Niosomal entrapment of hydroxypropyl-β-cylodextrin-methotrexate complex as a drug delivery device

An inclusion complex of methotrexate with hydroxypropyl-β-cylodextrin (HPβCyD) was prepared with a view to increase entrapment efficiency and thereby improve the anticancer activity and stability of the drug. The complex and the plain drug were entrapped in the niosomes using cholesterol, Span 60 and dicetyl phosphate. The niosomal entrapment efficiency was higher (89%) in the case of the drug-complex than with the plain drug (67%). When administered to tumour-bearing BALB/c mice at a dose of 5 mg kg^-1, the complex entrapped in the niosomes produced a higher percentage increase in life span. Better stability on storage was also observed with the niosome-entrapped complex. Thus complexation of methotrexate with HPβCyD increases the efficiency of entrapment in nonionic surfactant vesicles and the entrapped complex is stable and has improved anticancer activity.