Niven R W, Schreier H
Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville 32610.
Pharm Res. 1990 Nov;7(11):1127-33. doi: 10.1023/a:1015924124180.
A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, stearylamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 min at an output flow rate of 4.7 liters of air/min. The effects of nebulization on the vesicles were determined by monitoring the release of encapsulated 5,6-carboxylfluorescein (CF) from dispersions containing approximately 200 micrograms of total CF, of which 93.1 +/- 2.4% (N = 18) was initially encapsulated. In all experiments CF was released from the liposomes while being aerosolized, and this ranged from a mean of 12.7 +/- 3.8 to 60.9 +/- 1.9% of the encapsulated CF, depending upon the lipid composition. The lipid concentration in the dispersions did not affect the rate or percentage release of CF over a range of approximately 0.5 to 50 mg per nebulized dispersion. If liposomes are to be used as drug carriers in an inhalation aerosol a lipid composition should be employed which will minimize the release of encapsulated drug caused by nebulization.
用含有0至30摩尔%胆固醇、硬脂胺或二棕榈酰磷脂酰甘油的大豆磷脂酰胆碱或氢化大豆磷脂酰胆碱的脂质制备了一系列多层脂质体分散体。脂质体分散体用科里森雾化器以4.7升空气/分钟的输出流速雾化80分钟。通过监测含有约200微克总5,6-羧基荧光素（CF）的分散体中包封的5,6-羧基荧光素（CF）的释放来确定雾化对囊泡的影响，其中93.1±2.4%（N = 18）最初被包封。在所有实验中，CF在雾化时从脂质体中释放出来，根据脂质组成，释放量占包封CF的12.7±3.8%至60.9±1.9%。分散体中的脂质浓度在每雾化分散体约0.5至50毫克的范围内不影响CF的释放速率或释放百分比。如果脂质体要用作吸入气雾剂中的药物载体，应采用能使雾化引起的包封药物释放最小化的脂质组成。
