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星点设计–效应面法优化眼局部应用雷公藤红素纳米结构脂质载体处方
Preparation and Formulation Optimization of Loaded Celastrol Nanostructure Lipid Carriers for Topical Ocular Application

DOI: 10.12677/HJO.2019.84025, PP. 160-168

Keywords: 雷公藤红素，纳米结构脂质载体，星点设计-效应面法，粒径，包封率，载药量，微乳法
Celastrol, Nano-Structure Lipid Carrier, Central Composite Design-Response Surface Methodology, Encapsulation Rate, Drug Loading Rate

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Abstract:

目的：采用星点设计–效应面法(CCD-RSM)优化应用于眼局部应用雷公藤红素纳米结构脂质载体(CEL-NLC)处方。方法: 通过测定雷公藤红素在各种脂质的溶解度，筛选出溶解度较好的脂质，采用微乳法制备CEL-NLC，分别以药物/脂质用量比(X1)、表面活性剂/助表面活性剂用量比(X2)为考察对象，以粒径(Y1)、包封率(Y2)和载药量(Y3)为考察指标，经效应面法预测最佳处方，并验证最佳处方。结果：根据CCD-RSM优化得出最佳处方为雷公藤红素40 mg，棕榈酸0.09 g，油酸0.18 g，吐温-80 4.34 g，甘油2.16 g。按最优处方制备的CEL-NLC包封率为(75.28 ± 3.44)%，载药量为(0.45 ± 0.02)%；粒径为(18.66 ± 2.63) nm，多分散指数(PDI)为0.39 ± 0.03。实际值与预测值偏差均小于5%。结论：采用CCD-RSM优化的CEL-NLC处方，包封率高，粒径小，稳定性好，方法可靠，可进一步用于眼局部应用雷公藤红素的后续研究。
Objective: The central composite design-response surface methodology (CCD-RSM) was used to optimize the application of tricorne nanostructured lipid carrier (CEL-NLC) in the local application of eyes. Methods: The lipid with the best solubility was screened out by determining the solubility of celastrol in different lipids. CEL-NLC was prepared by microemulsion technique. Quality of solid lipid (X1), quality of liquid lipid (X2), surfactant/cosurfactant (X3) as objects of investigation, while particle size (Y1), encapsulation efficiency (Y2) and drug loadings rate (Y3) as dependent variables, the optimal prescription was obtained by CCD-RSM and verified subsequently. Results: The best prescription of CEL-NLC was Celastrol 0.04 g, palmitic acid 0.09 g, oleic acid 0.18g, tween-80 4.34 g and Glycerine 2.16 g. The encapsulation efficiency was (75.28 ± 3.44)%; the drug loading rate was (0.45 ± 0.02)%; the particle size was (18.66 ± 2.63) nm. The PDI was 0.39 ± 0.03. The deviation between the measured and predicted values was less than 5%. Conclusion: The optimized CEL-NLC obtained by CCD-RSM has high encapsulation efficiency, small particle size and good stability, which can be further used in the follow-up study of local application of Celastrol in eyes.

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