Journal
JOURNAL OF DRUG TARGETING
Volume 24, Issue 1, Pages 68-79Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/1061186X.2015.1055572
Keywords
Docking study; doxorubicin; glucose transporter proteins; niosomes; N-lauryl glucosamine
Categories
Funding
- UGC
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Background: Efficacy of an anticancer drug is challenged by severe adverse effects persuaded by the drug itself; hence designing a tumour targeted delivery system is chosen as an objective of this research work.Purpose: We propose, glucose transporter targeting ligand, i.e. synthesised N-lauryl glucosamine (NLG) anchored doxorubicin (DOX) in niosomal formulation.Methods: Synthesised NLG was incorporated into niosomal formulation of DOX using Span 60 as surfactant, cholesterol as membrane stabilizer and dicetyl phosphate (DCP) as stabilizer.Results: The formulation was stable with particle size of 1105nm, zeta potential -30 +/- 5mV and entrapment efficiency approximately 95%. DSC and XRD pattern of freeze-dried formulation demonstrated encapsulation of DOX in niosomal formulation. Cytotoxicity of targeted niosomal formulation (IC50=0.830ppm) was higher than non-targeted niosomal formulation (IC50=1.369ppm) against B6F10 melanoma cell lines. In vitro cellular internalization revealed that targeted niosomal formulation was internalised more efficiently with higher cellular retention by cancer cells compared to the non-targeted niosomal formulation and free DOX. In vitro receptor binding and docking study of targeted niosomal formulation had shown the comparative association potential with glucose receptor.Conclusion: NLG anchored niosomal formulation of DOX with enhanced cytotoxicity, internalization and receptor binding potential has implication in targeted cancer therapy.
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