Abstract:

[Abstract] Objective  To prepare the lidocaine hydrochloride-loaded lysine modified chitosan polymeric liposomes (LID-PLs) and to study its permeation characteristics through mouse skin in vitro. Methods  LID-PLs and lidocaine hydrochloride-loaded conventional liposomes (LID-CLs) were prepared by reverse-phase evaporation method. The diameter and zeta potential of LID-PLs and LID-CLs were determined by dynamic light scattering (DLS) using a Brookhaven Zetasizer. A HPLC method of determination of lidocaine hydrochloride was established. The isolated mouse skin and Franz diffusion cells were used to evaluate the permeation characteristics of LID-PLs, LID-CLs and lidocaine hydrochloride injection (LID-IJ). Results  The diameter of LID-PLs was significantly smaller than that of LID-CLs (61.2±8.14 nm vs 219±7.51 nm). The specificity of HPLC was high and the standard curve equation was =0.051X-2.701，r=0.999 9. The mean cumulative permeation of lidocaine was significantly higher at 5 min,10 min, 30 min, 2 h, 4 h, 6 h, 8 h, 12 h and 24 h after administration in LID-PLs group than those in LID-CLs group and LID-IJ group (P < 0.05 or P < 0.01). The mean cumulative permeation of lidocaine was significantly higher in LID-CLs group than that in LID-IJ group at 10 min, 30 min, 1.5 h, 2 h, 4 h, 6 h, 8 h, 12 h and 24 h after administration (P < 0.05 or P < 0.01). Conclusion  The preparation of LID-PLs is simple and it has good permeation in vitro. The HPLC method is accurate and reliable.

Key words: lidocaine hydrochloride, lysine modified chitosan, polymeric liposomes , in vitro, permeation through skin