7-Ethyl-10-hydroxycamptothecin proliposomes with a novel preparation method: optimized formulation, characterization and in-vivo evaluation

Drug Development and Industrial Pharmacy
Shujun WangHuimin Yao

Abstract

The proliposomes were used to solve the stability of the ordinary liposomes. 7-ethyl-10-hydroxycamptothecin (SN-38) proliposomes for intravenous (i.v.) administration were prepared successfully by a new method. SN-38 liposomes solution was reconstituting automatically from proliposomes on contact with the acetic acid buffer solution (0.2 M, pH 2.6). The formulation was optimized by the Box-Behnken design. The physicochemical characteristics of the SN-38 proliposomes were studied by scanning electron microscopy (SEM), transmission electron microscopy (TEM), differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The stability studies were also carried on. The FLU-HPLC system was served to study the concentration of SN-38 in the plasma of Sprague Dawley (SD) rats. The optimized formulation was SN-38: 0.03 g; Soybean phospholipid (SP): 0.6 g; dextrose: 3.00 g. The entrapment efficiency of the optimized formulation was >85% and the mean particle size was about 231 nm. The stability studies showed that SN-38 proliposomes were stable in dark at 20-25°C for 6 months at least. The pharmacokinetic parameters of i.v. administration demonstrated that the half-life of SN-38 loaded in the liposomes was prolonged in vivo. The SN...Continue Reading

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Citations

Apr 11, 2013·Drug Development and Industrial Pharmacy·Mahmoud Mokhtar IbrahimMahmoud M Mahdy
Aug 10, 2013·Journal of Controlled Release : Official Journal of the Controlled Release Society·Vaskor BalaClive A Prestidge
Aug 20, 2019·European Journal of Medicinal Chemistry·Fang Chen, Gangliang Huang

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