eprintid: 16053
rev_number: 2
eprint_status: archive
userid: 1
dir: disk0/00/01/60/53
datestamp: 2023-12-19 03:22:37
lastmod: 2023-12-19 03:22:37
status_changed: 2023-12-19 03:05:33
type: article
metadata_visibility: show
creators_name: Md Moshikur, R.
creators_name: Shimul, I.M.
creators_name: Uddin, S.
creators_name: Wakabayashi, R.
creators_name: Moniruzzaman, M.
creators_name: Goto, M.
title: Transformation of Hydrophilic Drug into Oil-Miscible Ionic Liquids for Transdermal Drug Delivery
ispublished: pub
keywords: Biocompatibility; Controlled drug delivery; Fatty acids; Hydrophilicity; Mammals; Organic solvents; Pharmacokinetics; Targeted drug delivery, Biocompatible; Hydrophilic drugs; In-vitro; In-vivo; Laurate; Permeation enhancers; Plasma concentration; Skin permeation; Synthesised; Transdermal delivery, Ionic liquids, drug carrier; ionic liquid; lauric acid; linoleic acid; oleic acid; solvent; stearic acid, animal; chemistry; cutaneous drug administration; drug delivery system; mouse; permeability; procedures; skin; skin absorption, Administration, Cutaneous; Animals; Drug Carriers; Drug Delivery Systems; Ionic Liquids; Laurates; Linoleic Acid; Mice; Oleic Acid; Permeability; Skin; Skin Absorption; Solvents; Stearates
note: cited By 6
abstract: The transdermal delivery of hydrophilic drugs remains challenging owing to their poor ability to permeate the skin; formulation with oil media is difficult without adding chemical permeation enhancers or co-solvents. Herein, we synthesized 12 oil-miscible ionic liquid (IL) drugs comprising lidocaine-, imipramine-, and levamisole (Lev)-hydrochloride with fatty acid permeation enhancers, i.e., laurate, oleate, linoleate, and stearate as counterions. A set of in vitro and in vivo studies was performed to investigate the potency and deliverability of the transdermal drug formulations. All of the synthesized compounds were freely miscible with pharmaceutically acceptable solvents/agents (i.e., ethanol, N-methyl pyrrolidone, Tween 20, and isopropyl myristate (IPM)). In vitro permeation studies revealed that the oleate-based Lev formulation had 2.6-fold higher skin permeation capability than the Lev salts and also superior ability compared with the laurate-, linoleate-, and stearate-containing samples. Upon in vivo transdermal administration to mice, the peak plasma concentration, elimination half-life, and area under the plasma concentration curve values of Lev-IL were 4.6-, 2.9-, and 5.4-fold higher, respectively, than those of the Lev salt. Furthermore, in vitro skin irritation and in vivo histological studies have demonstrated that Lev-IL has excellent biocompatibility compared with a conventional ionic liquid-based carrier. The results indicate that oil-miscible IL-based drugs provide a simple and scalable strategy for the design of effective transdermal drug delivery systems. © 2022 American Chemical Society.
date: 2022
publisher: American Chemical Society
official_url: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85144506615&doi=10.1021%2facsami.2c15636&partnerID=40&md5=57d340b7a7c3873d70a546a596a84c5b
id_number: 10.1021/acsami.2c15636
full_text_status: none
publication: ACS Applied Materials and Interfaces
volume: 14
number: 50
pagerange: 55332-55341
refereed: TRUE
issn: 19448244
citation:   Md Moshikur, R. and Shimul, I.M. and Uddin, S. and Wakabayashi, R. and Moniruzzaman, M. and Goto, M.  (2022) Transformation of Hydrophilic Drug into Oil-Miscible Ionic Liquids for Transdermal Drug Delivery.  ACS Applied Materials and Interfaces, 14 (50).  pp. 55332-55341.  ISSN 19448244