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Methotrexate Liposome as Oral Drug Delivery Carriers

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Author(s): Shyamala Bhaskaran1*, C.G.Harish2, P.K.Lakshmi3,

Journal: Journal of Pharmacy Research
ISSN 0974-6943

Volume: 4;
Issue: 9;
Start page: 3237;
Date: 2011;
Original page

Keywords: Multilamellar liposomes | unilamellar liposomes | soya lecithin | di-myristoyl phosphatidyl choline | methotrexate | zeta potential.

ABSTRACT
In the present study oral liposomes were prepared using methotrexate as a model drug. Both multilamellar vesicles (MLVs) and unilamellar vesicles (ULVs) wereprepared and characterized by SEM analysis for their surface characteristics, zeta potential for surface charges and particle size analysis. MLVs were prepared usingnatural (soya bean lecithin) and synthetic (DMPC) lipids. Various ratios of phosphatidyl choline: cholesterol and drug : lipid were tried. Also positive and negativecharges were induced to the liposomes using stearyl amine and dicetyl phosphate. Dynamic in vitro drug release was carried out using phosphate buffer pH 7.4. Ashort term stability studies was conducted for 2 months at 4oC and at room temperature (25oC). ULVs were prepared from MLVs by extrusion technique. Finalformulations were prepared after lyophilizing the selected liposomes in the form of dry syrup. DMPC liposomes showed a better entrapment than soya lecithinliposomes. Both MLVs and ULVs showed uniform particle size distribution. The zeta potential was satisfactory. Drug release from liposomes was biphasic withan initial fast release within 3 hrs and then an equilibrium state attained. SEM analysis showed smooth outer surface. Thus liposomes can be prepared for oral drugdelivery for the drug methotrexate.
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