Pegylated liposomal doxorubicin (DOXIL®, CAELYX®) distribution in tumour models observed with confocal laser scanning microscopy

Autor:	Paul S Uster, Peter K Working, Jan Vaage
Rok vydání:	1998
Předmět:	Pathology medicine.medical_specialty Liposome Chemistry Confocal Pharmaceutical Science Dosage form In vivo medicine Biophysics Doxorubicin Hydrochloride Distribution (pharmacology) Doxorubicin Drug carrier medicine.drug
Zdroj:	International Journal of Pharmaceutics. 162:77-86
ISSN:	0378-5173
DOI:	10.1016/s0378-5173(97)00415-8
Popis:	The activity of doxorubicin hydrochloride in preclinical tumor models is markedly improved by encapsulation in pegylated liposomes (DOXIL, CAELYX). To understand this response in better detail, spatial and temporal drug distribution in frozen tumor sections was observed with confocal laser scanning (CLS) microscopy. Tumor tissue absorption and distribution phases were markedly altered by pegylated liposome encapsulation. The resultant tumor tissue area under the curve was increased at least several fold over an equivalent dose of free drug. The majority of visible fluorescence was in the nuclear compartment; encapsulated drug apparently leaves liposomes in the interstitial spaces within minutes and appears in the nucleus. Pilot experiments suggest that drug and lipid uncouple at an extracellular location. The increased nuclear exposure to drug is likely responsible for the enhanced therapeutic effect of encapsulation in pegylated liposomes.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::c9cde7f3646408409ed293229ddb1cdb https://doi.org/10.1016/s0378-5173(97)00415-8 Zobrazit plný text záznamu Full Text from ScienceDirect