Zein Microneedles for Localized Delivery of Chemotherapeutic Agents to Treat Breast Cancer: Drug Loading, Release Behavior, and Skin Permeation Studies
Zein Microneedles for Localized Delivery of Chemotherapeutic Agents to Treat Breast Cancer: Drug Loading, Release Behavior, and Skin Permeation Studies
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DOI：
10.1208/s12249-018-1004-5
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发表时间：
2018-05-01
影响因子：
3.3
通讯作者：
Venuganti, Venkata Vamsi Krishna
中科院分区：
文献类型：
--
作者：
Bhatnagar, Shubhmita;Kumari, Pooja;Venuganti, Venkata Vamsi Krishna
局部给药化疗药物治疗乳腺癌可以限制其不良反应。本研究的目的是调查的物理化学性质的化疗药物在其负载，释放行为，并使用微针皮肤渗透的影响。玉米醇溶蛋白微针使用微模塑技术制造，在1-cm（2）面积中含有36个微针。这些微针装载有两种抗乳腺癌药物，他莫昔芬和吉西他滨，具有不同的水溶性。优化玉米蛋白微针中化疗剂的包埋或表面涂覆以实现更大的装载效率。使用包埋方法，他莫昔芬和吉西他滨的最大载量分别为607 +/- 21和1459 +/- 74 μ g。在离体猪皮中的皮肤渗透研究表明，微针上的涂层方法导致他莫昔芬更大的皮肤沉积;而戳和贴片方法将为吉西他滨提供更大的皮肤渗透。总之，可以得出结论，必须研究不同的装载策略和皮肤渗透方法，以使用聚合物微针递送小分子。
Localized delivery of chemotherapeutic agents to treat breast cancer could limit their adverse drug reactions. The aim of this study was to investigate the influence of physico-chemical properties of chemotherapeutic agents in their loading, release behavior, and skin permeation using microneedles. Zein microneedles were fabricated using the micromolding technique containing 36 microneedles in a 1-cm(2) area. These microneedles were loaded with two anti-breast cancer drugs, tamoxifen and gemcitabine, having different water solubilities. Entrapment or surface coating of chemotherapeutic agents in zein microneedles was optimized to achieve greater loading efficiency. The greatest loading achieved was 607 +/- 21 and 1459 +/- 74 mu g for tamoxifen and gemcitabine using the entrapment approach, respectively. Skin permeation studies in excised porcine skin showed that the coating on microneedles approach results in greater skin deposition for tamoxifen; while the poke-and-patch approach would provide greater skin permeation for gemcitabine. Taken together, it can be concluded that different loading strategies and skin penetration approaches have to be studied for delivery of small molecules using polymeric microneedles.