FORMULATION AND EVALUATION OF PARENTERAL METHOTREXATE NANOLIPOSOMES
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2014, Vol 6, Issue 11
Abstract
Objective: The objective of the present study was to encapsulate Methotrexate in liposomal formulation for treatment of cancer. Conventional compositions of Methotrexate are available but in high doses showvariation in bioavailability and they are associated with a number of toxicities when administered orally. To overcome these problems, in the present study, inclusion of Methotrexate in parenteral liposomal formulation was approached with the aim of increasing retention time at the site of action which leads to improvement in bioavailabilityand better tumor targeting.Methods: In this study, PEGylated Methotrexate liposomes containing Hydrogenated Soy Phosphatidyl Choline and Cholesterol were prepared by thin film hydration method. The main advantage of PEGylated lipid vesicles lies in the possibility of active-targeted delivery of drugs to the tissues or organs that need those most. Attempts were made to enhance the encapsulation by use of non-ionic surfactants such as Tween-80, Tween-20 and solubilityenhancers such as β-cyclodextrin. The characterization of formulated liposomes was carried out by vesicle size, zeta potential, %free drug and in-vitro dissolution.Results: Formulation containing 10mg/ml of Tween-20 and 20 mg/ml of β-cyclodextrin showed highest encapsulation efficiency. The optimized formulation has exhibited more than 90% release of the drug within a period of 4 days. The accelerated stability studies (40±2°C/ 75±5% RH) of the Methotrexate liposome were conducted for a period of three months and the formulation was found to be stable.Conclusion: These results suggest that the liposome encapsulated MTX may serve as a useful targeted drug delivery system for effective management of neoplastic diseases.Â
Authors and Affiliations
Shabnam -, Prathima Srinivas, D S Ravindra Babu
Keywords
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