[關(guān)鍵詞]
[摘要]
目的 制備具有較高包封率和載藥量且體外放置穩(wěn)定的莫西沙星脂質(zhì)體。方法 采用硫酸銨梯度法制備包載莫西沙星的脂質(zhì)體,以粒徑及其分布和包封率、載藥量為指標(biāo)對(duì)處方和工藝進(jìn)行優(yōu)化。結(jié)果 最佳制備條件為:空白脂質(zhì)體中硫酸銨質(zhì)量濃度70 mg/mL、磷脂質(zhì)量濃度50 mg/mL、脂質(zhì)體粒徑120 nm左右、透析時(shí)間5 h、載藥時(shí)藥脂比2∶3、孵育溫度40 ℃、孵育時(shí)間30 min。制備得到的莫西沙星脂質(zhì)體粒徑為(143.00±3.98)nm,包封率為(74.56±3.21)%,載藥量為(26.39±1.88)%。結(jié)論 硫酸銨梯度法制備的莫西沙星脂質(zhì)體包封率較高,粒徑均一,室溫放置穩(wěn)定性良好。
[Key word]
[Abstract]
Objective To prepare the moxifloxacin liposomes with high entrapment efficiency, drug loading capacity, and storage stability. Methods Ammonium sulfate gradient method was used to prepare moxifloxacin liposomes; the formulation and preparation process was optimized using the particle diameter, size distribution, entrapment efficiency, and drug loading capacity of the resultant liposomes as the evaluating indicators. Results The optimal preparation conditions included 70 mg/mL ammonium sulfate, 50 mg/mL HSPC, dialysis time of 5 h, and 120 nm in diameter for the resultant blank liposomes; the drug-lipid ratio was 2∶3, and the incubation temperature was at 40 ℃ for 30 min for drug-loading. The obtained moxifloxacin liposomes were (143.00 ± 3.98) nm in diameter, achieving high entrapment efficiency of (74.56 ± 3.21)% and drug loading capacity of (26.39 ± 1.88)%. Conclusion The moxifloxacin liposomes prepared by ammonium sulfate gradient method are with high entrapment efficiency and drug loading, capacity and are stable at room temperature.
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