Qi X R, Maitani Y, Shimoda N, Sakaguchi K, Nagai T
Department of Pharmaceutics, Hoshi University, Tokyo, Japan.
Chem Pharm Bull (Tokyo). 1995 Feb;43(2):295-9. doi: 10.1248/cpb.43.295.
We encapsulated erythropoietin (Epo) in dipalmitoylphosphatidylcholine (DPPC) liposomes with soybean-derived sterols (SS-liposomes) and its glucoside (SG-liposomes) by reverse-phase evaporation vesicle method, and evaluated them by subcutaneous administration in rats. With 4 min of sonication, the damage to Epo activity was observed mainly in the non-encapsulated Epo in the liposomes. This study indicated that the bilayer of liposomes had the ability to protect the Epo activity, by reducing the aggregation that was caused by interaction between Epo molecules. The SG-liposomes had a higher retention of the Epo activity the SS-liposomes. 25.3% or 33.6% of activity was retained by SS-liposomes under the conditions of 4 min or 1 min of sonication, while 53.3% or 58.3% of the activity was retained by SG-liposomes under the same conditions. Shorter sonication was available to minimize the loss of the Epo activity. Epo in SG-liposomes appeared to increase the activity.
我们通过反相蒸发囊泡法将促红细胞生成素（Epo）包裹在含有大豆衍生甾醇的二棕榈酰磷脂酰胆碱（DPPC）脂质体（SS-脂质体）及其葡糖苷（SG-脂质体）中，并通过在大鼠皮下给药来评估它们。超声处理4分钟时，观察到脂质体中未包裹的Epo的活性主要受到损伤。该研究表明，脂质体双层能够通过减少Epo分子间相互作用引起的聚集来保护Epo活性。SG-脂质体对Epo活性的保留率高于SS-脂质体。在超声处理4分钟或1分钟的条件下，SS-脂质体保留了25.3%或33.6%的活性，而在相同条件下，SG-脂质体保留了53.3%或58.3%的活性。较短时间的超声处理可将Epo活性的损失降至最低。SG-脂质体中的Epo似乎提高了活性。
