雪上一枝蒿生物碱水凝胶微针的制备及体外透皮研究  

Preparation of Hydrogel Microneedles of Alkaloid in Aconitum Brachypodum and In Vitro Transdermal Studies

作　　者：邓琴 陈晓兰 邓铋莉 徐剑 黄耀磊 谌文元 Deng Qin;Chen Xiaolan;Deng Bili;Xu Jian;Huang Yaolei;Chen Wenyuan(School of Pharmacy,Guizhou University of Traditional Chinese Medicine,Guiyang 550025,China)

机构地区：[1]贵州中医药大学药学院,贵阳550025

出　　处：《微纳电子技术》2024年第7期162-170,共9页Micronanoelectronic Technology

基　　金：贵州省基础研究计划(自然科学类)(黔科合基础-ZK[2023]一般407);国家苗药工程技术研究中心能力提升项目(黔科合中引地[2023]006);贵州省高层次创新型人才项目(黔科合平台人才-GCC[2023]037)。

摘　　要：采用化学交联法和离心浇注法制备雪上一枝蒿生物碱水凝胶微针(HMN-AAB)并考察其理化性质及体外透皮性能。单因素考察水凝胶微针的基质用量、干燥条件。通过正交实验优化微针基质用量,最终确定微针的制备工艺参数。采用高效液相色谱(HPLC)法测定其载药量,利用扫描电子显微镜观察其形貌,通过苏木精-伊红(HE)染色法分析其穿刺性能,并结合Franz扩散池考察其体外透皮性能。HMN-AAB的最佳制备参数为:聚乙烯马来酸酐共聚物2 g,聚乙二醇10000(PEG10000)0.75 g,无水碳酸钠0.3 g。制备的HMN-AAB的载药质量分数为4%。采用离心浇注法制备微针,通过程序升温进行干燥。HMN-AAB为正方形贴片,表面光滑,阵列完整,微针针尖呈圆锥形,含药量为(4.50±0.08)mg/片(以雪上一枝蒿甲素计)。体外透皮结果显示,48 h后HMN-AAB中药物的累积渗透率可达93%,明显高于普通凝胶膏剂组,释放曲线符合Higuchi方程。制备的HMN-AAB机械强度好、载药量大,实现了AAB的透皮递送。The hydrogel microneedles of alkaloid in aconitum brachypodum(HMNs-AAB)were prepared by chemical cross-linking and centrifugal casting methods,and their physicochemical properties and in vitro transdermal properties were investigated.The matrix dosage and drying conditions of hydrogel microneedles were investigated by single factor.Orthogonal experiment was carried out to optimize the matrix dosage of microneedles,and the preparation process parameters of microneedles were finally determined.The high performance liquid chromatography(HPLC)method was used to determine the drug loading capacity,the scanning electron microscope was used to observe the morphology,the hematoxylin-eosin(HE)staining method was used to analyze the puncture performance,and the in vitro transdermal performance was investigated in combination with Franz diffusion cell.Optimal preparation parameters of HMNs-AAB are that 2 g of polyethylene maleic anhydride copolymer,0.75 g of polyethylene 10000(PEG10000),0.3 g of anhydrous sodium carbonate.The drug loading mass fraction of the prepared HMNs-AAB is 4%.Microneedles were prepared by centrifugal casting method and dried by the procedure of elevated temperature.The HMNs-AAB were square patches with smooth surfaces and intact arrays.The tip of the microneedles is conical,and the drug content is(4.50±0.08)mg/tablet(calculated by Bullatine A).The in vitro transdermal results show that the cumulative penetration rate of the drug in the HMNs-AAB can reach 93%after 48 h,which is significantly higher than that of the normal gel cream group,and the release profile is in accordance with the Higuchi equation.The prepared HMNs-AAB have good mechanical strength and large drug loading capacity,which realizing transdermal delivery of AAB.

关 键 词：雪上一枝蒿 生物碱 水凝胶微针 离心浇注法 化学交联法 

分 类 号：R944.9[医药卫生—药剂学]