目的 評價硫酸長春新堿脂質(zhì)體的質(zhì)量。方法 采用pH梯度法制備硫酸長春新堿脂質(zhì)體。透射電鏡觀察脂質(zhì)體的外觀形態(tài), 陽離子交換樹脂柱法測定包封率, 并考察其pH值、粒徑、Zeta電位、穩(wěn)定性及體外釋放規(guī)律。結(jié)果 形態(tài)學(xué)觀察結(jié)果顯示, 脂質(zhì)體均勻圓整度良好。硫酸長春新堿脂質(zhì)體粒徑為120 nm左右, Zeta電位約為10 mV, 包封率均在90%以上。光照、4 ℃、18 ℃、25 ℃條件下, 脂質(zhì)體各項指標(biāo)無顯著變化。40 ℃條件下, 包封率明顯降低。結(jié)論 本法準(zhǔn)確, 操作簡便, 可用于硫酸長春新堿脂質(zhì)體的質(zhì)量評價。

Objective To evaluate the quality of Vincristine Sulphate Liposome. Methods Vincristine sulphate was encapsulated in the liposomes using the pH gradient-dependent remote loading technique. The morphological examination of liposomes was observed with transmission electron microscopy. The encapsulation efficiency was determined by cation exchange resin column. Their pH value, particle size, Zeta potential, stability, and in vitro delivery of vincristine sulphate were investigated. Results The morphology of Vincristine Sulphate Liposome showed that liposomes were uniformity, good roundness. The particle size of the liposomes was about 120 nm, the Zeta potential was about 10 mV, and the encapsulation efficiency was above 90%. Vincristine sulphate liposomes did not occur significant changes under the light condition and at 4 ℃, 18 ℃, and 25 ℃ conditions. At 40 ℃, the encapsulation efficiency decreased. Conclusion The method is accurate and simple to evaluate the quality of Vincristine Sulphate Liposomes.

國家重大新藥創(chuàng)制項目(2014ZX09507005-001)