Studies On Ultrasound Sunburn Treatment Compound Capsaicin Nanoemulsion Gel

OBJECTIVE: To prepare and evaluate a ultrasound sunburn treatment nanoemulsion gel for chronic injury of soft tissue.METHODS: Take the compound capsaicin cream as a model drug, formulated compound capsaicin nanoemulsion gel. The compound drug and distilled water were used to prepare compound capsaicin O/W nanoemulsion. Tween80 used as surfactant, and pseudo-ternary phase diagram was used to optimize the cosurfactant prescription, the ratio and the amount of mixed surfactants. With carbomer940 used as the gel matrix, capsaicin nanoemulsion as raw material medicine, Azone, 1, 2- propylene glycol, glycerin and PEG400 as penetration enhancers, prepared nanoemulsion gel. Using Franz diffusion cell for in vitro transdermal osmosis course study of gel .The optimum formulation of gel was selected regarding the cumulative amount of capsaicin across the rat skin in vitro transdermal osmosis as the index with orthogonal design. And study on the permeation kinetics and ultrasonic conditions. The optimum condition of ultrasonic penetration was selected with the index ofcumulative amount of capsaicin across the rat skin in vitro. Elementary preparation stability was investigated. Establish an method to determine the capsaicin in ultrasound sunburn treatment compound capsaicin nanoemulsion gel by HPLC. The skin irritation test and elementary pharmacodynamics studies of ultrasound sunburn treatment compound capsaicin nanoemulsion gel was conducted.RESULTS: The optimum formulation of compound capsaicin nanoemulsion was drugs mixed as oil phase of the nanoemulsion, Tween80 as surfactant, 1,2 - propanediol as cosurfactant, Km = 3:1. The ratio of each component of nanoemulsion was mixed oil 13.04%, Tween80/propylene glycol 34.78%, and water 52.17%. The optimum formulation of the gel was 1% carbomer940 +1% azone +20% propylene glycol +20% glycerol +1% PEG400. The best condition of ultrasound penetration is 1.5W(305KHz), 3min. Without ultrasound, the percutaneous permeation kinetics curve of the gel in vitro was Higuchi order, the equation was Q = 0.6593t^1/2 +0.2665, r = 0.9957; With ultrasound, the percutaneous permeation kinetics curve in vitro was First-order, the equation was ln(1-Q)=-0.0135t+4.595, r = 0.9978. The result of preliminary stability tests indicated that ultrasound sunburn treatment compound capsaicin nanoemulsion gel was stable, the appearance and spread and the drug content were not significant changed in speed up test of 30℃±2℃, RH65%±5% conditions in 0,1,2,3,6 months. Primary skin irritation test and pharmacodynamics experiments showed that ultrasound sunburn treatment compound capsaicin nanoemulsion gel had no significant skin irritation, significantly lengthen the reaction latent period of mousse hotboard, inhited inffammation of mousse auricle which caused by xylenl, caused a certain effect on chronic soft tissue injury in rats which caused by impact.CONCLUSION: The preparation of ultrasound sunburn treatment compound capsaicin nanoemulsion gel is reasonably and practicable, the compound capsaicin nanoemulsion gel has no significant skin irritation, with the effect of ultrasound sunburn treatment, the drugs release fast and long lasting, with a dual role of quick and slow release, it has anti-inflammatory and analgesic effects, and a effect on chronic soft tissue injury.