摘要
为了提高木犀草素的生物利用度,改善急性乳腺炎治疗顺应性,以期给乳腺炎患者提供一种新型的用药选择,采用浇注法成功制备了木犀草素全载药可溶性微针(LUT-DMN)。单因素考察可溶性微针的基质种类、基质比例、溶剂种类及用量、干燥条件,正交优选微针基质比例、溶剂用量,最终确定微针的最佳制备工艺参数,从外观形态、机械强度、溶解性能、皮肤屏障恢复性能等方面对其进行评价;采用高效液相色谱(HPLC)法测定LUT-DMN载药量,利用Franz扩散池对载药微针进行体外透皮释药性能考察。得到最优处方:PVA与Gantrez S-97质量比为1∶3,溶剂用量9 mL。每片载药量为(1.068 3±0.037 0)mg,机械性能良好。作用于大鼠皮肤2 h时针尖几乎完全溶解,2 h后皮肤恢复情况良好。体外透皮试验结果显示,48 h时LUT-DMN累积透过率达87.14%。LUT-DMN的成型和机械性能良好,相比于药物基质溶液组,其具有显著透皮性能,可促进药物透皮吸收。
In order to improve the bioavailability of luteolin and the treatment compliance of acute mastitis,and provide a new drug choice for patients with mastitis,soluble microneedles loaded with luteolin(LUT-DMN)were successfully prepared by casting method.The matrix types,matrix ratios,solvent types and dosages,and drying conditions of soluble microneedles were investigated by single factor.The matrix ratio and solvent dosage of microneedles were optimized by orthogonal optimization.Finally,the optimal preparation process parameters of microneedles were determined,and they were evaluated from the aspects of appearance,mechanical strength,solubility and skin barrier recovery performance.The drug loading of LUT-DMNs was determined by high performance liquid chromatography(HPLC)method,and the in vitro transdermal release performance of drug-loaded microneedles was investigated by Franz diffusion cell.The optimal prescription was obtained.The mass ratio of PVA and Gantrez S-97 is 1∶3,and the solvent dosage is 9 mL.The drug loading of each tablet is(1.0683±0.0370)mg and the mechanical properties are good.The needle tip is almost completely dissolved after 2 h of action on the rat skin,and the skin recovery is good after 2 h of action on the rat skin.The results of in vitro transdermal test show that the cumulative permeability of LUTDMNs reaches 87.14%at 48 h.LUT-DMN has good molding and mechanical properties.Compared with the drug matrix solution group,it has significant transdermal properties to promote drug transdermal absorption.
作者
姜林丽
陈晓兰
卢文钗
叶超
雷雪莲
余龙腾
Jiang Linli;Chen Xiaolan;Lu Wenchai;Ye Chao;Lei Xuelian;Yu Longteng(School of Pharmacy,Guizhou University of Traditional Chinese Medicine,Guiyang 550025,China)
出处
《微纳电子技术》
CAS
2024年第11期128-137,共10页
Micronanoelectronic Technology
基金
贵州中医药大学大学生创新创业训练计划项目(贵中医大创合字[2022]35号)
贵州省基础研究计划(自然科学类)(黔科合基础-ZK[2023]一般407)。
关键词
木犀草素
急性乳腺炎
可溶性微针
正交试验
体外透皮
luteolin
acute mastiti
soluble microneedle
orthogonal experiment
transdermal in vitro
作者简介
通信作者:陈晓兰。
