维生素C葡萄糖苷可溶性微针的制备和评价  

Preparation and evaluation of the ascorbic acid 2-glucoside loaded dissolving microneedles

作　　者：李华东 胡艳萍 李佳欣 廖朗坤 邱玉琴 LI Huadong;HU Yanping;LI Jiaxin;LIAO Langkun;QIU Yuqin(School of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China)

机构地区：[1]广东药科大学药学院,广东广州510006

出　　处：《广东药科大学学报》2023年第2期1-6,共6页Journal of Guangdong Pharmaceutical University

基　　金：2021年度省级大学生创新创业训练计划(S202110573031)。

摘　　要：目的 优化维生素C葡萄糖苷可溶性微针的处方及制备工艺,并对其进行评价。方法 根据吸湿性、机械强度、基底柔性筛选微针基质材料,采用两步法制备维生素C葡萄糖苷可溶性微针。以荧光素钠为模型药物筛选背衬溶剂,通过质构仪测定微针的硬度,结合模拟皮肤穿刺实验和台盼蓝染色法考察微针的皮肤穿刺能力。采用改良的Franz扩散池评价载药微针的体外经皮渗透性。结果 PVP K90微针机械强度最高,且基底具有一定柔性,因此优选20%PVP K90作为微针基质溶液。当背衬溶剂为乙醇时,针尖药物利用率较高。载药微针的机械强度较高,能够刺穿大鼠角质层。体外透皮试验表明,与水溶液透皮相比,微针能使维生素C葡萄糖苷的8 h累积透过量提高3倍。结论 可溶性微针能够促进维生素C葡萄糖苷的体外经皮渗透。Objective To optimize the formulation and preparation process of ascorbic acid 2-glucoside loaded dissolving microneedles and evaluate it.Methods Microneedle materials were optimized according to the hygroscopicity,mechanical strength and flexibility.The ascorbic acid 2-glucoside loaded dissolving microneedles were prepared by a two-step method.Sodium fluorescein was used as a model drug to screen the backing solvent.The hardness of microneedle was measured by texture analyzer,and the skin puncture ability of microneedle was investigated by a simulated skin puncture test and trypan blue staining.The in vitro percutaneous permeability of drug-loaded microneedles was evaluated by improved Franz diffusion cell.Results Owing to the relatively high mechanical strength and the flexibility,20% PVP K90 was selected as the microneedle matrix solution.When the backing solvent was ethanol,the drug utilization rate of needle tip was higher.The mechanical strength of drug-loaded microneedles was enough to pierce the stratum corneum of rats.The in vitro transdermal permeation study showed that DMNs could increase the cumulative amount of ascorbic acid 2-glucoside by 3 times compared with that of aqueous solution.Conclusion Dissolving microneedles can improve the transdermal permeation of ascorbic acid 2-glucoside.

关 键 词：可溶性微针 维生素C葡萄糖苷 吸湿性 机械强度 体外经皮渗透试验 

分 类 号：R943[医药卫生—药剂学]