Antitumor Activity of Doxorubicin Encapsulated in Poly (ethylene glycol)-Coated Liposomes

Antitumor Activity of Doxorubicin Encapsulated in Poly (ethylene glycol)-Coated Liposomes

The antitumor activity of doxorubicin (DXR) which had been encapsulated in poly (ethylene glycol) (PEG)-coated long-circulating liposomes was examined in mice inoculated with colon 26 carcinoma cells. Six mol% of the distearoylphosphatidylethanolamine derivative of PEGs with different molecular weig...

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Bibliographic Details
Published in:Biological & pharmaceutical bulletin Vol. 18; no. 9; pp. 1234 - 1237
Main Authors: HOSODA, Junichi, UNEZAKI, Sakae, MARUYAMA, Kazuo, TSUCHIYA, Seishi, IWATSURU, Motoharu
Format: Journal Article
Language:English
Published: Tokyo The Pharmaceutical Society of Japan 1995
Maruzen
Japan Science and Technology Agency
Subjects:
Animals
Antibiotics, Antineoplastic - administration & dosage
Antineoplastic agents
Biological and medical sciences
Chemotherapy
doxorubicin
Doxorubicin - administration & dosage
Doxorubicin - pharmacokinetics
Drug Carriers
drug delivery system
liposome
Liposomes
long-circulating liposome
Male
Medical sciences
Mice
Mice, Inbred BALB C
Neoplasms, Experimental - drug therapy
Pharmacology. Drug treatments
poly (ethylene glycol)
Polyethylene Glycols - administration & dosage
Antineoplastic agent
Control release polymer
Rodentia
Liposome
Drug carrier
Biological activity
Ethylene oxide polymer
Vertebrata
Mammalia
Mouse
Animal
Formulation
Dosage form
Anthracyclins
Pharmacokinetics
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Summary:The antitumor activity of doxorubicin (DXR) which had been encapsulated in poly (ethylene glycol) (PEG)-coated long-circulating liposomes was examined in mice inoculated with colon 26 carcinoma cells. Six mol% of the distearoylphosphatidylethanolamine derivative of PEGs with different molecular weights was incorporated in liposomes (90-110nm, mean diameter) composed of distearoylphosphatidylcholine/cholesterol (1/1, molar ratio), and the encapsulating efficiency of DXR in liposomes was more than 98% by the pH gradient method. Each concentration of DXR in blood and tumor tissue was significantly greater after administration of the drug encapsulated in PEG-coated liposomes (DXR-PEG-liposome) compared to the non-coated control liposomes or non-encapsulated free drug. DXR-PEG-liposome prepared with PEG1000 (DXR-PEG1000-liposome) more effectively increased the level of DXR in blood and tumor than did the preparations with PEG5000 or PEG12000. A single treatment with DXR-PEG1000-liposome (10mg DXR/kg) resulted in increased survival time. Further therapeutic improvement in terms of tumor growth retardation and prolongation of survival time were observed following multiple treatments with DXR-PEG1000-liposome (3×5mg DXR/kg). Long-circulating liposome coating optimized PEGs should be useful for the delivery of chemotherapeutic agents for the treatment of solid tumors.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.18.1234