Therapeutic effect of adriamycin encapsulated in long‐circulating liposomes on meth‐a‐sarcoma‐bearing mice

International Journal of Cancer - Tập 58 Số 3 - Trang 415-419 - 1994
Naoto Oku1, Kanako Doi1, Yukihiro Namba2, Osami Shoji1
1Department of Radiobiochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Yacta, Shizuoka 422, Japan
2Research Laboratories, Nippon fine Chemical Co. Ltd., Takasago, Hyogo 676, Japan

Tóm tắt

AbstractLong‐circulating liposomes modified with a uronic‐acid derivative, palmityl‐D‐glucuronide (PGIcUA), have been developed previously for the passive targeting of liposomes to tumor tissues. In this study, we examined the therapeutic effect of adriamycin (ADM) encapsulated in PGIcUA liposomes composed of dipalmitoylphosphatidylcholine (DPPC), cholesterol (Chol) and PGIcUA (molar ratio, 40/40/10) since this amount of PGIcUA was enough to endow liposomes with long‐circulating activity. Long‐circulating activity was also observed with palmityl‐D‐galacturonide (PGalUA) modified liposomes, suggesting that uronic acid plays an important role in preventing liposomes from being trapped in the reticuloendothelial system (RES). ADM was loaded in liposomes by a remote‐loading method. Free or liposomal ADM was injected i.v. into BALB/c mice bearing s.c.‐implanted Meth‐A sarcoma. The liposomal formulation was efficient for reducing tumors, prolonging survival time and curing the animals, especially in the case of large tumors where free ADM was not. Furthermore, PGIcUA liposomes were more effective than conventional liposomes containing dipalmitoylphosphatidylglycerol (DPPG) instead of PGIcUA for prolonging survival time in mire. It might therefore be appropriate to use PGIcUA liposomes as the carriers of anticancer drugs.

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International Journal of Cancer

Tập 58 Số 3

415-419

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