1. Choline and amino acid based biocompatible ionic liquid mediated transdermal delivery of the sparingly soluble drug acyclovir.
- Author
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Islam MR, Chowdhury MR, Wakabayashi R, Tahara Y, Kamiya N, Moniruzzaman M, and Goto M
- Subjects
- Acyclovir chemistry, Acyclovir metabolism, Administration, Cutaneous, Amino Acids toxicity, Animals, Cell Line, Choline toxicity, Drug Compounding, Ethanol chemistry, Female, Humans, Ionic Liquids, Mice, Inbred BALB C, Myristates chemistry, Solubility, Solvents chemistry, Swine, Swine, Miniature, Acyclovir administration & dosage, Amino Acids chemistry, Choline chemistry, Drug Carriers, Skin metabolism, Skin Absorption
- Abstract
Transdermal delivery of drugs is more challenging for drugs that are insoluble or sparingly soluble in water and most organic solvents. To overcome this problem, ionic liquid (IL)-mediated ternary systems have been suggested as potential drug carriers. Here, we report potent ternary (IL-EtOH-IPM) systems consisting of biocompatible ILs, ethanol (EtOH), and isopropyl myristate (IPM) that can dissolve a significant amount of the sparingly soluble drug acyclovir (ACV). The ternary systems were optically transparent and thermodynamically stable with a wide range of IL pertinence. An in vitro drug permeation study showed that the ILs in the ternary systems dramatically enhanced ACV permeation into and across the skin. Fourier Transform Infrared spectroscopy of the stratum corneum (sc) after treatment with ternary systems showed that the skin barrier function was reduced by disturbance of the regularly ordered arrangement of corneocytes and modification of the surface properties of the sc during permeation. Histological analysis, and skin irritation studies using a reconstructed human epidermis model showed the safety profile of the ternary system, and there were no significant changes in the structures of the sc, epidermis, and dermis. Therefore, ternary systems containing biocompatible ILs are promising for transdermal delivery of insoluble or sparingly soluble drugs., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier B.V. All rights reserved.)
- Published
- 2020
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