Preparation Of Transdermal Administration Of Lappaconitine Liposome Gel

This project is aimed at the clinical application of the common dosage form of lappaconitine on the market.According to the nature of lappaconitine,liposome technology was first used in the study of transdermal delivery system of lappaconitine.The sustained-release liposome gel preparation has the disadvantages of improving the short half-life of lappaconitine,low oral bioavailability,and large side effects.Through the preparation process and quality evaluation of the system,the research on the high-transformation of the external liposome gel dosage form can not only avoid the oral first-pass effect and gastrointestinal damage,but also the liposome encapsulation.The technology will significantly enhance the ability of lappaconitine to penetrate the skin,allowing it to be quickly percutaneously absorbed,and form a drug reservoir in the skin,prolonging the action time of the drug and better exerting the analgesic effect of the drug.This paper mainly completed the following research work:1.Preparation of Lappaconitine liposomes by classical liposome preparation method-film dispersion method and ethanol injection method,using orthogonal design experiments to optimize the formulation process,taking the encapsulation efficiency and drug loading of liposomes as reference indicators,the best preparation process of the two methods is obtained respectively.The physicochemical properties of the liposomes prepared by the two methods were compared,and the best method was selected.The bestprescription for the high-yield liposome gel was screened by single factor.2.The in vitro release process of lappaconitine liposomes was explored by in vitro dialysis bag experiments and in vitro transdermal experiments.The results show that the release process of the lappaconoid liposome gel conforms to the Higuchi equation;the lappaconoid liposome gel has a sustained release effect and can significantly increase the skin retention relative to the lappaconitine gel.3.Quality Evaluation.The particle size,zeta potential,PDI,encapsulation efficiency,drug loading and leakage rate of the three batches of Lappaconitine liposomes were detected,and the stability of Lappaconitine liposomes was investigated under different storage conditions.To evaluate the quality of lappaconitine liposome gel,and to investigate the initial stability of lappaconitine gel under high temperature,centrifugation and illumination.The results show that at 30 days,the zeta potential,PDI and particle size of lappaconitine liposomes do not change much,but the encapsulation efficiency,drug loading and leakage rate changed significantly.At 60 days,lappaconitine condensation The gel is more stable at 4℃ and protected from light.4.Pharmacodynamic experiments and skin irritation experimental studies.The effects of the two preparations on the hot plate method,the writhing test and the adjuvant arthritis test in mice were compared between the high-enduate liposome gel and the lappaconitine gel.The rabbit skin test was used to investigate the skin irritation of lappaconitine liposome gel.The results show that the lappaconitine liposome gel has a better anti-inflammatory and analgesic effect than the lappaconitine gel and is non-irritating.