Shaker Sherif, Gardouh Ahmed Rifaat, Ghorab Mamdouh Mostafa
Department of Pharmaceutical Research, Faculty of Pharmacy and Drug Technology, Heliopolis University for Sustainable Development, 2834 El Horreya, Cairo, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt.
Res Pharm Sci. 2017 Oct;12(5):346-352. doi: 10.4103/1735-5362.213979.
Ethanol injection is one of the techniques frequently used to produce liposomes which favors both simplicity and safety. In this process, an ethanolic solution of lipids is rapidly injected into an aqueous medium through a needle, dispersing the phospholipids throughout the medium and promoting the vesicle formation. Being a critical parameter that determines the fate of liposome and its distribution, we studied different factors affecting the particle size of liposomes including different phospholipid (Phosal 53 MCT) and cholesterol concentrations and the use of different types of non-ionic surfactants at fixed Phosal 53 MCT concentration of 50 mg per formulation. Both Phosal 53 MCT and cholesterol concentration had direct effect on liposomes particle size. Non-ionic surfactants produced liposomes of smaller particle size when compared to conventional liposomes formed using Phosal 53 MCT 300 mg per formulation only, whereas this effect was diminished when higher Phosal 53 MCT to cholesterol ratios were used that obviously increased liposomes size. Smaller liposomes sizes were obtained upon using non-ionic surfactants of lower hydrophilic/hydrophobic balance (HLB) as both Tween 80 and Cremophor RH 40 produced liposomes of smaller particle size compared to Poloxamer 407. The smallest liposomes particle size was successfully obtained in the formulation comprising 300 mg Phosal MCT, 150 mg cholesterol and 50 mg Tween 80.
乙醇注入法是常用于制备脂质体的技术之一,该方法兼具简便性与安全性。在此过程中,脂质的乙醇溶液通过针头快速注入水相中,使磷脂分散于整个介质中并促进囊泡形成。作为决定脂质体命运及其分布的关键参数,我们研究了不同因素对脂质体粒径的影响,包括不同的磷脂(Phosal 53 MCT)和胆固醇浓度,以及在每制剂固定Phosal 53 MCT浓度为50 mg的情况下使用不同类型的非离子表面活性剂。Phosal 53 MCT和胆固醇浓度均对脂质体粒径有直接影响。与仅使用每制剂300 mg Phosal 53 MCT形成的传统脂质体相比,非离子表面活性剂产生的脂质体粒径更小,然而当使用更高的Phosal 53 MCT与胆固醇比例时,这种效果会减弱,这明显增加了脂质体的大小。使用亲水/亲油平衡(HLB)较低的非离子表面活性剂可获得较小的脂质体粒径,因为与泊洛沙姆407相比,吐温80和聚氧乙烯蓖麻油RH 40产生的脂质体粒径更小。在包含300 mg Phosal MCT、150 mg胆固醇和50 mg吐温80的制剂中成功获得了最小的脂质体粒径。