Curcumin is a natural substance extracted from Curcuma longa Linn with beneficial pharmaceutical properties such as anticancer activity against several cellular lines. However, it presents poor bioavailability due to its low solubility in aqueous media and chemical instability. In this research, curcumin was encapsulated in polymer micelles obtained by the self-assembly of a biodegradable poly (ethylene glycol)-block-poly(ɛ-caprolactone) copolymer conjugated with cholesterol or oleic acid. A hydroxyl-terminated poly (ethylene glycol)-block-poly(ɛ-caprolactone) was reacted with cholesteryl chloroformate or oleyl chloride to obtain conjugated copolymers. The resulting polymeric materials were characterised through proton nuclear magnetic resonance, gel permeation chromatography and differential scanning calorimetry, and their critical aggregation concentration was measured through fluorescence spectroscopy. Poly (ethylene glycol)-block-poly(ɛ-caprolactone) conjugated with cholesterol and oleic acid posed an improved capacity of encapsulating curcumin, resulting in the loading capacities of 8.8% and 15.2%, respectively. Cell viability studies confirmed that curcumin loaded in polymer micelles maintained its anticancer activity against MCF-7 human breast cancer cells but presented low cytotoxicity against mouse fibroblasts. Hence, these formulations have good potential for applications in drug delivery systems for breast cancer treatment.

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通过与亲脂性生物分子的结合提高基于 PEG-b-PCL 的姜黄素纳米载体的性能

姜黄素是从 Curcuma longa Linn 中提取的天然物质，具有有益的药物特性，例如对多种细胞系的抗癌活性。然而，由于其在水性介质中的低溶解度和化学不稳定性，其生物利​​用度较差。在这项研究中，姜黄素被封装在聚合物胶束中，该胶束是通过与胆固醇或油酸共轭的可生物降解的聚（乙二醇）-嵌段-聚（ɛ-己内酯）共聚物的自组装而获得的。羟基封端的聚（乙二醇）-嵌段-聚（ɛ-己内酯）与氯甲酸胆固醇或油酰氯反应得到共轭共聚物。所得聚合物材料通过质子核磁共振、凝胶渗透色谱和差示扫描量热法表征，并通过荧光光谱测量它们的临界聚集浓度。与胆固醇和油酸共轭的聚（乙二醇）-嵌段-聚（ɛ-己内酯）提高了包封姜黄素的能力，导致负载能力分别为 8.8% 和 15.2%。细胞活力研究证实，加载在聚合物胶束中的姜黄素保持其对 MCF-7 人乳腺癌细胞的抗癌活性，但对小鼠成纤维细胞的细胞毒性较低。因此，这些制剂在用于乳腺癌治疗的药物递送系统中具有良好的应用潜力。导致负载能力分别为 8.8% 和 15.2%。细胞活力研究证实，加载在聚合物胶束中的姜黄素保持其对 MCF-7 人乳腺癌细胞的抗癌活性，但对小鼠成纤维细胞的细胞毒性较低。因此，这些制剂在用于乳腺癌治疗的药物递送系统中具有良好的应用潜力。导致负载能力分别为 8.8% 和 15.2%。细胞活力研究证实，加载在聚合物胶束中的姜黄素保持其对 MCF-7 人乳腺癌细胞的抗癌活性，但对小鼠成纤维细胞的细胞毒性较低。因此，这些制剂在用于乳腺癌治疗的药物递送系统中具有良好的应用潜力。