Document Detail

Methotrexate-loaded chitosan- and glycol chitosan-based nanoparticles: a promising strategy for the administration of the anticancer drug to brain tumors.
MedLine Citation:
PMID:  21948322     Owner:  NLM     Status:  MEDLINE    
Brain tumor treatment employing methotrexate (MTX) is limited by the efflux mechanism of Pg-p on the blood-brain barrier. We aimed to investigate MTX-loaded chitosan or glycol chitosan (GCS) nanoparticles (NPs) in the presence and in the absence of a coating layer of Tween 80 for brain delivery of MTX. The effect of a low Tween 80 concentration was evaluated. MTX NPs were formulated following the ionic gelation technique and size and zeta potential measurements were acquired. Transport across MDCKII-MDR1 monolayer and cytotoxicity studies against C6 glioma cell line were also performed. Cell/particles interaction was visualized by confocal microscopy. The particles were shown to be cytotoxic against C6 cells line and able to overcome MDCKII-MDR1 cell barrier. GCS-based NPs were the most cytotoxic NPs. Confocal observations highlighted the internalization of Tween 80-coated fluorescent NPs more than Tween 80-uncoated NPs. The results suggest that even a low concentration of Tween 80 is sufficient for enhancing the transport of MTX from the NPs across MDCKII-MDR1 cells. The nanocarriers represent a promising strategy for the administration of MTX to brain tumors which merits further investigations under in vivo conditions.
Adriana Trapani; Nunzio Denora; Giuliano Iacobellis; Johannes Sitterberg; Udo Bakowsky; Thomas Kissel
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2011-09-27
Journal Detail:
Title:  AAPS PharmSciTech     Volume:  12     ISSN:  1530-9932     ISO Abbreviation:  AAPS PharmSciTech     Publication Date:  2011 Dec 
Date Detail:
Created Date:  2011-11-29     Completed Date:  2012-03-26     Revised Date:  2013-06-27    
Medline Journal Info:
Nlm Unique ID:  100960111     Medline TA:  AAPS PharmSciTech     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1302-11     Citation Subset:  IM    
Department of Pharmaceutical Chemistry, School of Pharmacy, University of Bari, Italy.
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MeSH Terms
Antimetabolites, Antineoplastic / administration & dosage,  chemistry,  metabolism*
Blood-Brain Barrier / metabolism
Brain Neoplasms / metabolism*,  pathology
Capillary Permeability
Cell Line
Cell Survival / drug effects
Chemistry, Pharmaceutical
Chitosan / analogs & derivatives,  chemistry*
Dose-Response Relationship, Drug
Drug Carriers*
Drug Compounding
Glycols / chemistry*
Methotrexate / administration & dosage,  chemistry,  metabolism*
Microscopy, Atomic Force
Microscopy, Confocal
P-Glycoprotein / genetics,  metabolism
Particle Size
Polysorbates / chemistry
Technology, Pharmaceutical / methods*
Reg. No./Substance:
0/Antimetabolites, Antineoplastic; 0/Drug Carriers; 0/Glycols; 0/P-Glycoprotein; 0/Polysorbates; 59-05-2/Methotrexate; 9012-76-4/Chitosan

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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