was significantly higher than that in other treatments. It provided a novel path to develop rapid transdermal anaesthesia by combination of ultrasound pretreatment and lidocaine nano-formulation based on polymeric nanoparticles.
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center West China Hospital, West China Medical School, Sichuan University, Chengdu, 610041, China.
authors.forename: MaLing
authors.initials: M
authors.lastname: Gou
authors.forename: Lan
authors.initials: L
authors.lastname: Wu
authors.forename: QinQin
authors.initials: Q
authors.lastname: Yin
authors.forename: QingFa
authors.initials: Q
authors.lastname: Guo
authors.forename: Gang
authors.initials: G
authors.lastname: Guo
authors.forename: Jin
authors.initials: J
authors.lastname: Liu
authors.forename: Xia
authors.initials: X
authors.lastname: Zhao
authors.forename: YuQuan
authors.initials: Y
authors.lastname: Wei
authors.forename: Zhiyong
authors.initials: Z
authors.lastname: Qian
mesh_terms: D000279:Administration, Cutaneous; D000779:Anesthetics, Local / Q000008:administration & dosage; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry* / Q000528:radiation effects; D004339:Drug Compounding / Q000379:methods; D008012:Lidocaine / Q000008:administration & dosage* / Q000737:chemistry; D049329:Nanostructures / Q000737:chemistry* / Q000528:radiation effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D013010:Sonication / Q000379:methods*
chemical_list: D000779:Anesthetics, Local; D004337:Drug Carriers; D008012:Lidocaine