Aims: Biodegradable polymeric microneedles containing atorvastatin calcium were developed in order to improve the percutaneous absorption of the drug, useful for the treatment of hypercholesterolemia.

Background: 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.

Objective: 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.

Methods: 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.

Results: 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.

Conclusion: 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.

目的：开发了含有阿托伐他汀钙的可生物降解的聚合物微针，以改善药物的经皮吸收，可用于治疗高胆固醇血症。

背景：使用物理增强剂（如微针）在增加药物通过皮肤的递送方面已显示出良好的效果，使用微针对透皮给药具有非常重要的优势，例如，它们无痛，易于使用且安全，它们他们还提供了增加药物活性，剂量和减少不良反应的时间间隔的便利，可以立即去除皮肤系统。

目的：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），生物粘附力，润湿后生物粘附力，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，以证明其用途微针阿托伐他汀能够穿过皮肤。

方法：采用在模具中溶液浇铸的技术，以聚甲基乙烯基醚-马来酸为生物可降解聚合物制备微针。固化后，通过差示扫描量热法（DSC），扫描电子显微镜（SEM），生物粘附力，润湿后生物粘附力，断裂强度，药物释放测试和体外经皮吸收研究对这些微针进行表征。

结果：总的来说，就最佳配方而言，DSC的性能令人满意，且药物与赋形剂之间没有相互作用； SEM显示微针呈圆锥形，生物粘附力为1570 gf，润湿后生物粘附力为1503.4 gf，断裂强度为1566.7gf足以破坏角质层，良好的药物释放和33.4μg/ cm2 * h的通量，tLag为15.14 h，用于体外经皮吸收。

结论：结果表明，可能产生微针以增加阿托伐他汀钙经皮的经皮吸收，并有望替代口服途径治疗血脂异常。