Econazole Liposomal Gel

The basic physical-phemical properties of Econazole Nitrate were studied and the formulation was optimized by orthogonal design. The two different entrapment efficiencies were determined by mincolumn centrifugation method and ultraceritrifugation method, which demonstrated the distribution of Econazole Nitrate in 1 ipo some. A high-performance liquid chromatographic method for the quantitative determination of Econazole nitrate in epidermis and dermis was developed. The effects of the additives on the drug release from liposomal gel and the effects of pH, liposome size, ethanol content, phospholipid sorts and the additives on the content of drug in epidermis and dermis 24 hours after application were studied, which were compared with the ointment on sale. The results showed that pH, ethanol content, phospholipid sorts and the additives had significant effects on the content of drug in epidermis and dermis and HPMCiposome gel had a higher rate of drug release and a more content of Econazole nitrate in epidermis and dermis than other liposomal gels ,furthermore, much higher than the ointment on sale The clearance procedures of Econazole nitrate in rat back skin (epidermis and dermis) 3 days after application were studied and AUC were calculated by trapezoidal rule, which were compared with the marketed Econazole nitrate ointment. The results showed that the C of Econazole nitrate from the prepared liposomal gel in epidermis and dermis 3 days after application were significantly higher than that from the ointment on sale. The ratios of AUCLP. to AUC0. in epidermis and dermis were 4.87 and 1.30 respectively, which showed that liposomal gel could prolong duration time of Econazole nitrate in epidermis but not in dermis. It demonstrated Econazole nitrate liposomal gel was adapted to fungal skin infections whose focus is in epidermis. The physical-phemical properties, stability, skin irritation and preliminary clinical pharmacological action of prepared liposomal gel were investigated. The results of polarizing microscope observation scanning microscope observation and X-way diffraction test showed a lot of crystal of Econazole nitrate in the ointment on sale ,but no crystal in prepared liposomal gel. The irritation test and preliminary clinical investigation showed the prepared liposomal gel had no irritation for application and had significant pharmacological action for fungal skin infections.