| Background:Androgenic Alopecia(AGA),also known as seborrheic alopecia,is a skin disorder characterized by progressive hair loss that occurs during puberty or later adolescence,and is the most common form of hair loss.Due to the long treatment cycle of AGA,poor patient compliance,many adverse reactions of long-term oral drugs,and the high cost of non-drug treatment,it is of great significance to develop AGA therapeutic drugs with new targets.In 2017,it was first reported that the topical application of 1%cetirizine alcohol solution in the treatment of AGA has obvious curative effect.In view of the poor skin penetration and strong irritation of the ethanol solution,this study aimed to prepare a cetirizine hydrochloride for the treatment of AGA.Tirizine liposome gel preparation,and the quality and pharmacodynamics of the preparation were preliminarily investigated.Method:①Establish a high-performance liquid chromatography(HPLC)method for the determination of cetirizine hydrochloride,and verify the methodology.②Preparation of cetirizine hydrochloride liposome gel.The suitable method for preparing liposome was screened,and the encapsulation rate was used as the investigation index,and the ratio of soybean lecithin to cholesterol,the dosage of cetirizine hydrochloride,the hydration time,the hydration temperature and the amount of PBS were investigated by single factor test 5 The influence of these factors on the encapsulation efficiency of cetirizine hydrochloride liposomes,and then the preparation process was optimized through orthogonal experiments to determine the optimal formulation,and the physicochemical properties of the liposomes were investigated;Carbomer-940 was used as the Gel matrix,the preparation prescription of liposome gel was determined by investigating the content of carbomer-940 and the pH of the gel,and the cetirizine hydrochloride liposome was tested by appearance,pH value,centrifugation test and temperature test.Evaluate the quality of the gel;③To investigate the safety of cetirizine hydrochloride liposome gel on the intact and damaged skin of New Zealand rabbits.④ Preliminary pharmacodynamic study.To observe the effect of cetirizine hydrochloride liposome gel on hair growth in alopecia model mice.Result:①Establish a method for determination of cetirizine hydrochloride content with good specificity and high sensitivity;use thin film dispersion method to prepare cetirizine hydrochloride liposomes,and determine the best formulation process of cetirizine hydrochloride liposome gel:soybean Lecithin:cholesterol=5:1,the dosage is 25mg,the hydration temperature is 50℃,the hydration time is 0.5h,and the amount of PBS is 5ml;The encapsulation efficiency of the liposome solution was 74.11%,the drug loading was 5.12%,the particle size was(174.6±1.2)nm,the Zeta potential was(-43.2±1.6)mV,and the PDI was 0.263±0.013.The liposomes were observed under transmission electron microscopy.It is round-like,and the drug can be seen to be successfully encapsulated inside the liposome.②The prescription of liposome gel is:0.2g carbomer-940,10ml cetirizine hydrochloride liposome solution,2g glycerol,16mg ethylparaben,add distilled water to 20g,and finally add 0.35g triethanolamine By adjusting pH and consistency,the prepared liposome gel has uniform texture and good stability.③Animal experiments show that the prepared cetirizine hydrochloride liposome gel has no skin irritation and is safe.④Preliminary pharmacodynamic experiments showed that it has a promoting effect on the growth of back hair in mice.Conclusion:The cetirizine hydrochloride liposome gel prepared in this study is simple in process,stable in quality,easy to use,safe and effective in treating alopecia.The research results can provide a reference for the development of transdermal preparations for androgenetic alopecia. |
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