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Article

Ionic Liquid-In-Oil Microemulsions Prepared with Biocompatible Choline Carboxylic Acids for Improving the Transdermal Delivery of a Sparingly Soluble Drug

1
Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan
2
Department of Applied Chemistry and Chemical Engineering, Noakhali Science and Technology University, Noakhali 3814, Bangladesh
3
Advanced Transdermal Drug Delivery System Center, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan
4
Division of Biotechnology, Center for Future Chemistry, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan
5
Chemical Engineering Department, Universiti Teknologi PETRONAS, Seri Iskandar 32610, Perak, Malaysia
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(4), 392; https://doi.org/10.3390/pharmaceutics12040392
Received: 31 March 2020 / Revised: 21 April 2020 / Accepted: 22 April 2020 / Published: 24 April 2020
The transdermal delivery of sparingly soluble drugs is challenging due to of the need for a drug carrier. In the past few decades, ionic liquid (IL)-in-oil microemulsions (IL/O MEs) have been developed as potential carriers. By focusing on biocompatibility, we report on an IL/O ME that is designed to enhance the solubility and transdermal delivery of the sparingly soluble drug, acyclovir. The prepared MEs were composed of a hydrophilic IL (choline formate, choline lactate, or choline propionate) as the non-aqueous polar phase and a surface-active IL (choline oleate) as the surfactant in combination with sorbitan laurate in a continuous oil phase. The selected ILs were all biologically active ions. Optimized pseudo ternary phase diagrams indicated the MEs formed thermodynamically stable, spherically shaped, and nano-sized (<100 nm) droplets. An in vitro drug permeation study, using pig skin, showed the significantly enhanced permeation of acyclovir using the ME. A Fourier transform infrared spectroscopy study showed a reduction of the skin barrier function with the ME. Finally, a skin irritation study showed a high cell survival rate (>90%) with the ME compared with Dulbecco’s phosphate-buffered saline, indicates the biocompatibility of the ME. Therefore, we conclude that IL/O ME may be a promising nano-carrier for the transdermal delivery of sparingly soluble drugs. View Full-Text
Keywords: biocompatible; ionic liquid; transdermal drug delivery system; microemulsion biocompatible; ionic liquid; transdermal drug delivery system; microemulsion
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MDPI and ACS Style

Islam, M.R.; Chowdhury, M.R.; Wakabayashi, R.; Kamiya, N.; Moniruzzaman, M.; Goto, M. Ionic Liquid-In-Oil Microemulsions Prepared with Biocompatible Choline Carboxylic Acids for Improving the Transdermal Delivery of a Sparingly Soluble Drug. Pharmaceutics 2020, 12, 392. https://doi.org/10.3390/pharmaceutics12040392

AMA Style

Islam MR, Chowdhury MR, Wakabayashi R, Kamiya N, Moniruzzaman M, Goto M. Ionic Liquid-In-Oil Microemulsions Prepared with Biocompatible Choline Carboxylic Acids for Improving the Transdermal Delivery of a Sparingly Soluble Drug. Pharmaceutics. 2020; 12(4):392. https://doi.org/10.3390/pharmaceutics12040392

Chicago/Turabian Style

Islam, Md. R., Md. R. Chowdhury, Rie Wakabayashi, Noriho Kamiya, Muhammad Moniruzzaman, and Masahiro Goto. 2020. "Ionic Liquid-In-Oil Microemulsions Prepared with Biocompatible Choline Carboxylic Acids for Improving the Transdermal Delivery of a Sparingly Soluble Drug" Pharmaceutics 12, no. 4: 392. https://doi.org/10.3390/pharmaceutics12040392

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