目的 制備D-α-維生素E聚乙二醇1000琥珀酸酯（TPGs）修飾的雷公藤甲素固體脂質納米粒（TPGs-Tri-SLNs），并評價其質量。方法 采用熱熔乳化-超聲法制備TPGs-Tri-SLNs，并以山崳酸甘油酯濃度（X₁），大豆磷脂與TPGs比例（X₂）和山崳酸甘油酯與藥物比例（X₃）作為考察因素，以TPGs-Tri-SLNs的粒徑分布（Y₁）和藥物包封率（Y₂）作為評價指標，通過中心復合設計-效應面法優(yōu)化TPGs-Tri-SLNs的處方，粒度分析儀測定其粒徑分布，透射電鏡觀察其微觀形態(tài)，并考察了TPGs-Tri-SLNs的體外藥物釋放特性。結果 TPGs-Tri-SLNs的最佳處方組成為：山崳酸甘油酯濃度為10%，大豆磷脂與TPGs比例4：1，山崳酸甘油酯與藥物比例為60：1，按照最優(yōu)處方制備3批TPGs-Tri-SLNs的平均粒徑為（107.8±16.9）nm，包封率為91.4%±1.1%；在透射電鏡下可以觀察到TPGs-Tri-SLNs呈球型分布，表面光滑；TPGs-Tri-SLNs在前4 h內藥物釋放較快，后期釋藥速率較為平穩(wěn)，24 h藥物釋放可以達到85%。結論 通過中心復合設計-效應面法優(yōu)化并得到TPGs-Tri-SLNs的最優(yōu)處方，處方設計合理，制備工藝簡單。

Objective To prepare D-α-vitamin E polyethylene glycol 1000 succinate (TPGs) modified triptolide solid lipid nanoparticles (TPGs-Tri-SLNs) and evaluate their quality. Methods TPGs-Tri-SLNs were prepared by hot melt emulsificationultrasonic method, and the concentration of Compritol-888 ATO (X₁), the ratio of soybean phospholipid to TPGs (X₂) and the ratio of Compritol-888 ATO to triptolide (X₃) were used as the investigation factors, the particle size distribution (Y₁) and encapsulation efficiency (Y₂) of TPGs-Tri-SLNs were used as evaluation indexes, and the formulation of TPGs-Tri-SLNs was optimized by central composite design-response surface methodology (CCD-RSM). The particle size distribution of TPGs-Tri-SLNs were determined by particle size analyzer. The microscopic morphology was observed by transmission electron microscopy, and the in vitro drug release characteristics of TPGs-Tri-SLNs were investigated. Results The optimal formulation of TPGs-Tri-SLNs as follows:Compritol-888 ATO concentration was 10%, the ratio of soybean phospholipid to TPGs was 4:1, the ratio of Compritol-888 ATO to triptolide was 60:1. Three batches of TPGs-Tri-SLNs were prepared according to the optimal formulation. The average particle size was (107.8±16.9) nm and the encapsulation efficiency was 91.4%±1.1%. Under the transmission electron microscope, TPGs-Tri-SLNs could be observed to have a spherical distribution with a smooth surface. The drug release of TPGs-Tri-SLNs showed a bursting in the first 4 h, while it was slow and stable in the later stage, and the drug release in 24 h could reach 85%. Conclusion This study used central composite design-response surface methodology optimization and obtained the optimal formulation of TPGs-Tri-SLNs. The formulation design was reasonable and the preparation process was simple, which could be further investigated.

R927.11