| 引用本文: | 杜彭飞,杨蓉,易静,李红莲,任静.基于纳米结构脂质载体的白花丹醌纳米粒制备及评价[J].中国现代应用药学,2025,42(6):87-94. |
| dupengfei,yangrong,yijing,lihonglian,renjing.Preparation and Evaluation of Plumbagin Nanoparticles Based on Nanostructured Lipid Carriers[J].Chin J Mod Appl Pharm(中国现代应用药学),2025,42(6):87-94. |
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| 摘要: |
| 目的 制备甘露糖修饰的白花丹醌(Plumbagin,PLB)纳米结构脂质载体(Nanostructured lipid carriers,NLCs),对体外释药规律进行考察,并进行体外细胞毒性实验及初步药效学研究。方法 采用乙醇注入法制备白花丹醌纳米结构脂质载体(PLB-NLCs),在单因素筛选基础上结合BBD-RSM响应面法优化处方,进一步修饰后得到甘露糖基的白花丹醌纳米结构脂质载体(PLB-Man-NLCs)；采用透析法评价PLB-Man-NLCs的体外释放规律并拟合最优方程；使用NIH3T3细胞进行细胞毒性实验和抑制细胞增殖实验。结果 PLB-Man-NLCs的最优处方:药脂比为1:10,液固脂质比为1:3.85,PLB浓度为0.49 mg/mL。PLB-Man-NLCs呈现球形或类球形；粒径为(175.66±3.29)nm,Zate电位为(-42.81±2.44)mV；包封率和载药量分别为(85.89±0.75)%和(5.69±0.07)%。PLB-Man-NLCs体外释放曲线以Weibull方程拟合最佳。PLB-Man-NLCs能够降低PLB对NIH3T3细胞的毒性,抑制TGF-β1诱导的成纤维细胞增殖作用。结论 成功制备得到PLB-Man-NLCs,提高了PLB的溶解度和体外释放量,实验结果可为后期制剂开发奠定良好理论基础。 |
| 关键词: 白花丹醌 纳米结构脂质载体 BBD-RSM响应面法 体外释放 细胞毒性 |
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| 基金项目:国家药监局药物制剂体内外相关性技术研究重点实验室开放课题资助(2022-KFKT-002) |
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| Preparation and Evaluation of Plumbagin Nanoparticles Based on Nanostructured Lipid Carriers |
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dupengfei, yangrong, yijing, lihonglian, renjing
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Chengdu University School of Pharmacy
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| Abstract: |
| OBJECTIVE To prepare nanostructured lipid carriers (NLCs) of plumbagin (PLB) modified with mannose, investigate the in vitro drug release pattern, and conduct in vitro cytotoxicity experiments and preliminary pharmacological studies. METHODS PLB-NLCs were prepared using the ethanol injection method, and then mannose-modified PLB-NLCs (PLB-Man-NLCs) were obtained by combining single-factor screening with Box-Behnken design-response surface methodology (BBD-RSM). The in vitro release pattern of PLB-Man-NLCs was evaluated using dialysis method and fitted with the optimal equation. NIH3T3 cells were used forotoxicity and cell proliferation inhibition experiments. RESULTS The optimal formulation of PLB-Man-NLCs was as follows: drug-to-lip ratio of 1:10, liquid-to-solid lipid ratio of 1:3.85, and PLB concentration of 0.49/mL. PLB-Man-NLCs spherical or quasi-spherical shape with a particle size of (175.66±3.29) nm a Zeta potential of (-42.81±.44) mV. The encapsulation efficiency and drug loading were (85.89±0.)% and (5.69±0.07)%, respectively. The release curve of PLB-Man-Ns was best fitted the Weibull equation. PLB-Man-Ns reduced the toxicity of PLB to NIH3T3 cells and inhibited TGF-β1-induced fibroblast proliferation. CONCLUSION PLB-Man-NLCs were successfully prepared, which the solubility and in vitro release of PLB. The experimental results provide a solid theoretical basis for further formulation development. |
| Key words: plumbagin nanostructured lipid carriers BBD-RSM in vitro release cytotoxicity |
