Tumor Uptake and Therapeutic Effects of Drugs Encapsulated in Long-Circulating Pegylated Stealth® Liposomes

Autor:	Gail Colbern, Jan Vaage, Dorothy Donovan, Paul Uster, Peter Working
Rok vydání:	2000
Předmět:	Drug Liposome Materials science Cholesterol media_common.quotation_subject Phospholipid Pharmaceutical Science Pharmacology law.invention chemistry.chemical_compound chemistry Confocal microscopy law Cytoplasm Phosphatidylcholine medicine Doxorubicin medicine.drug media_common
Zdroj:	Journal of Liposome Research. 10:81-92
ISSN:	1532-2394 0898-2104
DOI:	10.3109/08982100009031097
Popis:	In this study, tumor uptake and clearance of doxorubicin were determined for two formulations of the drug: the free form in aqueous solution and the encapsulated form in polyethylene glycol-coated (pegylated, STEALTH®) liposomes composed of cholesterol/hydrogenated soy phosphatidylcholine/ polyethylene glycol-distearoyl-phosphatidyl-ethanolamine (Doxil®). The determinations used confocal laser scanning microscopy in a pancreatic carcinoma model in nude mice. The movement of pegylated liposomes containing doxorubicin from blood vessels into tumors was studied using confocal microscopy combined with autoradiography of liposomes containing a tritium-labeled phospholipid. Laser microscopy measurements showed that the lipo-some-encapsulated doxorubicin remained in the tumor longer than the free drug and produced a six-fold increase in the area under the concentration-time curve (AUC). Autoradiography showed that the extravasated tritium-labeled lipid had entered the nuclei as well as the cytoplasm of t...
Databáze:	OpenAIRE
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