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"LIPOSOMAL COMPOSITION FOR THE TREATMENT OF LEISHMANIASIS AND METHOD FOR MANUFACTURING THEREOF"
专利权人:
发明人:
DR SHAILZA SINGH,MISS VINEETHA MANDLIK
申请号:
IN2190/MUM/2014
公开号:
IN2014MU02190A
申请日:
2014.07.07
申请国别(地区):
IN
年份:
2014
代理人:
摘要:
In one of the aspect of the invention, a set of novel inhibitors have been indentified for the Inositol phosphorylceramide synthase (IPCS) protein. These were entrapped in the liposome for the purpose of delivery to the targeted area. Molecular dynamics simulation of the docked complexes has revealed the binding modes of the compounds with the Inositol phosphorylceramide synthase (IPCS) protein. These of selected by in-silico approaches have been studied for their efficacy and cytotoxicity in-vitro, these inhibitors includes C1:(3-(l,3-Benzodioxol-5-yl)-2oxo-2H-chromen-6-yl-acetate) C2: (6-Amino-3-(l,3-benzodioxol-5-yl)-2H-chromen-2-one) C3:3-(l,3-Benzodioxol-5-yl)-6-{[(lE)-2-furylmethylenelamino}-2H-chromen-2-one C4:3-(l3-Benzodioxol-5-yl)-6-{[(lE)-lH-pyrrol-2-ylmethylene]amino}-2H-chromene-2-one C5: (3-(l,3-Benzodioxol-5-yl)-6-nitro-2H-chromen-2-one In one the most important aspect of the invention an inhibitor for control Inositol phosphorylceramide synthase (IPCS) is selected is C2: (6-Amino-3-(l,3-benzodioxol-5-yl)-2H-chromen-2-one) In an another important aspect of the invention it is provided that the inhibitor for the Inositol phosphorylceramide synthase (IPCS) is selected is C2: (6-Amino-3-(l,3-benzodioxol-5-yl)-2H-chromen-2-one) as a free drug. Liposomal formulation of C2 was prepared to improve the efficacy, the liposomal formulation is provided. In an another aspect of the invention, a method for manufacturing the liposomal formulation is provided which is manufactured as follows: Phospholipid, drug and phospholipid derivative were dissolved solvent. Solvent was evaporated into a thin and uniform lipid-drug film with the help of a rotary evaporator. After thorough drying with vacuum pump lipid-drug, film was hydrated with H20 for 2 h elevated temperature. It was passed though Sephadex G-25 column and extruded through 200 nm Whatmann polycarbonate membrane at elevated temperature to obtain sub 200 nm particles. Liposomes were stored at 4oC for further use
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