[关键词]
[摘要]
为了增加人参皂苷Rg3的生物利用度,使用聚乙二醇-聚乳酸聚乙醇酸共聚物(缩写为PEG-PLGA)作为载体,通过薄膜水化法来制备Rg3-PEG-PLGA纳米胶束,并通过粒径、包封率和载药率等指标来评价其性能。本研究使用单因素试验和响应面法对Rg3纳米胶束的制备工艺进行优化,并对优化后的产品质量进行评价。结果表明,经过工艺优化,Rg3纳米胶束的载药率为2.62%,包封率为90.99%。此外,Rg3-PEG-PLGA纳米胶束在体外72小时内累计释放率达到了93.60%。其临界胶束浓度(CMC)值为3.67 μg/mL,平均粒径大小为52.16 nm,PDI值为0.09,Zeta电位为-24.37 mV,粘度约为0.89 mP·s/cp。扫描电镜(SEM)显示其形态为类球形。体外释放结果显示,Rg3纳米胶束具有较好的缓释效果。经过优化的制备工艺稳定可行,所得到的纳米胶束具有均一的粒径分布,包封率和载药率较高,并且具备缓释功能。研究证明该制备方法简便、安全,且可放大至工业生产规模。使Rg3-PEG-PLGA纳米胶束产品具有重要的实用意义。
[Key word]
[Abstract]
To enhance the bioavailability of ginsenoside Rg3, Rg3-PEG-PLGA nano-micelles were prepared using the film hydration method. Polyethylene glycol-polylactic acid polyglycolic acid copolymer (PEG-PLGA) was employed as the carrier material. The properties of the nano-micelles were evaluated based on particle size, encapsulation rate, and drug loading. Single-factor experiments and response surface methodology were utilized to optimize the preparation process of Rg3 nano-micelles, and the quality of the optimized product was assessed.The results demonstrated that after optimization, the drug loading rate of Rg3 nano-micelles reached 2.62%, and the encapsulation rate was 90.99%. In vitro studies revealed that the cumulative release rate of Rg3-PEG-PLGA nano-micelles reached 93.60% within 72 hours. The critical micelle concentration (CMC) was determined to be 3.67 μg/mL. The average particle size was measured to be 52.16 nm, with a polydispersity index (PDI) of 0.09 and a zeta potential of -24.37 mV. The viscosity was found to be approximately 0.89 mP·s/cp. Scanning electron microscopy (SEM) revealed a spheroidal morphology of the nano-micelles.The in vitro release results confirmed that the Rg3 nanoparticles exhibited a sustained release effect. The optimized preparation process was deemed stable and feasible, yielding nanoparticles with a uniform particle size distribution, high encapsulation efficiency and drug loading, and sustained release properties. The simplicity, safety, and scalability of this preparation method make it highly practical and suitable for industrial production. This makes Rg3-PEG-PLGA nano-micelles a promising and valuable product with significant practical applications.
[中图分类号]
[基金项目]
2023吉林省教育厅科学技术研究项目;吉林省科技厅项目;吉林市科技局项目;吉林省重大科技专项