Center of Excellence in Natural Products for Ageing and Chronic Diseases, Chulalongkorn University, Bangkok 10330, Thailand; Pharmaceutical Sciences and Technology Program, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.
Center of Excellence in Natural Products for Ageing and Chronic Diseases, Chulalongkorn University, Bangkok 10330, Thailand; Pharmaceutical Sciences and Technology Program, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.
Carbohydr Polym. 2022 Jul 15;288:119401. doi: 10.1016/j.carbpol.2022.119401. Epub 2022 Mar 24.
Chitosan (Ch)-coated nanostructured lipid carriers (NLCs) have great potential for transdermal delivery with high localization of chemotherapeutics in breast cancer. This study used tetrahydrocurcumin (THC), a primary metabolite of curcumin with enhanced antioxidant and anticancer properties, as a model compound to prepare NLCs. Response surface methodology was employed to optimize THC-loaded Ch-coated NLCs (THC-Ch-NLCs) fabricated by high-shear homogenization. The optimized THC-Ch-NLCs had particle size of 244 ± 18 nm, zeta potential of -17.5 ± 0.5 mV, entrapment efficiency of 76.6 ± 0.2% and drug loading of 0.28 ± 0.01%. In vitro release study of THC-Ch-NLCs showed sustained release following the Korsmeyer-Peppas model with Fickian and non-Fickian diffusion at pH 7.4 and 5.5, respectively. THC-Ch-NLCs demonstrated significantly enhanced in vitro skin permeation, cell uptake, and remarkable cytotoxicity toward MD-MBA-231 breast cancer cells compared to the unencapsulated THC, suggesting Ch-NLCs as potential transdermal nanocarriers of THC for triple-negative breast cancer treatment.
壳聚糖（Ch）涂层的纳米结构化脂质载体（NLCs）具有将化学疗法药物高度定位在乳腺癌中的经皮递药的巨大潜力。本研究使用四氢姜黄素（THC）作为模型化合物来制备 NLCs，THC 是姜黄素的主要代谢物，具有增强的抗氧化和抗癌特性。采用响应面法优化了通过高剪切匀化制备的负载姜黄素的壳聚糖（Ch）涂层的纳米结构化脂质载体（THC-Ch-NLCs）。优化的 THC-Ch-NLCs 的粒径为 244 ± 18nm，Zeta 电位为-17.5 ± 0.5mV，包封效率为 76.6 ± 0.2%，载药量为 0.28 ± 0.01%。THC-Ch-NLCs 的体外释放研究表明，在 pH 7.4 和 5.5 下，分别遵循 Korsmeyer-Peppas 模型，呈现出溶出的持续释放，具有 Fickian 和非 Fickian 扩散。与未包封的 THC 相比，THC-Ch-NLCs 表现出显著增强的体外皮肤渗透、细胞摄取以及对 MD-MBA-231 乳腺癌细胞的显著细胞毒性，表明 Ch-NLCs 是治疗三阴性乳腺癌的潜在经皮纳米载体。
