Innovative polymeric system (IPS) for solvent-free lipophilic drug transdermal delivery via dissolving microneedles
Innovative polymeric system (IPS) for solvent-free lipophilic drug transdermal delivery via dissolving microneedles
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DOI：
10.1016/j.jconrel.2015.12.038
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发表时间：
2016-02-10
影响因子：
10.8
通讯作者：
Jung, Hyungil
中科院分区：
文献类型：
--
作者：
Dangol, Manita;Yang, Huisuk;Jung, Hyungil
亲脂性药物是药物开发过程中的潜在候选药物。然而，由于需要有害的有机溶剂来溶解它们，这些药物通常无法进入制药市场，并且在这样做时突出了无溶剂系统的重要性。尽管透皮给药系统（TDDS）被认为是有前景的安全给药途径，但涉及无溶剂或粉末形式的亲脂性药物的系统尚未被描述。在这里，我们报告，为第一次，一种新的方法，每种亲脂性药物的粉末形式的基础上，创新的聚合物系统（IPS）的交付。由于药物与生物可降解聚合物之间的内部化学键导致的粉末形式的亲脂性药物的相变和纳米尺寸的胶体结构的形成允许溶解微针（DMN）的制造以产生强大的TDDS。我们表明，与基于溶剂的系统相比，基于IPS的DMN与粉末辣椒素增强了DBA/1小鼠模型中治疗风湿性关节炎的治疗效果，表明这种新的无溶剂平台用于亲脂性药物递送的有希望的潜力。(C)© 2016 Elsevier B. V.版权所有。
Lipophilic drugs are potential drug candidates during drug development. However, due to the need for hazardous organic solvents for their solubilization, these drugs often fail to reach the pharmaceutical market, and in doing so highlight the importance of solvent free systems. Although transdermal drug delivery systems (TDDSs) are considered prospective safe drug delivery routes, a system involving lipophilic drugs in solvent free or powder form has not yet been described. Here, we report, for the first time, a novel approach for the delivery of every kind of lipophilic drug in powder form based on an innovative polymeric system (IPS). The phase transition of powder form of lipophilic drugs due to interior chemical bonds between drugs and biodegradable polymers and formation of nano-sized colloidal structures allowed the fabrication of dissolving microneedles (DMNs) to generate a powerful TDDS. We showed that IPS based DMN with powder capsaicin enhances the therapeutic effect for treatment of the rheumatic arthritis in a DBA/1 mouse model compared to a solvent-based system, indicating the promising potential of this new solvent-free platform for lipophilic drug delivery. (C) 2016 Elsevier B.V. All rights reserved.