木芙蓉叶总黄酮可溶性微针的制备及其性能评价  

Preparation and performance evaluation of soluble microneedles of total flavonoids from hibiscus leaves

作　　者：谢树才 陈晓兰 万静 邓铋莉 董娜娜 胡娟 XIE Shu-cai;CHEN Xiao-lan;WAN Jing;DENG Bi-li;DONG Na-na;HU Juan(Guizhou University of Traditional Chinese Medicine,Guiyang 550025,China;Bijie Medical College,Bijie 551700,China)

机构地区：[1]贵州中医药大学,贵阳550025 [2]毕节医学高等专科学校,毕节551700

出　　处：《中国新药杂志》2024年第2期177-186,共10页Chinese Journal of New Drugs

基　　金：贵州省普通高等学校科技拔尖人才支持计划项目:木芙蓉总黄酮可溶性微针系统的构建及评价(黔教合KY字[2018]051);贵州省国内一流建设学科项目(中药学):中药民族药新剂型新工艺的系统研究(GNYL[2017]008)

摘　　要：目的:制备木芙蓉叶总黄酮(total flavonoids in Hibiscus leaves,TFH)可溶性微针(dissolving microneedles,DMNs),并考察其理化性质及体外透皮性能.方法:采用离心法制备木芙蓉叶总黄酮可溶性微针(DMNs-TFH),单因素考察可溶性微针的基质比例、基质与溶剂比例、干燥条件,Box-Behnken响应面优化微针基质用量,最终确定微针的制备工艺参数.采用HPLC法测定其载药量,体视显微镜观察其外貌形态,HE染色观察其穿刺性能.并结合Franz扩散池考察其体外透皮性能.结果:TFH的最佳处方为Gantrez S-97∶聚乙烯醇(PVA)=1.5∶1,基质与溶剂的比例为1∶4,制得DMNs-TFH针体呈圆锥形,表面平整,长度约为550μm,每片面积为2.79 cm2,含药量(以芦丁计)为(1.0806±0.026)mg,针尖药物含量占10%.体外透皮结果显示,24h后DMNs-TFH中总黄酮的累积渗透率可达70%,而TFH溶液则透过很少,证明可溶性微针对TFH透皮递送具有良好的促进作用,能有效穿透离体皮肤.结论:制备的DMNs-TFH机械强度好、载药量大,实现了TFH的透皮递送.Objective:To prepare soluble microneedles of total flavonoids in Hibiscus leaves(TFH)and investigate their physicochemical properties and transdermal properties in vitro.Methods:The soluble microneedles were prepared by centrifugation,the substrate proportion,substrate to solvent proportion and drying conditions were investigated,the substrate amount was optimized by Box-Behnken response surface method,and the preparation process parameters of microneedles were finally determined.The drug loading was measured by HPLC,the physical appearance was observed by body optic microscope,and its puncture performance was evaluated by HE staining.The in vitro transdermal properties were investigated by combination with the Franz diffusion pool.Results:It was determined that the best prescription of total flavonoids soluble microneedle was gantrez s-97∶polyvinyl alcohol(PVA)=1.5∶1,the ratio of matrix to solvent was 1∶4,and the needle body of DMNs-TFH was conical,the surface was flat,and the length was about 550μm.The area of each tablet was 2.79 cm2,the drug content(calculated by rutin)was(1.0806±0.026)mg,and the drug content needle tip accounts for 10%.The results of in vitro skin penetration showed that the cumulative permeability of total flavonoids in DMNs-TFH could reach 70%after 24 hours,while the penetration of TFH solution was very little,which proved that soluble micro had good promoting effect on TFH transdermal delivery and could effectively penetrate the isolated skin.Conclusion:The prepared DMNs-TFH have good mechanical strength and large drug loading,which realizes the transdermal delivery of TFH.

关 键 词：木芙蓉叶总黄酮 芦丁 可溶性微针 性能 

分 类 号：R943[医药卫生—药剂学]