Suppr超能文献

基于生物相容离子液体的胶束用于增强紫杉醇的透皮递送

Biocompatible Ionic Liquid-Mediated Micelles for Enhanced Transdermal Delivery of Paclitaxel.

机构信息

Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan.

Department of Chemistry, Jashore University of Science and Technology, Jashore 7408, Bangladesh.

出版信息

ACS Appl Mater Interfaces. 2021 May 5;13(17):19745-19755. doi: 10.1021/acsami.1c03111. Epub 2021 Apr 23.

Abstract

Chemotherapeutic cytotoxic agents such as paclitaxel (PTX) are considered essential for the treatment of various cancers. However, PTX injection is associated with severe systemic side effects and high rates of patient noncompliance. Micelle formulations (MFs) are nano-drug delivery systems that offer a solution to these problems. Herein, we report an advantageous carrier for the transdermal delivery of PTX comprising a new MF that consists of two biocompatible surfactants: cholinium oleate ([Cho][Ole]), which is a surface-active ionic liquid (SAIL), and sorbitan monolaurate (Span-20). A solubility assessment confirmed that PTX was readily solubilized in the SAIL-based micelles via multipoint hydrogen bonding and cation-π and π-π interactions between PTX and SAIL[Cho][Ole]. Dynamic light scattering (DLS) and transmission electron microscopy revealed that in the presence of PTX, the MF formed spherical PTX-loaded micelles that were well-distributed in the range 8.7-25.3 nm. According to DLS, the sizes and size distributions of the micelle droplets did not change significantly over the entire storage period, attesting to their physical stability. transdermal assessments using a Franz diffusion cell revealed that the MF absorbed PTX 4 times more effectively than a Tween 80-based formulation and 6 times more effectively than an ethanol-based formulation. and skin irritation tests revealed that the new carrier had a negligible toxicity profile compared with a conventional ionic liquid-based carrier. Based on these findings, we believe that the SAIL[Cho][Ole]-based MF has potential as a biocompatible nanocarrier for the effective transdermal delivery of poorly soluble chemotherapeutics such as PTX.

摘要

化疗细胞毒性药物,如紫杉醇(PTX),被认为是治疗各种癌症的重要药物。然而,PTX 注射与严重的全身副作用和高患者不依从率有关。胶束制剂(MFs)是一种纳米药物递送系统,可解决这些问题。在此,我们报告了一种用于 PTX 经皮递药的有利载体,该载体由两种生物相容性表面活性剂组成的新 MF 组成:胆碱油酸酯([Cho][Ole]),它是一种具有表面活性的离子液体(SAIL),和山梨糖醇单月桂酸酯(Span-20)。溶解度评估证实,PTX 可通过多点氢键以及 PTX 和 SAIL[Cho][Ole]之间的阳离子-π 和 π-π 相互作用,轻易地溶解在基于 SAIL 的胶束中。动态光散射(DLS)和透射电子显微镜显示,在存在 PTX 的情况下,MF 形成了球形的载有 PTX 的胶束,这些胶束在 8.7-25.3nm 的范围内分布良好。根据 DLS,在整个储存期内,胶束液滴的大小和尺寸分布没有明显变化,证明了它们的物理稳定性。Franz 扩散池的经皮评估显示,MF 比基于吐温 80 的制剂更有效地吸收 4 倍的 PTX,比基于乙醇的制剂更有效地吸收 6 倍的 PTX。而且,皮肤刺激试验表明,与传统的基于离子液体的载体相比,新载体的毒性谱可以忽略不计。基于这些发现,我们认为基于 SAIL[Cho][Ole]的 MF 有潜力成为一种生物相容的纳米载体,可有效经皮递运疏水性化疗药物,如 PTX。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验