Preliminary Study On Permeability In Vitro And Pharmacodynamics Of New Type Oral Topical Anesthetic

Objective:To study the character of permeation through mouse skin in vitro of lidocaine hydrochloride-loaded lysine modified chitosan polymeric liposomes (LID-CLs) and its Efficacy of whole animal studies and in vitro animal experiments.Methods:LID-CLs 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-CLs, lidocaine hydrochloride-loaded conventional liposomes (LID-CLs) and lidocaine hydrochloride injection. Through the Toad sciatic nerve anesthesia experiments, the hot plate test in mice and rabbit corneal reflection experiment to evaluate the anesthetic effect of LID-TAT-PLs,LID-CLs and LID-IJ.Results:The permeation rate and cumulative permeation amount of LID-CLs were higher than those of LID-CLs and lidocaine hydrochloride injection,5min after administration had drug through, the24h cumulative transmission rate (88.15±11.11)%, significantly higher than the LID-CLS ((73.91±12.13)%, P<0.05) and LID-IJ ((26.31±5.43)%, P<0.01); The toad sciatic nerve block anesthesia of LID-TAT-PLs were stronger than those of LID-CLs and lidocaine hydrochloride injection. A significant difference received after administration5minutes (P<0.05); The pain threshold of mice of LID-TAT-PLs were significantly improved than LID-CLs (t=4.016, P<0.05) and LID-IJ (t=5.652, P<0.05); LID-TAT-PLs on the corneal surface anesthetic effects, and the ability to extend the duration of anesthesia, no significant stimulation of the cornea.Conclusions:The preparation of LID-TAT-PLs were simple. LID-TAT-PLs had good permeation in vitro and narcotic effect of animal experiments.