Scopus Journal Metrics

CiteScore (2016): 2.10

SNIP (2016): 1.075

SJR (2016): 0.61

Platinum Open Access

(no processing or publication fees)

Adv Pharm Bull. 2016;6(3):367-375.
doi: 10.15171/apb.2016.048
PMID: 27766220
PMCID: PMC5071799
Scopus id: 84995676495
  Abstract View: 408
  PDF Download: 257

Research Article

Enhanced in Vitro Anti-Tumor Activity of 5-Azacytidine by Entrapment into Solid Lipid Nanoparticles

Farhad Jahanfar 1,2, Akbar Hasani 2, Dariush Shanebandi 3, Mohammad Rahmati 2, Hamed Hamishehkar 4 *

1 Biotechnology Research Center and Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran.
2 Department of Biochemistry and Clinical Laboratories, Faculty of Medicine, Tabriz University of Medical Sciences, Tabriz, Iran.
3 Immunology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
4 Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.


Purpose:In this study the effectiveness of encapsulating of 5-azacytidine into the lipid nanoparticles was investigated and in vitroeffect of encapsulated 5-azacytidine studied on MCF-7 cell lines

Methods:5-azacytidine -loaded solid lipid nanoparticles were produced by double emulsification (w/o/w) method by using stearic acid as lipid matrix, soy lecithin and poloxamer 407 as surfactant and co-surfactant respectively. Particle size, zeta potential, surface morphology, entrapment efficiency and kinetic of drug release were studied. In vitroeffect of 5-azacytidine on MCF-7 cell line studied by MTT assay, DAPI staining, Rhodamine B relative uptake, and also Real time RT-PCR was performed for studying difference effect of free and encapsulated drug on expression ofRARß2 gene.

Results:The formulation F5 with 55.84±0.46 % of entrapment efficiency shows zero order kinetic of drug release and selected for in vitro studies; the cytotoxicity of free drug and encapsulated drug in 48 h of incubation have significant difference. DAPI staining shows morphology of apoptotic nucleus in both free and encapsulated drug, Rhodamine B labeled SLNs show time dependency and accumulation of SLNs in cytoplasm. Real time qRT-PCR doesn’t show any significant difference (p>0.05) in expression of RARß2 gene in both cells treated with free or encapsulated drug.

Conclusion:The results of the present study indicated that the entrapment of 5-azacytidine into SLNs enhanced its cytotoxicity performance and may pave a way for the future design of a desired dosage form for 5-azacytidine.

First name
Last name
Email address
Security code

Submitted: 12 Feb 2016
Revised: 25 Apr 2016
Accepted: 27 Apr 2016
First published online: 25 Sep 2016
EndNote EndNote

(Enw Format - Win & Mac)

BibTeX BibTeX

(Bib Format - Win & Mac)

Bookends Bookends

(Ris Format - Mac only)

EasyBib EasyBib

(Ris Format - Win & Mac)

Medlars Medlars

(Txt Format - Win & Mac)

Mendeley Web Mendeley Web
Mendeley Mendeley

(Ris Format - Win & Mac)

Papers Papers

(Ris Format - Win & Mac)

ProCite ProCite

(Ris Format - Win & Mac)

Reference Manager Reference Manager

(Ris Format - Win only)

Refworks Refworks

(Refworks Format - Win & Mac)

Zotero Zotero

(Ris Format - FireFox Plugin)