University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Studies, Panjab University, Chandigarh, 160 014, India.
Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist. Ajmer, Rajasthan, 305 817, India.
AAPS PharmSciTech. 2019 Feb 5;20(3):100. doi: 10.1208/s12249-019-1301-7.
Beta-carotene (BC), a red-colored pigment found in plants and animals, is one of the most extensively investigated carotenoids due to its provitamin-A, antioxidant, and anticancer properties. The anticancer activity of BC through oral administration is severely affected due to its low bioavailability and oxidative degradation. The present study aimed to formulate and characterize solid lipid nanoparticles (SLNs) of BC for enhanced bioavailability and therapeutic efficacy. Beta-carotene-loaded solid lipid nanoparticles (BC-SLNs) were prepared employing different combinations of glyceryl monostearate and gelucire. The characterization studies were performed for particle size, morphology, release behavior, and stability. BC-SLNs were also studied for in vitro cytotoxicity in human breast cancer cell lines (MCF-7) and pharmacokinetic studies in Wistar rats. The cytotoxicity studies confirmed that encapsulation of BC within the lipid bilayers of nanoparticles did not affect its anticancer efficacy. An improved anticancer activity was observed in BC-SLNs as compared to the free BC. BC-SLNs enhanced the bioavailability of BC on oral administration by sustaining its release from the lipid core and prolongation of circulation time in the body. Similarly, area under the curve (AUC) enhanced 1.92-times more when BC was incorporated into SLNs as compared to free BC. In conclusion, solid lipid nanoparticles could be an effective and promising strategy to improve the biopharmaceutical properties of carotenoids for anticancer effects.
β-胡萝卜素（BC）是一种存在于动植物中的红色色素，由于其具有维生素 A 前体、抗氧化和抗癌特性，因此是研究最多的类胡萝卜素之一。由于其生物利用度低和氧化降解，BC 通过口服的抗癌活性受到严重影响。本研究旨在制备和表征β-胡萝卜素固体脂质纳米粒（BC-SLNs），以提高其生物利用度和治疗效果。采用不同组合的单硬脂酸甘油酯和 Gelucire 制备负载β-胡萝卜素的固体脂质纳米粒（BC-SLNs）。对粒径、形态、释放行为和稳定性进行了表征研究。还研究了 BC-SLNs 在人乳腺癌细胞系（MCF-7）中的体外细胞毒性和在 Wistar 大鼠中的药代动力学研究。细胞毒性研究证实，BC 被包裹在纳米粒的脂质双层内不会影响其抗癌功效。与游离 BC 相比，BC-SLNs 表现出增强的抗癌活性。BC-SLNs 通过从脂质核中持续释放并延长其在体内的循环时间，提高了口服 BC 的生物利用度。同样，当 BC 被纳入 SLNs 时，AUC 增加了 1.92 倍，与游离 BC 相比。总之，固体脂质纳米粒可能是一种有效和有前途的策略，可以改善类胡萝卜素的生物制药特性，以达到抗癌效果。
