Design of Curcumin Loaded Carbon Nanodots Delivery System: Enhanced Bioavailability, Release Kinetics, and Anticancer Activity
Design of Curcumin Loaded Carbon Nanodots Delivery System: Enhanced Bioavailability, Release Kinetics, and Anticancer Activity
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DOI：
10.1021/acsabm.0c01144
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发表时间：
2020-12-21
影响因子：
4.7
通讯作者：
Wei, Jianjun
中科院分区：
文献类型：
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作者：
Arvapalli, Durga M.;Sheardy, Alex T.;Wei, Jianjun
尽管姜黄素具有潜在的健康益处，如抗氧化、抗癌、抗炎和抗菌特性，但其使用受到生物利用度差和水溶性低的限制。姜黄素的纳米配方由于其增加的生物利用度、溶解度、循环时间、靶向特异性、减少生物降解、更好的稳定性和改善的细胞摄取而获得了很多关注。由于碳纳米点具有良好的生物相容性、水溶性和光致发光特性，本研究旨在利用碳纳米点作为姜黄素的载药载体来提高姜黄素的生物利用度。两种CNDs （E-CNDs和U-CNDs）用于姜黄素的负载，并对其粒径、形态、负载能力（以吸附效率和负载能力衡量）、稳定性、光致发光特性、体外药物释放研究、细胞摄取和抗癌活性进行了表征。所制备的姜黄素负载CNDs （Curc-CNDs）尺寸在10 nm左右或以下，稳定性良好。Curc-E-CNDs在溶液中的姜黄素吸附效率为91%，而Curc-U-CNDs的吸附效率为82%。两者的负载能力均为cnd重量的3.4-3.8%。在pH为5的缓冲液中，Curc-E-CNDs和Curc-U-CNDs在72 h内分别释放了60%和74%的姜黄素，在96 h内释放了近90%的姜黄素。这两种Curc-CNDs都被细胞吸收，并对癌细胞表现出明显的细胞毒性。研究结果清楚地描述了CNDs作为姜黄素有效载体的作用，其释放时间延长，生物利用度提高，从而提高了姜黄素的整体抗肿瘤活性。
Despite the potential health benefits of curcumin, such as antioxidant, anticancer, anti-inflammatory, and antimicrobial properties, its usage is limited by poor bioavailability and low aqueous solubility. Nano-formulations of curcumin have gained a lot of attention due to their increased bioavailability, solubility, circulation times, targeted specificity, decreased biodegradation, better stability, and improved cellular uptake. The current study aimed to enhance the bioavailability of curcumin using carbon nanodots (CNDs) as loading vehicles to deliver curcumin due to their excellent biocompatibility, aqueous solubility, and photoluminescence properties. Two types of CNDs (E-CNDs and U-CNDs) were used for curcumin loading and characterized for particle size, morphology, loading capability (measured as adsorption efficiency and loading capacity), stability, photoluminescence properties, in vitro drug release studies, cellular uptake, and anticancer activity. The prepared curcumin-loading CNDs (Curc-CNDs) displayed sizes around or below 10 nm with good stability. The Curc-E-CNDs demonstrated a curcumin adsorption efficiency of 91% in solution, while the Curc-U-CNDs have an adsorption efficiency of 82%. Both have a loading capacity of 3.4-3.8% with respect to the weight of the CNDs. Curcumin release followed a controlled sustained pattern that a total of 60% and 74% of curcumin was released at 72 h from Curc-E-CNDs and Curc-U-CNDs, respectively, in pH 5 buffer, and almost 90% was released in culture media within 96 h. Both of the Curc-CNDs were uptaken by cells and exhibited prominent cytotoxicity toward cancer cells. The results clearly depict the role of CNDs as efficient carriers for curcumin delivery with prolonged release and enhanced bioavailability, thereby improving the overall antitumor activity.