Lv Xiaoyan, Yin Junjing, Yang Xiucheng, Liu Sha, Sun Kaoxiang
School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, China.
Zhongguo Fei Ai Za Zhi. 2018 Sep 20;21(9):663-669. doi: 10.3779/j.issn.1009-3419.2018.09.02.
Afatinib, a second-generation irreversible epidermal growth factor inhibitor receptor for the development of non-small cell lung cancer and secondary drug resistance, has low bioavailability and adverse reactions due to current oral administration. The aim of this study was to prepare a novel drug delivery system, afatinib liposome, and to establish a method for the determination of encapsulation efficiency.
Four different preparation methods were used to prepare afatinib liposomes, and the optimal preparation process was determined by comparing the encapsulation efficiency and particle size.
It has been verified that sephadex microcolumn centrifugation can be used to purify afatinib liposomes, and UV spectrophotometry can be employed to determine the entrapment efficiency of liposomes. Among different preparation methods, the encapsulation efficiency of afatinib liposomes prepared by ammonium sulfate gradient method was 90.73% and the average particle size was 108.6 nm.
Ammonium sulfate gradient method can be successfully applied to prepare afatinib liposomes that performed higher encapsulation efficiency and smaller particle size. The UV spectrophotometry employed to determine the liposome encapsulation efficiency was easy operation and with high accuracy.
阿法替尼是一种用于非小细胞肺癌治疗及继发性耐药的第二代不可逆表皮生长因子抑制剂受体，目前口服给药存在生物利用度低及不良反应等问题。本研究旨在制备一种新型药物递送系统——阿法替尼脂质体，并建立一种测定包封率的方法。
采用四种不同的制备方法制备阿法替尼脂质体，通过比较包封率和粒径确定最佳制备工艺。
已证实葡聚糖凝胶微柱离心法可用于纯化阿法替尼脂质体，紫外分光光度法可用于测定脂质体的包封率。在不同制备方法中，采用硫酸铵梯度法制备的阿法替尼脂质体包封率为90.73%，平均粒径为108.6nm。
硫酸铵梯度法可成功应用于制备包封率较高、粒径较小的阿法替尼脂质体。采用紫外分光光度法测定脂质体包封率操作简便、准确性高。
