| RRC ID |
58866
|
| 著者 |
Islam MR, Chowdhury MR, Wakabayashi R, Tahara Y, Kamiya N, Moniruzzaman M, Goto M.
|
| タイトル |
Choline and amino acid based biocompatible ionic liquid mediated transdermal delivery of the sparingly soluble drug acyclovir.
|
| ジャーナル |
Int J Pharm
|
| 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.
|
| 巻・号 |
582
|
| ページ |
119335
|
| 公開日 |
2020-5-30
|
| DOI |
10.1016/j.ijpharm.2020.119335
|
| PII |
S0378-5173(20)30319-7
|
| PMID |
32311469
|
| MeSH |
Acyclovir / administration & dosage*
Acyclovir / chemistry
Acyclovir / metabolism
Administration, Cutaneous
Amino Acids / chemistry*
Amino Acids / toxicity
Animals
Cell Line
Choline / chemistry*
Choline / toxicity
Drug Carriers*
Drug Compounding
Ethanol / chemistry
Female
Humans
Ionic Liquids
Mice, Inbred BALB C
Myristates / chemistry
Skin / metabolism*
Skin Absorption*
Solubility
Solvents / chemistry
Swine
Swine, Miniature
|
| IF |
4.845
|
| 引用数 |
1
|
| リソース情報 |
| ヒト・動物細胞 |
L929 |
