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新型可持续聚(δ-癸内酯)基胶束细胞内递送潜力的评估

Assessment of Intracellular Delivery Potential of Novel Sustainable Poly(δ-decalactone)-Based Micelles.

作者信息

Bansal Kuldeep Kumar, Özliseli Ezgi, Saraogi Gaurav Kumar, Rosenholm Jessica M

机构信息

Pharmaceutical Sciences Laboratory, Faculty of Science and Engineering, Åbo Akademi University, 20520 Turku, Finland.

School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, UK.

出版信息

Pharmaceutics. 2020 Aug 2;12(8):726. doi: 10.3390/pharmaceutics12080726.

Abstract

Biodegradable polymers from renewable resources have attracted much attention in recent years within the biomedical field. Lately, poly(δ-decalactone) based copolymer micelles have emerged as a potential drug delivery carrier material as a sustainable alternative to fossil-based polymers. However, their intracellular drug delivery potential is not yet investigated and therefore, in this work, we report on the synthesis and cellular uptake efficiency of poly(δ-decalactone) based micelles with or without a targeting ligand. Folic acid was chosen as a model targeting ligand and Rhodamine B as a fluorescent tracer to demonstrate the straightforward functionalisation aspect of copolymers. The synthesis of block copolymers was accomplished by a combination of facile ring-opening polymerisation and click chemistry to retain the structure uniformity. The presence of folic acid on the surface of micelles with diameter ~150 nm upsurge the uptake efficiency by 1.6 fold on folate receptor overexpressing MDA-MB-231 cells indicating the attainment of targeting using ligand functionality. The drug delivery capability of these carriers was ascertained by using docetaxel as a model drug, whereby the in vitro cytotoxicity of the drug was significantly increased after incorporation in micelles 48 h post incubation. We have also investigated the possible endocytosis route of non-targeted micelles and found that caveolae-mediated endocytosis was the preferred route of uptake. This work strengthens the prospect of using novel bio-based poly(δ-decalactone) micelles as efficient multifunctional drug delivery nanocarriers towards medical applications.

摘要

近年来,可再生资源制成的可生物降解聚合物在生物医学领域备受关注。最近,基于聚(δ-癸内酯)的共聚物胶束已成为一种潜在的药物递送载体材料,可作为化石基聚合物的可持续替代品。然而,它们的细胞内药物递送潜力尚未得到研究,因此,在这项工作中,我们报告了带有或不带有靶向配体的聚(δ-癸内酯)基胶束的合成及其细胞摄取效率。选择叶酸作为模型靶向配体,罗丹明B作为荧光示踪剂,以展示共聚物简单的功能化方面。通过简便的开环聚合和点击化学相结合来完成嵌段共聚物的合成,以保持结构均匀性。在直径约150 nm的胶束表面存在叶酸,使叶酸受体过表达的MDA-MB-231细胞的摄取效率提高了1.6倍,这表明利用配体功能实现了靶向。通过使用多西他赛作为模型药物来确定这些载体的药物递送能力,在孵育48小时后将药物掺入胶束中后,药物的体外细胞毒性显著增加。我们还研究了非靶向胶束可能的内吞途径,发现小窝介导的内吞是首选的摄取途径。这项工作增强了使用新型生物基聚(δ-癸内酯)胶束作为高效多功能药物递送纳米载体用于医学应用的前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/777a/7465297/5336d74b740c/pharmaceutics-12-00726-sch001.jpg

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