Abstract:

[Abstract] Objective  To prepare the lidocaine hydrochloride-loaded transactivation (TAT) conjugated octadecyl quaternized lysine modified chitosan polymeric liposomes (LID-TAT-PLs) and to study its in vitro skin permeation characters in mice. Methods  LID-TAT-PLs were prepared by reverse-phase evaporation method. The concentrations of lidocaine hydrochloride were determined by HPLC. The isolated mouse skin and Franz diffusion cell were used to evaluate the characters of permeation of LID-TAT-PLs, LID-PLs and lidocaine hydrochloride injection (LID-IJ). Results  The permeation rate and cumulative permeation amount were significantly higher in LID-TAT-PLs group than those of LID-PLs and LID-IJ groups (P ＜0.05). Conclusion  TAT can significantly enhance the transdermal permeation of drugs in mice. The LID-TAT-PLs can be prepared via a relatively simple method.

Key words: lidocaine hydrochloride, octadecyl quaternized lysine modi?ed chitosan, transactivation, polymetric liposomes, permeation through skin