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Objective To prepare berberine hydrochloride nanoemulsion, optimize its formulation composition and preparation process, and investigate its in vitro characteristics. Methods BBR-NE was prepared by water drop addition and pseudo-ternary phase diagram was drawn. The formulation of NE was optimized by central composite design-response surface methodology to choose the optimal formulation composition. The particle size, potential and appearance of the prepared BBR-NE were characterized. Results The optimal prescription of BBR-NE was determined as the oil phase Capryol 90 accounted for 32.84% of the system, the surfactant Tween-80 accounted for 33.90%, the co-surfactant 1,2-propylene glycol accounted for 16.95%, and water relative system accounted for 15.25%. The prepared NE was clear and transparent in appearance, regular in shape and uniform in size, with an average particle diameter of (68.85±8) nm, polydiseperse index of (0.245±0.03) and drug loading of 0.83 mg/g. The in vitro drug release results of NE showed that the in vitro drug release behavior was passive diffusion, which had a certain slow releasing effect and met the first-order release equation. Conclusion The BBR-NE can provide a new dosage form for the clinical use of berberine.
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Objective:To optimize the preparation technology of rutin nanoemulsion. Methods:The pseudoternary phase diagram of rutin nanoemulsion under the condition of different Kmwas drawn. With the drug loading and the particle size as the independent var-iables,and the percent of oil and the weight ratio of surfactant to cosurfactant as the dependent variables, the blank formula of rutin nanoemulsion was optimized by central composite design-response surface method. Results:The optimal formula was as follows:the ra-tio of ethyl oleate, cremopher RH40,1,2-propanediol and water was 7: 13: 5: 25. The average particle size of the prepared rutin nanoemulsion was 26.51 nm,and the drug loading was 8.97 mg·ml-1. Conclusion:The central composite design-response surface method can obtain a good formula of rutin nanoemulison,and the model has a good predictive function.
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Objective To optimize a W/O microemulsion formulation of troxerutin and evaluate its physical properties such as morphology, droplet size, stability and content of troxerutin. Methods The W/O microemulsion was optimized using a pseudoternary phase diagram and the area of the microemulsion region was used to screen and determine microemulsion components.HPLC assay was used for determination of the loading content. Results The optimal formulation contained lecithin, ethanol, isopropyl myristate and water (23.30:11.67:52.45:12.59).The microemulsion was physicochemically stable with round shape and uniform size, and the mean droplet size was about 50. 20 nm. Conclusion Microemulsion was developed successfully.It will expect to be the new preparation for troxerutin.
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Objective: The objectives of this study were to identify stable anhydrous emulsions via pseudo ternary phase diagram, optimize artemether-loaded batches using factorial design and subsequently evaluate the antimalarial activity. Methodology: Using labrasol®, triacetin® and lauroglycol 90® as the surfactant, oil and co-surfactant respectively, pseudo ternary phase diagram was generated from the quantitative titration of water with the anhydrous emulsion. Stable combinations from the phase diagram were subjected to a 23 full factorial experimental design. The 22 softwaregenerated formulations were experimentally formulated and characterized for droplet size, polydispersity index, viscosity and thermodynamic stability. Droplet size was chosen and subsequently fitted into the Response column of the software, thus prompting the generation of graphs and Desirability table of 125 predicted formulations. Out of the 125 predictions, three with the least droplet sizes (less than 100 nm) were adjudged as optimized batches. Subsequently, they were formulated, converted to powder by adsorption on magnesium aluminum metasilicate and evaluated. Antimalarial effectiveness of the drug-loaded formulation was also investigated. Results: Triacetin® most significantly (P<0.05) contributed to droplet size variation. The droplet size of the experimental formulations approximated that of the statistical predictions. The anhydrous emulsions (AEs) were powderable and the granulations rated fair and passable according to Carr’s scale. Artemether-loaded anhydrous emulsion (AE) demonstrated highest antimalarial activity. Conclusion: We therefore conclude that optimization proved a useful tool for the identification of excipient proportions with optimal effects.
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Objective: To develop the matrine self-microemulsifying drug delivery system (SMEDDS) and evaluate its quality. Methods: The solubility test and pseudoternary phase diagram were utilized to select proper matrine microemulsions prescription. On this basis, matrine-SMEDDS was formulated and HPLC method was used to determine the drug content in matrine-SMEDDS; The appearance, morphology, particle size, particle size distribution, Zeta potential, drug loading, and stability of matrine in the liposome were studied. Results: The best prescription of matrine-SMEDDS was matrine-oleic-ethyloleate-EL-40-isopropanol (0.5:0.15:0.15:0.35:0.35). The selected matrine-SMEDDS was transparent liquid with good liquidity and stability and could form O/W type microemulsion with water, with an average particle size of (68.00 ± 0.07) nm (n = 3). The average drug loading was 42.689 mg/mL (n = 3). Conclusion: The preparation technology is simple and stable, and provides a strong foundation for research of matrine-SMEDDS.