Wang Ting, Wang Ning, Jin Xin, Zhang Kai, Li Tiefu
Department of Pharmacy, Jining Medical College, No. 669 Xueyuan Road, Sunshine City (Rizhao), Shandong Province 276826, China.
J Liposome Res. 2009;19(3):231-40. doi: 10.1080/08982100902788390.
A novel liposome preparation method is described involving the freeze-drying of oil-in-water emulsions containing sucrose in the aqueous phase as a lyoprotectant and phospholipids in the oil as emulsifiers. The oil-in-water emulsions can be prepared by emulsification and then lyophilized to obtain dry products that will, upon rehydration, form unilamellar liposomes with a mean size of less than 200 nm, as proved by dynamic light scattering, atomic force micrographs, freeze-fracture electron micrographs, and small-angle X-ray scattering (SAXS). With or without combination with active loading, this method can be used successfully to encapsulate amphiphilic or lipophilic drugs into liposomes, although it cannot be applied to hydrophilic drugs. The lyophilized products are stable and can be rehydrated to form liposomes, even after a storage period of 10 months. Based on the encapsulation efficiency for hydrophilic drugs, as well as the scanning electron micrograph and SAXS of the freeze-dried products, a unique liposome formation mechanism is proposed.
描述了一种新型脂质体制备方法，该方法涉及对水包油乳液进行冷冻干燥，其中水相含有作为冻干保护剂的蔗糖，油相中含有作为乳化剂的磷脂。水包油乳液可通过乳化制备，然后冻干以获得干燥产物，经动态光散射、原子力显微镜图像、冷冻断裂电子显微镜图像和小角X射线散射（SAXS）证明，该干燥产物在复水后将形成平均尺寸小于200 nm的单层脂质体。无论是否与主动载药相结合，该方法都能成功地将两亲性或亲脂性药物包封到脂质体中，不过它不适用于亲水性药物。冻干产物很稳定，即使在储存10个月后仍可复水形成脂质体。基于对亲水性药物的包封效率以及冻干产物的扫描电子显微镜图像和SAXS，提出了一种独特脂质体形成机制。
