Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India.
Skin Pharmacol Physiol. 2013;26(3):127-38. doi: 10.1159/000348469. Epub 2013 Mar 21.
The overall aim of the present work was to elucidate the effects of iontophoresis on assisting permeation/deposition of peptide dendrimers across/within human skin.
A series of peptide dendrimers containing arginine and histidine as terminal acids were synthesized and characterized. These dendrimers were subjected to passive and iontophoretic permeation studies across human epidermis.
The synthesized peptide dendrimers were found to be stable in epidermal, dermal and skin extracts up to 6 h. Passive diffusion studies revealed that none of the synthesized peptide dendrimers permeated human epidermis up to 6 h, although minute concentrations of low molecular weight dendrimers were detected in receptor medium at the end of 24 h. Application of iontophoresis significantly increased the permeation of all the tested peptide dendrimers across human skin in a molecular weight-dependent manner compared to simple passive diffusion. Electromigration was found to be the dominant mechanism behind the iontophoretic permeation of peptide dendrimers across human skin.
The present study demonstrates that iontophoresis is an effective technique in enhancing the transdermal permeation of peptide dendrimers. MESSAGE OF THE PAPER: This study foresees the possibility of applying peptide dendrimers in iontophoretic delivery of drugs and macromolecules across/within the skin.
本研究的总体目的是阐明离子导入对辅助肽树突状聚合物穿过/进入人体皮肤的渗透/沉积的影响。
合成并表征了一系列含有精氨酸和组氨酸作为末端酸的肽树突状聚合物。这些树突状聚合物进行了被动和离子电渗递药研究，以研究其穿过人体表皮的情况。
研究发现，所合成的肽树突状聚合物在表皮、真皮和皮肤提取物中在 6 小时内是稳定的。被动扩散研究表明，在 24 小时结束时，受体介质中仅检测到低分子量树突状聚合物的微量浓度，但没有一种所合成的肽树突状聚合物在 6 小时内穿过人体表皮。与简单的被动扩散相比，离子导入显著增加了所有测试的肽树突状聚合物穿过人体皮肤的渗透，这是一种分子量依赖性的方式。电迁移被发现是肽树突状聚合物穿过人体皮肤进行离子电渗递药的主要机制。
本研究表明，离子导入是增强肽树突状聚合物经皮渗透的有效技术。
本研究预见了在离子电渗递药技术中应用肽树突状聚合物将药物和大分子递送至皮肤内外的可能性。
