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用于局部和透皮递送低渗透性治疗剂的新型反向电渗析驱动离子电渗系统。

Novel reverse electrodialysis-driven iontophoretic system for topical and transdermal delivery of poorly permeable therapeutic agents.

作者信息

Kim Ki-Taek, Lee Joon, Kim Min-Hwan, Park Ju-Hwan, Lee Jae-Young, Song Joo-Hyun, Jung Minwoong, Jang Myoung-Hoon, Cho Hyun-Jong, Yoon In-Soo, Kim Dae-Duk

机构信息

a College of Pharmacy and Research Institute of Pharmaceutical Sciences , Seoul National University , Gwanak-gu, Seoul , Republic of Korea.

b Biosensor Laboratories Inc , Seoul National University , Gwanak-gu, Seoul , Republic of Korea.

出版信息

Drug Deliv. 2017 Nov;24(1):1204-1215. doi: 10.1080/10717544.2017.1367975.

DOI:10.1080/10717544.2017.1367975
PMID:28844174
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8241169/
Abstract

Topical and transdermal drug delivery has great potential in non-invasive and non-oral administration of poorly bioavailable therapeutic agents. However, due to the barrier function of the stratum corneum, the drugs that can be clinically feasible candidates for topical and transdermal delivery have been limited to small-sized lipophilic molecules. Previously, we fabricated a novel iontophoretic system using reverse electrodialysis (RED) technology (RED system). However, no study has demonstrated its utility in topical and/or transdermal delivery of poorly permeable therapeutic agents. In this study, we report the topical delivery of fluorescein isothiocyanate (FITC)-hyaluronic acid (FITC-HA) and vitamin C and the transdermal delivery of lopinavir using our newly developed RED system in the in vitro hairless mouse skin and in vivo Sprague-Dawley rat models. The RED system significantly enhanced the efficiency of topical HA and vitamin C and transdermal lopinavir delivery. Moreover, the efficiency and safety of transdermal delivery using the RED system were comparable with those of a commercial ketoprofen patch formulation. Thus, the RED system can be a potential topical and transdermal delivery system for various poorly bioavailable pharmaceuticals including HA, vitamin C, and lopinavir.

摘要

局部和透皮给药在生物利用度低的治疗药物的非侵入性和非口服给药方面具有巨大潜力。然而，由于角质层的屏障功能，可用于局部和透皮给药的临床上可行的候选药物仅限于小分子亲脂性分子。此前，我们利用反向电渗析（RED）技术制造了一种新型离子电渗系统（RED系统）。然而，尚无研究证明其在低渗透性治疗药物的局部和/或透皮给药中的效用。在本研究中，我们报告了在体外无毛小鼠皮肤和体内Sprague-Dawley大鼠模型中，使用我们新开发的RED系统进行异硫氰酸荧光素（FITC）-透明质酸（FITC-HA）和维生素C的局部给药以及洛匹那韦的透皮给药。RED系统显著提高了局部HA和维生素C以及透皮洛匹那韦给药的效率。此外，使用RED系统进行透皮给药的效率和安全性与市售酮洛芬贴剂相当。因此，RED系统可能成为包括HA、维生素C和洛匹那韦在内的各种生物利用度低的药物的潜在局部和透皮给药系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/2599e9bbc82a/IDRD_A_1367975_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/31da84fa5307/IDRD_A_1367975_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/446fd42c5faa/IDRD_A_1367975_F0002a_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/c67a16659bf7/IDRD_A_1367975_F0002b_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/9f97cbfd6a96/IDRD_A_1367975_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/84346c624c11/IDRD_A_1367975_F0004_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/fabefc9a5901/IDRD_A_1367975_F0005_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/2599e9bbc82a/IDRD_A_1367975_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/31da84fa5307/IDRD_A_1367975_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/446fd42c5faa/IDRD_A_1367975_F0002a_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/c67a16659bf7/IDRD_A_1367975_F0002b_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/9f97cbfd6a96/IDRD_A_1367975_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/84346c624c11/IDRD_A_1367975_F0004_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/fabefc9a5901/IDRD_A_1367975_F0005_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c15e/8241169/2599e9bbc82a/IDRD_A_1367975_F0006_C.jpg

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