二甲双胍层状液晶的制备及对小鼠放射性皮炎的治疗效果  

Preparation of metformin lamellar liquid crystal and its therapeutic effect on radiation dermatitis in mice

作　　者：于翔 马振超[2] 朱佳伟 常皓[4] 汤恺娴 何敏[1] 郑超 Yu Xiang;Ma Zhen-chao;Zhu Jia-wei;Chang Hao;Tang Kai-xian;He Min;Zheng Chao(Institute of Electrical and Information Engineering,Hunan University,Changsha 410082,China;Center of Clinical Trials,Huzhou Central Hospital,Huzhou 313000,China;School of Pharmacy,Wenzhou Medical University,Wenzhou 325035,China;Institute of Basic Medicine and Oncology,Chinese Academy of Sciences,Hangzhou 310022,China)

机构地区：[1]湖南大学电气与信息工程学院,长沙410082 [2]湖州市中心医院临床试验中心,湖州313000 [3]温州医科大学药学院,温州325035 [4]中国科学院杭州医学研究所生物医学工程研究室,杭州310022

出　　处：《中国药物应用与监测》2024年第5期674-678,共5页Chinese Journal of Drug Application and Monitoring

基　　金：国家自然科学基金项目(82203983);湖州市医药卫生重点项目(2022GZB03)。

摘　　要：目的 构建和表征二甲双胍层状液晶,并考察该制剂对放射性皮炎的外用疗效。方法 以单油酸甘油酯、乙醇和水为基质材料,通过注入法制备二甲双胍层状液晶;采用偏光镜和小角度X光衍射进行物理表征;将计算机模拟与体外释放实验相结合阐述制剂的释药机理;利用Franz扩散池技术考察制剂的体外透皮行为;建立放射性皮炎小鼠模型,以皮肤损伤程度为指标评价制剂的治疗效果。结果 二甲双胍层状液晶具有双折射现象;同时,该样品的小角度X光散射峰对应的散射矢量比值为3:4,与传统的层状液晶空间群一致;药物主要通过扩散的形式从液晶中释放;二甲双胍层状液晶组5 h的体外透皮量[(2 190±182)μg·cm^(-2)]要显著大于二甲双胍溶液组[(979±126)μg·cm^(-2)];二甲双胍层状液晶能加快小鼠的放射性皮损恢复。结论 本研究成功制备具有高效皮肤渗透特性的二甲双胍层状液晶,该液晶在放射性损伤性疾病的治疗的预防和管理方面具有重大应用潜力。Objective To construct and characterize a lamellar liquid crystal formulation of metformin and investigate its topical efficacy in treating radiation dermatitis.Methods The metformin lamellar liquid crystal was prepared using glycerol monooleate,ethanol and water as matrix materials through the injection method.Physical characterization was conducted using polarizing mirrors and small angle X-ray diffraction.The in vitro transdermal behavior of the formulation was investigated using Franz diffusion cell technology.Additionally,a mouse model of radiation dermatitis was established to evaluate the therapeutic effect of the formulation based on the degree of skin damage.Results The lamellar liquid crystal of metformin exhibited a birefringence phenomenon.Meanwhile,its small angle X-ray scattering peak corresponded to a scattering vector ratio of 3:4,being in consistent with the traditional lamellar liquid crystal space group.Drug releasing from the liquid crystal mainly occurred through diffusion.The 5-hour in vitro transdermal dose of the metformin lamellar liquid crystal group((2190±182)μg·cm^(-2))was significantly higher than that of the metformin solution group((979±126)μg·cm^(-2)).Furthermore,the metformin lamellar liquid crystal significantly accelerated wound healing in irradiated mice.Conclusion This study successfully prepared metformin layered liquid crystals with efficient skin penetration properties,which has significant potential for application in the prevention and management of radiation-induced diseases.

关 键 词：层状液晶 二甲双胍 放射性皮炎 经皮递送 

分 类 号：R943[医药卫生—药剂学] R965[医药卫生—药学]