Unidad de Investigacion Multidisciplinaria. Laboratorio 12: Sistemas transdermicos, Facultad de Estudios Superiores Cuautitlan-Universidad Nacional Autonoma de Mexico (FESC-UNAM), Carretera Cuautitlan Teoloyucan km 2.5, San Sebastian Xhala C.P. 54714, Cuautitlan Izcalli, Mexico.
College of Pharmacy, The University of Texas at Austin, 2409 West University Avenue, PHR 4.214, Austin, Texas 78712, United States.
Curr Pharm Biotechnol. 2020;21(9):852-861. doi: 10.2174/1389201021666200217103302.
Biodegradable polymeric microneedles containing atorvastatin calcium were developed in order to improve the percutaneous absorption of the drug, useful for the treatment of hypercholesterolemia.
The use of physical enhancers like microneedles have shown good results to increase the delivery of drugs through the skin, the use of microneedles has very important advantages for transdermal drug delivery, for example, they are painless, easy to use and safe, they increase time interval of drug activity, dose, and reductions in adverse reactions, they also offer, the facility to remove the system instantly of the skin.
Develop polymer microneedles loaded with a calcium atorvastatin and evaluate them by Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), bioadhesion, postwetting- bioadhesion, breaking strength, drug release test and in vitro percutaneous absorption studies to demonstrate the use of microneedles atorvastatin is able to cross the skin.
The microneedles were made with poly (methyl vinyl ether-alt-maleic acid) as biodegradable polymer using the technique of casting in solution in a mold. After solidification these microneedles were characterized by Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), bioadhesion, post-wetting-bioadhesion, breaking strength, drug release test and in vitro percutaneous absorption studies.
In general, the performances were satisfactory for optimal formulation in terms of DSC with no interactions between drug and excipients, SEM shows microneedles with a conical shape, bioadhesion of 1570 g.f, post wetting-bioadhesion of 1503.4 g.f, breaking strength of 1566.7g.f that is sufficient to disrupt Stratum corneum, good drug release and a flux of 33.4 μg/cm2*h with a tLag of 15.14 h for the in vitro percutaneous absorption.
The results indicate that it is possible to generate microneedles to increase the percutaneous absorption of calcium atorvastatin transdermally, with the potential to be used as an alternative to the oral route for the treatment of dyslipidemias.
为了提高药物的经皮吸收，开发了载有阿托伐他汀钙的可生物降解聚合物微针。
使用物理增强剂（如微针）已显示出可显著增加药物经皮传递的效果。微针在经皮药物传递方面具有非常重要的优势，例如无痛、易于使用且安全，它们增加了药物活性的时间间隔、剂量和减少了不良反应，还提供了即时从皮肤去除系统的便利。
开发载有阿托伐他汀钙的聚合物微针，并通过差示扫描量热法（DSC）、扫描电子显微镜（SEM）、生物黏附性、湿后-生物黏附性、断裂强度、药物释放试验和体外经皮吸收研究对其进行评估，以证明载有阿托伐他汀的微针能够穿透皮肤。
使用聚（甲基乙烯基醚-马来酸酐）作为可生物降解聚合物，通过在模具中溶液浇铸技术制备微针。固化后，通过差示扫描量热法（DSC）、扫描电子显微镜（SEM）、生物黏附性、湿后-生物黏附性、断裂强度、药物释放试验和体外经皮吸收研究对微针进行了表征。
一般来说，从 DSC 角度来看，最优配方的性能令人满意，药物与赋形剂之间没有相互作用；SEM 显示微针呈锥形；生物黏附力为 1570 g.f；湿后-生物黏附力为 1503.4 g.f；断裂强度为 1566.7 g.f，足以破坏角质层；药物释放良好，体外经皮吸收的通量为 33.4 μg/cm2*h，tLag 为 15.14 h。
结果表明，有可能生成微针以增加阿托伐他汀钙经皮吸收，有可能替代口服途径用于治疗血脂异常。
