多囊脂质体-海藻酸钠微球的理化性质及初步稳定性研究

Physicochemical Property and Stability of MVLs-Alg Microspheres

目的:制备蛋白类药物的多囊脂质体-海藻酸钠(MVLs-Alg)微球,并研究其理化性质和初步的稳定性。方法:以牛血清蛋白(BSA)为模型蛋白药物,采用内部/凝胶化法制备MVLs-Alg微球,然后采用差示热分析MVLs-Alg微球中MVLs与Alg之间的关系,以及研究温度(4、25、40℃)对其包封率和基质中磷脂的过氧化值的影响。结果:制备的微球球型度好,MVLs与Alg之间可能发生了相互吸附,放置90d时,4、25、40℃条件下微球包封率分别为85.36%、63.75%、50.49%,磷脂过氧化值随温度升高不断增大,但与MVLs比较变化不明显。结论:所制备的微球明显提高了脂类的稳定性,可用于蛋白质类药物的输送。

OBJECTIVE： To prepare multivesicular liposomes-sodium polymannuronate microspheres （MVLs-Alg） for protein drugs and to study the physico - chemical property and elementary stability of MVLs - Alg. METHODS： MVLs and Alg were used as matrix and BSA as a model protein drug, MVLs- Alg microspheres were prepared by interior/ gelatin method. The relationship between MVLs and Alg was analyzed by differential thermal analysis and the effect of temperature （4, 25, 40 ℃ ） on entrapment efficiency and peroxide value of phospholipid in base material was investigated. RESULTS： The MVLs-Alg microspheres were spherical. Analyzed by DTA, it was considered that physical adsorption between MVLs and Alg was potentially existed. Storing for 90 days at 4, 25, and 40 ℃ respectively, the encapsulation efficiency of the MVLs- Alg microsphereswere were 85.36%, 63.75%, and 50.49%, respectively. The peroxide value of phospholipid increased increasingly, but not significant as compared with MVLs. CONCLUSIONS： The stability of MVLs- Alg microspheres was heightened compared with that of MVLs and which can be used for the delivery of protein drugs.