Biocompatible Ionic Liquid Enhances Transdermal Antigen Peptide Delivery and Preventive Vaccination Effect.,Molecular Pharmaceutics

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Biocompatible Ionic Liquid Enhances Transdermal Antigen Peptide Delivery and Preventive Vaccination Effect.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-09-09 , DOI: 10.1021/acs.molpharmaceut.0c00598
Yoshiro Tahara ₁ , Kaho Morita ₁ , Rie Wakabayashi _{1,

2} , Noriho Kamiya _{1,

2,

3} , Masahiro Goto _{1,

2,

3}

Affiliation

Ionic liquids (ILs) attract significant attention as novel solvents for drug delivery systems because of their ability to solubilize poorly soluble drugs and tune the physiological properties of active pharmaceutical ingredients. For the next generation of IL-based drug delivery systems, biocompatibility is a high priority. In the current study, choline–fatty acids ([Cho][FA]) were used as a biocompatible IL to mediate the dissolution of a water-soluble antigen peptide in an oil-based skin penetration enhancer. Among the candidate fatty acids (C8, C10, C12, C14, C16, C18:0, and C18:1), C18:1 was selected because of its low cytotoxicity and mediation of skin permeability for an antigen peptide. Using IL[Cho][C18:1] and an oil-based penetration enhancer, the flux of transdermal delivery of the peptide increased 28-fold compared with delivery using an aqueous vehicle. Furthermore, the IL-mediated transcutaneous vaccination succeeded in suppressing tumor growth in vivo compared to injection. The skin irritation produced by this formulation was tested using an in vitro 3D constructed skin tissue model and an in vivo histological study, which concluded that the formulation did not cause skin irritation. The results suggest that biocompatible IL-mediated dissolution in an oil-based skin penetration enhancer is a promising strategy for transdermal drug delivery.

中文翻译：

生物相容性离子液体增强透皮抗原肽递送和预防接种效果。

离子液体 (IL) 作为药物递送系统的新型溶剂引起了极大的关注，因为它们能够溶解难溶性药物并调节活性药物成分的生理特性。对于下一代基于 IL 的药物递送系统，生物相容性是重中之重。在目前的研究中，胆碱-脂肪酸 ([Cho][FA]) 被用作生物相容性 IL，以介导水溶性抗原肽在油基皮肤渗透促进剂中的溶解。在候选脂肪酸（C8、C10、C12、C14、C16、C18:0 和 C18:1）中，选择 C18:1 是因为其低细胞毒性和介导抗原肽的皮肤渗透性。使用 IL[Cho][C18:1] 和油基渗透增强剂，与使用水性载体的递送相比，肽的透皮递送通量增加了 28 倍。此外，与注射相比，IL 介导的经皮疫苗接种成功地抑制了体内肿瘤生长。使用体外 3D 构建的皮肤组织模型和体内组织学研究测试了该制剂产生的皮肤刺激，得出的结论是该制剂不会引起皮肤刺激。结果表明，生物相容性 IL 介导的油基皮肤渗透促进剂中的溶解是一种有前途的透皮药物递送策略。使用体外 3D 构建的皮肤组织模型和体内组织学研究测试了该制剂产生的皮肤刺激，得出的结论是该制剂不会引起皮肤刺激。结果表明，生物相容性 IL 介导的油基皮肤渗透促进剂中的溶解是一种有前途的透皮药物递送策略。使用体外 3D 构建的皮肤组织模型和体内组织学研究测试了该制剂产生的皮肤刺激，得出的结论是该制剂不会引起皮肤刺激。结果表明，生物相容性 IL 介导的油基皮肤渗透促进剂中的溶解是一种有前途的透皮药物递送策略。

更新日期：2020-10-05

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