title: Transcriptional transactivator peptide modified lidocaine-loaded nanoparticulate drug delivery system for topical anesthetic therapy.
abstract: OBJECTIVE
  For the topical anesthetic, transcriptional transactivator peptide (TAT) modified lidocaine (LID) loaded nanostructured lipid carriers (TAT-NLCs-LID) were prepared and then used for improving transdermal delivery of local anesthetic drug.
  
  
  METHODS
  In this study, TAT was conjugated with Distearoyl phosphatidylethanolamine-(polyethylene glycol)2000-maleimide (DSPE-PEG2000-Mal) to obtain TAT-PEG2000-DSPE. TAT-NLCs-LID were successfully prepared and characterized by determination of their particle size, morphology, drug encapsulation efficiency and in vitro drug release behavior. The skin permeation of LID-LNPs was examined using a Franz diffusion cell mounted with depilated mouse skin in vitro and in vivo anesthesia effect was evaluated on mice.
  
  
  RESULTS
  The results showed that TAT-NLCs-LID have substantially small mean diameter (157.9 nm) and high encapsulation efficiency (81.8%). From the in vitro skin permeation results, transdermal flux of TAT-NLCs-LID was about several times higher than that of LID solution and NLCs-LID. In vivo anesthesia effect evaluation illustrated that TAT-NLCs-LID can enhance the transdermal delivery of LID by reducing the pain threshold in mice.
  
  
  CONCLUSIONS
  These results indicate that the novel TAT containing drug delivery system is very useful for overcoming the barrier function of the skin and could deliver anesthetic through the skin. TAT-NLCs-LID could function as promising topical anesthetic system.
authors.affiliation: a Department of Anorectal Surgery and.
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.affiliation: b Department of Anesthesiology , Shandong Provincial Qianfoshan Hospital, Shandong University , Ji'nan , China.
authors.forename: Shenhui
authors.initials: S
authors.lastname: Wang
authors.affiliation: b Department of Anesthesiology , Shandong Provincial Qianfoshan Hospital, Shandong University , Ji'nan , China.
authors.forename: Pengcai
authors.initials: P
authors.lastname: Shi
mesh_terms: D000279:Administration, Cutaneous; D000779:Anesthetics, Local / Q000008:administration & dosage / Q000737:chemistry*; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation; D015696:Gene Products, tat / Q000737:chemistry*; D008012:Lidocaine / Q000008:administration & dosage / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry; D008301:Maleimides / Q000737:chemistry; D051379:Mice; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry; D010316:Particle Size; D010539:Permeability; D010714:Phosphatidylethanolamines / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
chemical_list: C519184:1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 2000); D000779:Anesthetics, Local; D004337:Drug Carriers; D015696:Gene Products, tat; D008055:Lipids; D008301:Maleimides; D010714:Phosphatidylethanolamines; C043592:maleimide; D011092:Polyethylene Glycols; D008012:Lidocaine
keywords: Lidocaine; local anesthetics; nanostructured lipid carriers; transcriptional transactivator peptide; transdermal drug delivery