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利福平纳米脂质载体的制备及质量评价
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| 篇名： | 利福平纳米脂质载体的制备及质量评价 |
| TITLE： | |
| 摘要： | 目的：制备利福平（RFP）纳米脂质载体（RFP-NLCs），提高其水溶性，并评价其质量。方法：以液固脂质材料油酸及单硬脂酸甘油酯为脂质材料，大豆卵磷脂为乳化剂，泊洛沙姆188为非离子型表面活性剂，采用熔融-超声乳化法制备RFP-NLCs。以粒径和包封率的综合评分为指标，以脂质材料的用量、液态脂质材料比例、投药量和大豆卵磷脂-泊洛沙姆188质量比为因素，采用正交试验优化处方。测定最优处方所制脂质载体的形态、粒径、多分散指数（PDI）、Zeta电位、包封率、载药量和体外释放度。结果：最优处方中脂质材料用量为150 mg，液态脂质比例为30％，RFP用量为10 mg，大豆卵磷脂-泊洛沙姆188的质量比为1 ∶ 3。所制RFP-NLCs的外观较圆整，粒径为（124.07±3.25） nm，PDI为0.104±0.010，Zeta电位为（－31.07±2.94） mV，包封率为（80.90±2.59）％，载药量为（4.81±0.68）％（n＝3）。与RFP原料药比较，RFP-NLCs体外释放度明显减缓，12 h内的累积释放度为63.2％，释药行为符合Weibull方程。结论：筛选处方可成功制备RFP-NLCs；所制RFP-NLCs粒径小、包封率较高，具有体外缓释特征。 |
| ABSTRACT： | OBJECTIVE： To prepare rifampicin （RFP） nano-structured lipid carriers （RFP-NLCs） to improve its water-solubility， and evaluate its quality. METHODS： Using liquid-solid lipid materials oleate and glyceryl monostearate as lipid materials， soy lecithin as emulsifier， poloxamer 188 as nonionic surfactant， melting-ultrasonic emulsification was used to prepare RFP-NLCs. Using the comprehensive scores of particle size and encapsulation efficiency as indexes， the amount of lipid materials， proportion of liquid lipid materials， dosage， and mass ratio of soy lecithin-poloxamer 188 as factors， orthogonal test was adopted to optimize the formulation. The morphology， particle size， polydispersity index （PDI）， Zeta potential， encapsulation efficiency， drug loading and in vitro release degree of prepared lipid carriers with optimal formulation were evaluated. RESULTS： In the optimal formulation， the amount of lipid materials was 150 mg， proportion of liquid lipid materials was 30％， amount of RFP was 10 mg， and mass ratio of soy lecithin-poloxamer 188 was 1 ∶ 3. Prepared RFP-NLCs had rounded appearance， particle size was （124.07±3.25） nm， PDI was 0.104±0.010， Zeta potential was （－31.07±2.94） mV， encapsulation efficiency was （80.90±2.59）％， and drug loading was （4.81±0.68）％ （n＝3）. Compared with RFP raw materials， in vitro release degree of RFP-NLCs significantly slowed down， and the cumulative release degree within 12 h was 63.2％， which was in line with Weibull equation. CONCLUSIONS： Screened formulation can successfully prepare RFP-NLCs； the prepared RFP-NLCs have small particle size and high encapsulation efficiency， and the in vitro drug release shows certain sustained-release characteristics. |
| 期刊： | 2017年第28卷第34期 |
| 作者： | 胡建军，余莉，陈海林，林薇，金海英 |
| AUTHORS： | HU Jianjun，YU Li，CHEN Hailin，LIN Wei，JIN Haiying |
| 关键字： | 利福平；纳米脂质载体；制备；质量评价 |
| KEYWORDS： | Rifampicin； Nano-structured lipid carriers； Preparation； Quality evaluation |
| 阅读数： | 402 次 |
| 本月下载数： | 8 次 |
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