Bansal Kuldeep Kumar, Özliseli Ezgi, Saraogi Gaurav Kumar, Rosenholm Jessica M
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.
Pharmaceutics. 2020 Aug 2;12(8):726. doi: 10.3390/pharmaceutics12080726.
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.
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。