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Enhanced Transdermal Permeability via Constructing the Porous Structure of Poloxamer-Based Hydrogel

机译：通过构建基于泊洛沙姆的水凝胶的多孔结构增强透皮渗透性

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A major concern for transdermal drug delivery systems is the low bioavailability of targeted drugs primarily caused by the skin’s barrier function. The resistance to the carrier matrix for the diffusion and transport of drugs, however, is routinely ignored. This study reports a promising and attractive approach to reducing the resistance to drug transport in the carrier matrix, to enhance drug permeability and bioavailability via enhanced concentration-gradient of the driving force for transdermal purposes. This approach simply optimizes and reconstructs the porous channel structure of the carrier matrix, namely, poloxamer 407 (P407)-based hydrogel matrix blended with carboxymethyl cellulose sodium (CMCs). Addition of CMCs was found to distinctly improve the porous structure of the P407 matrix. The pore size approximated to normal distribution as CMCs were added and the fraction of pore number was increased by over tenfold. Transdermal studies showed that P407/CMCs saw a significant increase in drug permeability across the skin. This suggests that P407/CMC with improved porous structure exhibits a feasible and promising way for the development of transdermal therapy with high permeability and bioavailability, thereby avoiding or reducing use of any chemical enhancers.
机译：透皮给药系统的主要问题是靶向药物的生物利用度低，这主要是由皮肤的屏障功能引起的。但是，通常会忽略对药物扩散和运输的载体基质的抗性。这项研究报告了一种有希望和有吸引力的方法，可以降低对载体基质中药物运输的抵抗力，通过增加用于透皮目的的驱动力的浓度梯度来提高药物的渗透性和生物利用度。这种方法只是简单地优化和重建了载体基质的多孔通道结构，即与羧甲基纤维素钠（CMC）混合的基于泊洛沙姆407（P407）的水凝胶基质。发现添加CMC可明显改善P407基质的多孔结构。当添加CMC时，孔径接近于正态分布，并且孔数的分数增加了十倍以上。透皮研究表明，P407 / CMCs穿过皮肤的药物渗透性显着提高。这表明具有改善的多孔结构的P407 / CMC为开发具有高渗透性和生物利用度的透皮疗法展示了可行且有希望的方式，从而避免或减少了任何化学增强剂的使用。

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