Validation of tumour models for use in anticancer nanomedicine evaluation: the EPR effect and cathepsin B-mediated drug release rate.

ABSTRACT:

Purpose

Intravenously (i.v.) administered nanomedicines have the potential for tumour targeting due to the enhanced permeability and retention (EPR) effect, but in vivo tumour models are rarely calibrated with respect to functional vascular permeability and/or mechanisms controlling intratumoural drug release. Here the effect of tumour type and tumour size on EPR-mediated tumour localisation and cathepsin B-mediated drug release was studied.

Methods

Evans Blue (10 mg/kg) and an N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer–doxorubicin (Dox) conjugate (FCE28068) (5 mg/kg Dox-equiv) were used as probes and tumour levels (and Dox release) measured at 1 h after i.v. administration in a panel of murine and human xenograft tumours.

Results

Evans Blue and FCE28068 disp

SUBMITTER: Duncan R 

PROVIDER: S-EPMC3718995 | biostudies-literature | 2013 Aug

REPOSITORIES: biostudies-literature