OBJECTIVE To prepare liposomes encapsulating puerarin-hydroxypropropyl-β-cyclodextrin complexes,and screen the optimal formulation,and study its pharmaceutical characteristics in vitro.METHODS Phase solubility studies at pH values and physiologically acceptable HP-β-CD-concentrations were performed,and solubilized puerarin was quantified by HPLC.The puerarin-cyclodextrin indusion compound was prepared with lyophilization technique.The inclusion compound was identified by X-ray diffraction(XRD) and differential scanning calorimetry(DSC) methods and in vitro dissolution test.The liposomes encapsulating puerarin-cyclodextrin complexes were prepared by thin film method with freeze-thawing steps.Unloaded puerarin were separated by dialyzation.HPLC method was used to determine the encapsulation efficiency of liposomes encapsulating puerarin-cyclodextrin complexes.According to the entrapment efficiency,an optimal technique was chosen with orthogonal design.The shape,particle size and Zeta-potential of the liposomes were investigated with transmission electron microscope and laser scatter.The release of puerarin from liposomes was studied in vitro.RESULTS The prepared liposomes demonstrated good stability and encapsulation efficiency was(68.10+0.7)%(n=3).The average size was 395.7 nm and the Zeta potential of the modified liposomes was-34.04 mV.The release in vitro was characterized by Higuchi equation.:Q=12.711t1/2+7.090(r=0.983).CONCLUSION Thin film method with freeze-thawing steps could increase the entrapment efficiency of liposomes encapsulating puerarin-cyclodextrin complexes and the stability of liposomes in plasma.The in vitro release profile studies showed that the liposomes entrapment of inclusion complexes displayed slower release rate.
SONG Jin-chun;CHEN Ji-li;HUNG Ling.
Preparation of Liposomes Encapsulating Puerarin-Cyclodextrin Complexes and Its Pharmaceutical Characteristics in Vitro[J]. Chinese Pharmaceutical Journal, 2008, 43(23): 1792-1797
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