联用纳米技术与促渗剂改善滇白珠提取物的透皮行为  

Improved transdermal behavior of Gaultheria leucocarpa extract via combined application of nanotechnology and permeation enhancers

作　　者：王皎 杨月蕊 鲁晓蓉 折改梅[3] 王文苹 WANG Jiao;YANG Yue-rui;LU Xiao-rong;SHE Gai-mei;WANG Wen-ping(School of Chinese Materia Medica and Yunnan Key Laboratory of Southem Medicinal Resource,Yunnan University of Chinese Medicine,Kunming 650500,China;Key Laboratory of External Drug Delivery System and Preparation Technology,Yunnan University of Chinese Medicine,Kunming 650500,China;School of Traditional Chinese Medicine,Beijing University of Chinese Medicine,Beijing 100029,China)

机构地区：[1]云南中医药大学中药学院,云南昆明650500 [2]云南中医药大学云南省高校外用给药系统与制剂技术研究重点实验室,云南昆明650500 [3]北京中医药大学中药学院,北京100029

出　　处：《云南民族大学学报（自然科学版）》2024年第6期705-711,共7页Journal of Yunnan Minzu University:Natural Sciences Edition

基　　金：国家自然科学基金(81660665);云南省科技厅重大科技专项计划(202103AC100005);云南省科技厅基础研究计划中医联合专项重点项目(202001AZ070001-011);云南省中青年学术和技术带头人后备人才项目(202205AC160038)。

摘　　要：为探究纳米制剂技术和促渗剂对滇白珠提取物体外透皮性能的影响,分别采用介质研磨法和薄膜分散法,将提取物制备成纳米混悬液和纳米脂质体,测定了其中总黄酮和水杨酸类成分的载药量与包封率.随后,通过Franz扩散池法,进一步评估这2种制剂在小鼠皮肤上的累积渗透率和皮内滞留量.结果发现,24 h内,脂质体水杨酸累积渗透量是纳米混悬液的1.34倍;皮内滞留量为纳米混悬液的3.78倍;不同促渗剂对累积渗透量的影响按照氮酮≈薄荷醇>丙二醇>无促渗剂的顺序递减,但对皮内滞留量的影响基本可忽略.水杨酸类成分的渗透和滞留均显著高于总黄酮.因此,纳米制剂技术、促渗剂及活性成分的性质均对体外透皮行为产生不同程度的影响,采取综合策略可提高中药制剂的经皮吸收性能.To investigate the effect of nanotechnology and penetration enhancers on the in vitro transdermal performance of Gaultheria leucocarpa var.yunnanensis extract,the extract was formulated into a nano-suspension and a nano-liposome using media milling and thin-film dispersion methods,respectively.The drug loading and encapsulation efficiency of total flavonoids and salicylic acid components were measured.Subsequently,the Franz diffusion cell method was used to further evaluate the cumulative permeation rate and skin retention of these two formulations on mouse skin.The results showed that within 24 h,the cumulative permeation of salicylic acid in the liposome was 1.34 times that of the nano-suspension,while the skin retention was 3.78 times higher.The effects of different penetration enhancers on the cumulative permeation volume decrease in the order of azone≈menthol>propylene glycol>no penetration enhancer,but their effect on skin retention was negligible.The permeation and retention of salicylic acid were significantly higher than those of total flavonoids.Therefore,nanotechnology,penetration enhancers,and the properties of active ingredients all have varying effects on in vitro transdermal behavior,and a comprehensive strategy should be adopted to improve the transdermal absorption performance of traditional Chinese medicine formulations.

关 键 词：滇白珠 脂质体 纳米混悬液 透皮性能 相互作用 

分 类 号：R285.5[医药卫生—中药学]