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基于近红外光响应性的盐酸阿霉素纳米脂质体的制备工艺优化
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| 篇名： | 基于近红外光响应性的盐酸阿霉素纳米脂质体的制备工艺优化 |
| TITLE： | |
| 摘要： | 目的：建立盐酸阿霉素纳米脂质体药物含量的测定方法，并优化其制备工艺。方法：采用紫外-可见分光光度法测定盐酸阿霉素纳米脂质体的药物含量；采用薄膜分散法制备盐酸阿霉素纳米脂质体。以粒径、包封率、载药量为指标，以磷脂与药物质量比（mg/mg）、磷脂与胆固醇质量比（mg/mg）、超声时间（min）为因素，采用星点设计-响应面法优化制备工艺；采用近红外光照射考察盐酸阿霉素纳米脂质体的光热转换效应。结果：盐酸阿霉素检测质量浓度的线性范围为1.01～16.16 μg/mL（r＝0.999 7），精密度、稳定性、重复性均符合《中国药典》相关要求。最优制备工艺为磷脂与药物质量比13.30 ∶ 1（mg/mg）、磷脂与胆固醇质量比4.09 ∶ 1（mg/mg）、超声时间10 min。在此工艺条件下，所得的盐酸阿霉素纳米脂质体的粒径、载药量分别为（200.5±25.1）nm、（11.02±0.20）％，与预测值（196.3 nm、10.68％）的相对误差分别为1.82％、1.63％，实测值与预测值一致性良好。于808 nm近红外光照射下，盐酸阿霉素纳米脂质体具有浓度和时间依赖性的光热转换效应。结论：所建含量测定方法简便、准确度较好，优化所得工艺简单、可行。 |
| ABSTRACT： | OBJECTIVE： To establish a methaod for content determination of doxorubicin hydrochloride nano-liposomes， and to optimize its preparation technology. METHODS： The contents of doxorubicin hydrochloride nano-liposomes was determined by UV spectrophotometry. The membrane dispersion method was used to prepare doxorubicin hydrochloride nano-liposomes. Using particle size， encapsulation efficiency and drug-loading amount as indexes， the weight ratio of phospholipid to drug （mg/mg）， the weight ratio of phospholipid to cholesterol （mg/mg） and ultrasonic time （min） as factors， central composite design-response surface methodology was used to optimize the preparation technology. The photothermal conversion effect of doxorubicin hydrochloride nano-liposomes was investigated by near infrared irradiation. RESULTS： The linear range of doxorubicin hydrochloride were 1.01-16.16 μg/mL（r＝0.999 7）； precision， stability and reproducibility tests were all in line with the requirments of Chinese Pharmacopoeia. The optimal preparation technology included that the weight ratio of phospholipid to drug was 13.30 ∶ 1（mg/mg）； the weight ratio of phospholipid to cholesterol was 4.09 ∶ 1 （mg/mg）； the ultrasonic time was 10 min. Under this technology， the particle size and drug-loading amount of doxorubicin hydrochloride nano-liposomes were （200.5±25.1） nm and （11.02±0.20）％， relative errors of which to predicted value （196.3 nm， 10.68％） were 1.82％ and 1.63％. The consistency between measured value and predicted value was good. Doxorubicin hydrochloride nano-liposomes exhibited concentration- dependent and time-dependent photothermal conversion characteristics under near infrared irradiation at 808 nm. CONCLUSIONS： Established method is simple and good accuracy. The optimized preparation technology is simple and feasible. |
| 期刊： | 2019年第30卷第10期 |
| 作者： | 祝侠丽，王莎莎，李玲华，巴妍妍，刘黎明，贾永艳 |
| AUTHORS： | ZHU Xiali，WANG Shasha，LI Linghua，BA Yanyan，LIU Liming，JIA Yongyan |
| 关键字： | 盐酸阿霉素；纳米脂质体；近红外光响应性；星点设计-响应面法；粒径；载药量 |
| KEYWORDS： | Doxorubicin hydrochloride； Nano-liposomes； Near-infrared light response； Central composite design-response surface methodology； Particle； Drug-loading amount |
| 阅读数： | 303 次 |
| 本月下载数： | 11 次 |
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