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Lecithin/chitosan controlled release nanopreparations of tamoxifen citrate: loading, enzyme-trigger release and cell uptake.
- Source :
-
Journal of controlled release : official journal of the Controlled Release Society [J Control Release] 2013 May 10; Vol. 167 (3), pp. 276-83. Date of Electronic Publication: 2013 Feb 18. - Publication Year :
- 2013
-
Abstract
- Tamoxifen citrate (TAM), an anticancer drug with amphiphilic properties, was loaded in lecithin/chitosan nanoparticles (LCN) with a view to oral administration. The influence of tamoxifen loading on the physico-chemical properties of nanoparticles was studied. Size, surface charge and morphological properties of tamoxifen-loaded nanoparticles (LCN-TAM) were assessed. The increase in the tamoxifen amount in the LCN-TAM preparation up to 60 mg/100 ml maintained the positive zeta potential value of about +45 mV. A statistically significant decrease in particle size was observed for TAM amounts between 5 and 20mg. A strong influence of loaded tamoxifen on the structure of lecithin/chitosan nanoparticles was observed, supported by the quantification of free chitosan and morphological analysis. A loading of tamoxifen in nanoparticles of around 19% was obtained. The release of the drug from the LCN-TAM colloidal dispersion was measured, showing that tamoxifen citrate was released very slowly in simulated gastro-intestinal fluids without enzymes. When enzymes able to dismantle the nanoparticle structure were added to the dissolution medium, drug release was triggered and continued in a prolonged manner. Tamoxifen-loaded nanoparticles showed cytotoxicity towards MCF-7 cells comparable to that obtained with tamoxifen citrate solution, but the rate of this toxic effect was dependent on drug release. Caco-2 cells, used as a model of the intestinal epithelium, were shown to take up the TAM loaded nanoparticles extensively.<br /> (Copyright © 2013 Elsevier B.V. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemistry
Biological Transport
Caco-2 Cells
Cell Survival drug effects
Gastric Juice chemistry
Humans
Intestinal Secretions chemistry
Lipase chemistry
MCF-7 Cells
Muramidase chemistry
Nanoparticles chemistry
Nanoparticles ultrastructure
Pancreatin chemistry
Progesterone chemistry
Tamoxifen chemistry
Antineoplastic Agents administration & dosage
Chitosan chemistry
Drug Delivery Systems
Lecithins chemistry
Nanoparticles administration & dosage
Tamoxifen administration & dosage
Subjects
Details
- Language :
- English
- ISSN :
- 1873-4995
- Volume :
- 167
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Journal of controlled release : official journal of the Controlled Release Society
- Publication Type :
- Academic Journal
- Accession number :
- 23428841
- Full Text :
- https://doi.org/10.1016/j.jconrel.2013.02.009