摘要
羟基频哪酮视黄酸酯(HPR)作为新型维生素A衍生物,存在光热稳定性差、水溶性低等缺点,导致其透皮治疗效果较差。为了提高HPR的透皮性能,将HPR与生育酚乙酸酯(VE)复配,采用超重力技术制备了HPR/VE纳米乳。在超重力水平为8、循环乳化时间5 min的优化条件下制备的HPR/VE纳米乳(HPR质量分数为0.6%~3.7%)的粒径为89.7~131 nm,多分散指数(PDI)为0.13~0.15,液滴呈现规则的球形。在4℃和25℃下储存3个月,HPR/VE纳米乳的粒径、HPR含量、pH和zeta电位均无明显变化;在3000 r/min下离心30 min,纳米乳的粒径及PDI均未发生显著变化,并且无晶体析出或乳液分层现象。皮肤渗透实验结果显示,HPR/VE纳米乳的12 h累积渗透量为8.33μg/cm^(2),皮内驻留量为17.07μg/cm^(2),其12 h累积渗透量分别是市售乳剂和原料药的2倍和4倍,皮内驻留量分别是市售乳剂和原料药的1.5倍和2.8倍。研究结果表明,基于超重力技术制备的HPR/VE纳米乳液具有粒径小、分布均匀、形貌规整等特点,并表现出良好的储存稳定性和皮肤渗透性,在经皮给药领域具有潜在的应用价值。
As a new vitamin A derivative,hydroxypinacolone retinoate(HPR)has the disadvantages of poor photothermal stability and low water solubility,resulting in poor transdermal therapeutic effects.In order to improve the transdermal performance of HPR,it was combined with tocopherol acetate(VE),and HPR/VE composite nanoemulsions were prepared using high‑gravity technology.The average particle size of the HPR/VE nanoemulsions(with mass fractions of HPR in the range 0.6%-3.7%)prepared under the optimized conditions of a high‑gravity level of 8 and a cyclic emulsification time of 5 min was in the range 89.7-131 nm,the polydispersity index(PDI)was 0.13-0.15,and the droplets had a regular spherical morphology.There were no significant changes in the particle size,drug loading of HPR,pH and zeta potential of the HPR/VE nanoemulsions after being stored at 4℃and 25℃for 3 months.After centrifugation at 3000 r/min for 30 min,the particle size and PDI of the nanoemulsion had not changed significantly,and there was no crystal precipitation or emulsion stratification.Skin penetration experiments showed that the cumulative penetration amount of the HPR/VE nanoemulsion within 12 hours was 8.33μg/cm^(2),and the intradermal retention amount was 17.07μg/cm^(2).The cumulative penetration amounts within 12 hours are 2 times and 4 times that of the commercially available emulsion and the crude drug,respectively.The intradermal retention amounts are 1.5 times and 2.8 times that of the commercially available emulsion and the crude drug,respectively.The results show that the HPR/VE nanoemulsion prepared using high‑gravity technology has the characteristics of small particle size,uniform distribution and regular morphology,and exhibits good storage stability and skin permeability,suggesting it has potential applications in the field of transdermal drug delivery.
作者
辛宇
盛虹瑞
左先波
乐园
XIN Yu;SHENG HongRui;ZUO XianBo;LE Yuan(State Key Laboratory of Organic−Inorganic Composites,Beijing University of Chemical Technology,Beijing 100029;Big Data Center of Information Department,China−Japan Friendship Hospital,Beijing 100029;Research Center of the Ministry of Education for High Gravity Engineering and Technology,Beijing University of Chemical Technology,Beijing 100029,China)
出处
《北京化工大学学报(自然科学版)》
北大核心
2025年第4期1-9,共9页
Journal of Beijing University of Chemical Technology(Natural Science Edition)
基金
中日友好医院高水平医院临床业务费专项成果转化项目(2023-NHLHCRF-YXHZ-ZRZD-06)。
关键词
超重力技术
纳米乳
羟基频哪酮视黄酸酯
生育酚乙酸酯
经皮渗透
high-gravity technology
nanoemulsion
hydroxypinacolone retinoate
tocopherol acetate
percutaneous osmosis
