リポソーム- SOD の調製と静脈内投与後の血中動態

概要

論文の詳細を見る
Liposomal-encapsulated superoxide dismutase (L-SOD) was prepared with a view to prolonging the half-life and pharmacodynamic action time. Presome^<[◯!R]> was adopted as a phospholipid in the preparation of L-SOD. L-SOD was sterilized through polycarbonate membrane filters having pore diameters of 0.2μm and 0.4μm. The liposomal particle size, as measured by the dynamic light scattering method, was 198±40 nm. Effective SOD encapsulation efficiency was approximately 25.8%. Immediately after the i.v. injection of L-SOD into rats, blood levels of SOD decreased in a bi-exponential manner; the half-lives of the a-and p-phases were 16.6minutes and 7.8hours, respectively. AUC and MRT increased as compared with the i.v. injection of r-hSOD (free SOD). The SOD-activity in plasma was on a low level. These results suggested that still more L-SOD was trapped in the reticulo-endothelial system (RES), involving such organs as in the liver and spleen. In an effect to increase the SOD activity in plasma and prolong the circulation time of lipo-somes in blood, we prepared L-SOD modified with polyethyleneglycol derivatives (L-SOD/PEG-DOPE; L-SOD/PEG.DMG). After the i.v. injection of L-SOD/PEG・DOPE and L-SOD/PEG.DMG into rats, the SOD activity in plasma became higher and also the circulation time of liposomes in blood became longer as compared with the L-SOD i.v. injection.
日本医療薬学会の論文
1994-02-20