Miniemulsion polymerization at low temperature: A strategy for one-pot encapsulation of hydrophobic anti-inflammatory drugs into polyester-containing nanoparticles.
Miniemulsion polymerization at low temperature: A strategy for one-pot encapsulation of hydrophobic anti-inflammatory drugs into polyester-containing nanoparticles.
复制标题
低温细乳液聚合：将疏水性抗炎药物一锅包封到含聚酯纳米颗粒中的策略。
DOI：
10.1016/j.jcis.2021.12.189
复制
发表时间：
2021
影响因子：
9.9
通讯作者：
U. Schubert
中科院分区：
文献类型：
--
作者：
Alicia De San Luis;Maximilian Kleinsteuber;Timo Schuett;S. Schubert;U. Schubert
假设传统的聚合物纳米颗粒作为药物递送系统的合成方法是基于使用大量的有机溶剂，因此需要几个步骤来获得水性分散体。鉴于对新的环境友好方法的需求，乳液聚合及其相关技术是以更清洁、可再现和更快的方式生产生物可降解纳米颗粒的单分散水性分散体的良好替代方案。聚乙烯低温细乳液聚合技术2-乙基-2-恶唑啉作为表面活性剂已被开发用于聚（甲基丙烯酸羟乙酯-乳酸）和聚（甲基丙烯酸羟乙酯-乳酸-共-乙醇酸）纳米颗粒。此外，抗炎药物BRP-187用于证明该技术在疏水药物包封中的潜力。研究了低聚物组成对细乳液和最终分散体稳定性、最终低聚物转化率、聚合物粒径和药物包封率的影响，得到了粒径在170 ~ 250 nm之间的单分散球形颗粒，药物包封率可达66%。与传统的合成技术相比，残留的有机溶剂被完全去除，因此，氧化还原引发的细乳液聚合的潜力，以获得稳定的药物负载的聚（甲基丙烯酸羟乙酯-乳酸）和聚（甲基丙烯酸羟乙酯-乳酸-共-乙醇酸）纳米粒子在一个有效的和快速的方式显示。
HypothesisConventional synthesis methods of polymeric nanoparticles as drug delivery systems are based on the use of large amounts of organic solvents, hence requiring several steps for the obtaining of waterborne dispersions. In view of the need for new environmentally friendly methods, emulsion polymerization and their related techniques are a good alternative for the production of monodispersed waterborne dispersions of biodegradable nanoparticles in a cleaner, reproducible and faster manner.ExperimentsHerein, the miniemulsion polymerization technique at low temperature using poly(2-ethyl-2-oxazoline) as surfactant has been developed for poly(hydroxyethyl methacrylate-lactic acid) and poly(hydroxyethyl methacrylate-lactic-co-glycolic acid) nanoparticles. Additionally, the anti-inflammatory drug BRP-187 was used to proof the potential of this technique in the encapsulation of hydrophobic drugs. The effect of the oligomer composition on the miniemulsion and the final dispersion stability, the final oligomer conversion, the polymer particle size and the drug encapsulation efficiency has been studied.FindingsMonodisperse spherical particles ranging between 170 and 250 nm in diameter in long term non-toxic stable waterborne dispersions were obtained with drug encapsulation efficiencies up to 66%. In contrast with conventional synthesis techniques, residual organic solvents are completely removed and, thus, the potential of redox initiated miniemulsion polymerization to obtain stable drug loaded poly(hydroxyethyl methacrylate-lactic acid) and poly(hydroxyethyl methacrylate-lactic-co-glycolic acid) nanoparticles in an efficient and fast manner is shown.