title: [Preliminary study on transdermal characteristics and sunface anesthetic effects of lidocaine hydrochloride loaded trans-activator of transcription peptide conjugated nano-niosome in animals].
abstract: OBJECTIVE
  To prepare a new dental topical anesthetics, lidocaine hydrochloride loaded trans-activator of transcription peptide conjugated nano-niosome (LID-TAT-N), and to evaluate its transdermal properties and topical anesthesia effects.
  
  
  METHODS
  LID-TAT-N was prepared using reverse-phase evaporation method, and lidocaine loaded conventional liposome (LID-CL) was prepared in the same manner as positive control. The diameter, ζ potential and encapsulation efficiency of LID-TAT-N and LID-CL were measured. The skin permeation of LID-TAT-N was examined, and compared with LID-CL and lidocaine injection (LID-IJ, as negative control), using a Franz diffusion cell mounted with depilated mouse skin in vitro for 12 hours. Each experiment was repeated six times. The anesthetic effect of the new topical anesthetic was investigated on the cornea of rabbits.
  
  
  RESULTS
  The mean diameter of LID-TAT-N was smaller than that of LID-CL [(152.7 ± 10.6) nm vs. (259.5 ± 15.5) nm, P < 0.01]. The 12 h cumulative permeation amount was significantly higher in LID-TAT-N group [(1 340.0 ± 97.5) µg · cm(-2)] than those of LID-CL and LID-IJ groups [(1 060.6 ± 80.2), (282.6 ± 65.1) µg · cm(-2), respectively, P < 0.05]. Rabbit corneal reflex results showed that LID-TAT-N had anesthetic effect and the duration of analgesia [(24.8 ± 2.8) min] was also longer than that of LID-IJ [(14.5 ± 2.3) min, P < 0.05].
  
  
  CONCLUSIONS
  LID-TAT-N had good transdermal ability, and the advanced skin penetration feature can improve its tropical anesthetic effect.
authors.affiliation: Department of Orthodontics, Stomatological Hospital, Tianjin Medical University, Tianjin 300070, China.
authors.forename: Yue
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Department of Prosthodontics, Stomatological Hospital, Tianjin Medical University, Tianjin 300070, China; Email: namezhanglianyun@tom.com.
authors.forename: Lianyun
authors.initials: L
authors.lastname: Zhang
authors.forename: Changyi
authors.initials: C
authors.lastname: Li
authors.forename: Hanjie
authors.initials: H
authors.lastname: Wang
authors.forename: Qin
authors.initials: Q
authors.lastname: Li
mesh_terms: D000279:Administration, Cutaneous; D000766:Anesthesia, Dental; D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D001767:Blinking / Q000187:drug effects / Q000502:physiology; D003315:Cornea / Q000187:drug effects / Q000502:physiology; D008012:Lidocaine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008081:Liposomes; D051379:Mice; D058726:Nanoconjugates / Q000008:administration & dosage* / Q000737:chemistry; D010455:Peptides; D011817:Rabbits; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D015534:Trans-Activators / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D000779:Anesthetics, Local; D008081:Liposomes; D058726:Nanoconjugates; D010455:Peptides; D015534:Trans-Activators; D008012:Lidocaine