Sterically stabilized liposomes: improvements in pharmacokinetics and antitumor therapeutic efficacy.

Demetrios Papahadjopoulos1, Theresa M. Allen1, Alberto Gabizón1, E. Mayhew1, Katherine K. Matthay1, S.K. Huang1, K D Lee1, Martin C. Woodle1, Danilo D. Lasič1, C. T. Redemann1
1Department of Pharmacology, University of California, San Francisco 94143.

Tóm tắt

The results obtained in this study establish that liposome formulations incorporating a synthetic polyethylene glycol-derivatized phospholipid have a pronounced effect on liposome tissue distribution and can produce a large increase in the pharmacological efficacy of encapsulated antitumor drugs. This effect is substantially greater than that observed previously with conventional liposomes and is associated with a more than 5-fold prolongation of liposome circulation time in blood, a marked decrease in uptake by tissues such as liver and spleen, and a corresponding increased accumulation in implanted tumors. These and other properties described here have expanded considerably the prospects of liposomes as an effective carrier system for a variety of pharmacologically active macromolecules.

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