title: Preparation and evaluation of lidocaine hydrochloride-loaded TAT-conjugated polymeric liposomes for transdermal delivery.
abstract: Transactivation transcriptional activator (TAT) peptides were conjugated on the octadecyl-quaternized, lysine-modified chitosan to form polymeric liposomes (TAT-PLs) with cholesterol for improving transdermal delivery of local anesthetic lidocaine hydrochloride (LID). In this study, the LID loaded TAT-conjugated polymeric liposomes (LID-TAT-PLs) have been successfully prepared. LID-TAT-PLs were characterized by determination of their particle size, polydispersity, morphology, drug encapsulation efficiency, drug release behavior in vitro, and storage-stability. The skin permeation of LID-TAT-PLs was examined using a Franz diffusion cell mounted with depilated mouse skin in vitro, and penetration of TAT-PLs was visualized by confocal laser scanning microscopy (CLSM). The results showed that LID-TAT-PLs were spherical in solution, with substantially smaller mean diameter (154.7±10.7 nm), higher encapsulation efficiency (80.05±2.64%) and better stability in contrast to conventional liposomes (CLs). From the in vitro skin permeation results, transdermal flux of LID-TAT-PLs was approximately 4.17 and 1.75 times higher than that of LID solution and LID CLs (P<0.05). CLSM studies also confirmed that TAT-PLs reached viable layers of the skin. Hence, the results indicate that LID-TAT-PLs are effective and potential alternative for the LID transdermal formulation.
authors.affiliation: School of Stomatology, Tianjin Medical University, Tianjin 300070, PR China.
authors.forename: Yue
authors.initials: Y
authors.lastname: Wang
authors.forename: Wenya
authors.initials: W
authors.lastname: Su
authors.forename: Qin
authors.initials: Q
authors.lastname: Li
authors.forename: Changyi
authors.initials: C
authors.lastname: Li
authors.forename: Hanjie
authors.initials: H
authors.lastname: Wang
authors.forename: Yuchen
authors.initials: Y
authors.lastname: Li
authors.forename: Yan
authors.initials: Y
authors.lastname: Cao
authors.forename: Jin
authors.initials: J
authors.lastname: Chang
authors.forename: Lianyun
authors.initials: L
authors.lastname: Zhang
mesh_terms: D000279:Administration, Cutaneous; D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D048271:Chitosan / Q000737:chemistry; D002784:Cholesterol / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D004355:Drug Stability; D004356:Drug Storage; D005260:Female; D015696:Gene Products, tat / Q000737:chemistry; D008012:Lidocaine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008081:Liposomes; D008239:Lysine / Q000737:chemistry; D008297:Male; D051379:Mice; D018613:Microscopy, Confocal; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D012869:Skin Absorption
chemical_list: D000779:Anesthetics, Local; D004337:Drug Carriers; D015696:Gene Products, tat; D008081:Liposomes; D011108:Polymers; D048271:Chitosan; D002784:Cholesterol; D008012:Lidocaine; D008239:Lysine