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550 μm,每片面积为2.79 cm2,含药量(以芦丁计)为(1.080 6±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.
Preparation and performance evaluation of soluble microneedles of total flavonoids from hibiscus leaves
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 550 μ m.The area of each tablet was 2.79 cm2,the drug content(calculated by rutin)was(1.080 6±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.
total flavonoids from Hibiscus leavesrutindissolving microneedlesperformance
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