Abstract

Ring opening copolymerization is the most frequently applied reaction for the synthesis of polycaprolactone–polyethylene glycol–polycaprolactone (PCL–PEG–PCL). In this reaction, a number of expensive and toxic organic solvents are being used for the purpose of purification and extraction of the prepared copolymer. Exposure to these organic solvents can cause serious issues to the human health and also impart serious environmental pollution. In the current work, a new, economical and organic solvent free approach was used for the synthesis of triblock copolymer. The results of the current studies confirmed the successful formation of triblock copolymer as revealed by Fourier transform infrared spectra, ¹³carbon nuclear magnetic resonance (¹³C-NMR) and proton nuclear magnetic resonance (¹H-NMR). Gel permeation chromatography analysis ensured the homo-distribution of the prepared copolymer. The prepared copolymer was further evaluated as a carrier for the drug loading. Nanomicelles were successfully prepared by the nanoprecipitation technique and exhibited an average size distribution of 42.50 nm and an encapsulation efficiency of 90%. The prepared nanomicelles also exhibited safety at the concentration of 50 µg/ml and a long-term storage stability. All these studies suggested the success of the new simplest and economical method for the synthesis of PCL–PEG–PCL and its subsequent applications as a carrier for fabrication and efficient delivery of hydrophobic drug molecules.

Graphic Abstract

摘要

开环共聚是合成聚己内酯-聚乙二醇-聚己内酯（PCL-PEG-PCL）最常用的反应。在该反应中，为了纯化和提取所制备的共聚物，使用了许多昂贵且有毒的有机溶剂。暴露于这些有机溶剂会严重危害人体健康，并给环境造成严重污染。在当前的工作中，一种新的，经济的和无有机溶剂的方法被用于合成三嵌段共聚物。当前研究的结果证实了三嵌段共聚物的成功形成，如傅立叶变换红外光谱，¹³碳核磁共振（¹³核磁共振和质子核磁共振（¹ H-NMR）。凝胶渗透色谱分析确保了所制备共聚物的均匀分布。进一步评估了所制备的共聚物作为载药的载体。通过纳米沉淀技术成功制备了Nanomicelles，其平均尺寸分​​布为42.50 nm，包封效率为90％。所制备的纳米胶束在浓度为50 µg / ml时也显示出安全性，并具有长期存储稳定性。所有这些研究表明，合成PCL–PEG–PCL的最简单，最经济的新方法取得了成功，并随后将其用作疏水性药物分子的制备和有效递送的载体。

图形摘要