In Vitro and in Vivo Evaluation of Paclitaxel–Lapatinib-Loaded F127 Pluronic Micelles Publisher Pubmed



Dehghankelishadi P^{1, 2} ; Saadat E¹ ; Ravar F¹ ; Safavi M³ ; Pordeli M⁴ ; Gholami M⁵ ; Dorkoosh FA^{1, 2} Show Affiliations
Source: Drug Development and Industrial Pharmacy Published:2017

Abstract

The aim of this study was to evaluate the in vitro and in vivo efficacy of paclitaxel–lapatinib-loaded Pluronic micelles. Lapatinib and pluronic sensitize the cancerous cells to paclitaxel via efflux pump inhibition. In addition, pluronic polymers can trigger intrinsic apoptosis pathways. Furthermore, micellar system can passively target the chemotherapeutic agents by enhanced permeability and retention effect. The paclitaxel–lapatinib-loaded micelles were characterized in means of encapsulation efficacy and size. The in vitro analyses were performed by MTT assay and uptake studies. Real-time imaging and in vivo anti-tumor efficacy studies were also performed. The prepared micelles have acceptable encapsulation ratio and size. Hemolysis assay confirmed that the micelles are hemo-compatible. MTT assay demonstrated that drug-loaded micelles have superior cytotoxicity compared with the naked drugs. The confocal microscopy and flowcytometry analyses showed that micelles are mainly internalized by endocytosis. According to the results of the in vivo imaging, the micelles are accumulated within liver. In vivo anti-tumor efficacy studies confirmed that tumor inhibition of drug-loaded micelles was significant compared to Intaxel®. © 2016 Informa UK Limited, trading as Taylor & Francis Group.