混合油酸-芥酸脂质体作为抗癌药物载体。
Mixed Oleic Acid-Erucic Acid Liposomes as a Carrier for Anticancer Drugs.
机构信息
Department of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur 50603, Malaysia.
Department of Pharmacology, Faculty of Medicine, University of Malaya, Kuala Lumpur 50603, Malaysia.
出版信息
Curr Drug Deliv. 2020;17(4):292-302. doi: 10.2174/1567201817666200210122933.
BACKGROUND
Liposomes are mostly known to be prepared from phospholipids and lipids and have a remarkable capacity to encapsulate both lipophobic and lipophilic molecules. However, there is little research on developing fatty acid liposomes for chemotherapy.
OBJECTIVE
We have successfully prepared mixed fatty acid liposomes from two monounsaturated fatty acids, namely oleic acid and erucic acid, which stabilised by DOPEPEG2000. The Critical Vesicular Concentration (CVC) of liposomes was found to be within 0.09 to 0.21 mmol dm, with an average particle size of 400 nm.
METHODS
Encapsulation of various anticancer drugs such as folinic acid, methotrexate, doxorubicin, or irinotecan resulted in Encapsulation Efficiency (%EE) of up to 90%. Using a 3-(4, 5-dimethylthiazol-2- yl)-2,5-diphenyltetrazolium bromide (MTT) assay, the median Inhibitory Concentration (IC) values of mixed oleic acid-erucic acid encapsulating hydrophilic drugs was remarkably reduced at the end of 24 hours of incubation with the human lung carcinoma cell line A549.
RESULTS
The results suggest that mixed oleic acid-erucic acid liposomes are a potential new approach to further develop as an alternative vehicle of various drugs for cancer treatment.
背景
脂质体主要由磷脂和脂质组成，具有包裹疏水性和亲脂性分子的显著能力。然而，关于开发用于化疗的脂肪酸脂质体的研究甚少。
目的
我们成功地用两种单不饱和脂肪酸油酸和芥酸制备了由 DOPEPEG2000 稳定的混合脂肪酸脂质体。发现脂质体的临界囊泡浓度（CVC）在 0.09 至 0.21 mmol dm 之间，平均粒径为 400nm。
方法
封装各种抗癌药物，如叶酸、甲氨蝶呤、阿霉素或伊立替康，包封效率（%EE）高达 90%。使用 3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐（MTT）测定法，在与人类肺癌细胞系 A549 孵育 24 小时后，混合油酸-芥酸包封亲水性药物的半数抑制浓度（IC）值显著降低。
结果
结果表明，混合油酸-芥酸脂质体是一种有潜力的新方法，可以进一步开发为各种癌症治疗药物的替代载体。
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