J B Varuna Kumara, Ramakrishna Sistla, Madhusudhan Basavaraj
Research Center for Nanoscience and Technology, Department of Biochemistry and Food Technology, Davangere University, Shivagangotri, Davanagere-577 002, Karnataka, India.
Pharmacology Division, Indian Institute of Chemical Technology (IICT), Hyderabad-500 007, India.
IET Nanobiotechnol. 2017 Feb;11(1):96-103. doi: 10.1049/iet-nbt.2016.0062.
Atorvastatin known to be a potential inhibitor of HMG-CoA reductase involved in the synthesis of cholesterol. It is touted as miracle drug due to its profound effect in decreasing the low-density lipoproteins in blood. Unfortunately, the high dosage used poses side-effects relatively in comparison to other statins. On the other hand, curcumin has a diverse therapeutic potential in health and disease. However, the poor aqueous solubility and low bioavailability hinders the therapeutic potential of it when administrated orally. Therefore, it was thought to minimise the frequency of atorvastatin doses to avoid the possibility of drug resistance and also to overcome the limitations of curcumin for desirable therapeutic effects by using nanocarriers in drug delivery. In this investigation, synergistic effect of atorvastatin and curcumin nanocarriers was encapsulated by chitosan polymer. The chitosan nanocarriers prepared by ionic gelation method were characterised for their particle size, zeta potential, and other parameters. The drug-loaded nanocarriers exhibited good encapsulation efficiency (74.25%) and showed a slow and sustained release of atorvastatin and curcumin 60.36 and 61.44%, respectively, in a span of 48 h. The drug-loaded nanocarriers found to be haemocompatible and qualified for drug delivery in atherosclerosis.
阿托伐他汀是已知的参与胆固醇合成的HMG-CoA还原酶的潜在抑制剂。由于其在降低血液中低密度脂蛋白方面的显著作用，它被誉为神奇药物。不幸的是，与其他他汀类药物相比，使用的高剂量会带来相对较多的副作用。另一方面，姜黄素在健康和疾病方面具有多种治疗潜力。然而，其较差的水溶性和低生物利用度阻碍了口服给药时的治疗潜力。因此，人们认为通过在药物递送中使用纳米载体来减少阿托伐他汀的给药频率，以避免耐药性的可能性，并克服姜黄素在实现理想治疗效果方面的局限性。在本研究中，阿托伐他汀和姜黄素纳米载体的协同效应通过壳聚糖聚合物进行包封。通过离子凝胶法制备的壳聚糖纳米载体对其粒径、zeta电位和其他参数进行了表征。载药纳米载体表现出良好的包封效率（74.25%），并在48小时内分别缓慢持续释放阿托伐他汀和姜黄素60.36%和61.44%。发现载药纳米载体具有血液相容性，适用于动脉粥样硬化的药物递送。
