Ethanol injection method for hydrophilic and lipophilic drug-loaded liposome preparation
Ethanol injection method for hydrophilic and lipophilic drug-loaded liposome preparation
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DOI：
10.3109/08982100903347923
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发表时间：
2010-09-01
影响因子：
4.4
通讯作者：
Fessi, Hatem
中科院分区：
文献类型：
--
作者：
Jaafar-Maalej, Chiraz;Diab, Roudayna;Fessi, Hatem
在这篇文章中，疏水性（丙酸倍氯米松; BDP）和亲水性（阿糖胞苷; Ara-C）药物已被封装在脂质体中，以便通过肺部途径给药。为此，选择了一种易于放大的脂质体制备方法，即乙醇注射法。研究了关键工艺和配方参数的影响。制备载药脂质体，并在尺寸、zeta电位、包封率、释放研究、细胞摄取和空气动力学行为方面进行表征。成功地获得了尺寸在约80至170 nm范围内的小的多层囊泡。结果表明，磷脂和胆固醇的量对脂质体的大小和包封率的显着影响。疏水性药物（BDP）的包封率约为100%，亲水性药物（Ara-C）的包封率约为16%。体外释放研究表明，与Ara-C相比，BDP的释放曲线延长，Ara-C释放更快。细胞摄取试验表明，荧光脂质体已被很好地内化到SW-1573人肺癌细胞的细胞质中，证实了使用脂质体用于肺细胞靶向的可能性。雾化Ara-C和BDP脂质体的空气动力学直径与肺深部沉积相一致。总之，精心制作的脂质体似乎是阿糖胞苷和BDP肺部给药的有前途的载体。
In this article, a hydrophobic (beclomethasone dipropionate; BDP) and a hydrophilic (cytarabine; Ara-C) drugs have been encapsulated in liposomes in order to be administered via the pulmonary route. For this aim, a liposome preparation method, which is easy to scale up, the ethanol injection method, has been selected. The effects of critical process and formulation parameters have been investigated. The drug-loaded liposomes were prepared and characterized in terms of size, zeta potential, encapsulation efficiency, release study, cell uptake, and aerodynamic behavior. Small multilamellar vesicles, with sizes ranging from about 80 to 170 nm, were successfully obtained. Results indicated a significant influence of phospholipid and cholesterol amounts on liposome size and encapsulation efficiency. The higher encapsulation efficiencies were about 100% for the hydrophobic drug (BDP) and about 16% for the hydrophilic one (Ara-C). The in vitro release study showed a prolonged release profile for BDP, in contrast with Ara-C, which was released more rapidly. The cell-uptake test revealed that fluorescent liposomes have been well internalized into the cytoplasm of SW-1573 human lung carcinoma cells, confirming the possibility to use liposomes for lung cell targeting. Nebulized Ara-C and BDP liposomes presented aerodynamic diameters compatible with deep lung deposition. In conclusion, the elaborated liposomes seem to be promising carriers for both Ara-C and BDP pulmonary delivery.