RESUMO
AIM: To prepare liposomes of nosiheptide and study its ability to inhibit hepatitis B virus HBsAg and HBeAg secreted. METHODS: Liposomes of nosiheptide was prepared by sodium deoxycholate dialysis and sonication. Nosheptide was determined by HPLC and partical size was determined by using laser light scattering instrument. Transmission electron microscopy (TEM) was used to examine the morphology of liposomes. Its actions to inhibit hepatitis B virus HBsAg and HBeAg secreted was studied by a HBV-transfectted cell line (HepG2 2. 2. 15 ). RESULTS: Encapsulation efficiency of liposomes by chloroform:methanol (2:1, v/v) was higher than that by dioxane. With the increase of the ratio of nosiheptide: PC (W/W), the encapsulation efficiency of liposomes decreased with the increase of ratio of sodium deoxycholate: PC, the liposomes partical size decreased. The liposomes kept stable at -20 degrees C after 2 years. The drug concentrations of liposomes that inhibit HBsAg secreted by (46.9 +/- 2. 6) %, (55.4 +/- 1.2) %, (65 +/- 3) % and HBeAg secreted by (15.1 +/- 2.3) %, (36.2 +/- 1.7) %, (36.8 +/- 2.5) % were 1.25, 2.5, 5.0 microg x mL(-1), respectively. CONCLUSION: Liposomes of nosheptide can be prepared by sodium deoxycholate dialysis and sonication, which ability to inhibit hepatitis B virus HBsAg and HBeAg secreted is better than nosheptide.