RESUMO
Objective To prepare multicomponent microemulsion of Chinese materia medica (CMM) with different oil-water partition coefficients (logP values) by simplex lattice method and evaluate its quality. Methods The surfactants, cosurfactants and oil phases were screened by saturated solubility method. Ochratins, ligustrazine, ferulic acid, puerarin and geniposide were model drugs to represent the complex components of CMM. Based on the pseudo-ternary diagram, simplex lattice method was adopted to optimize the multicomponent microemulsion of CMM with different logP values by appearance, particle size and polydispersity index as evaluation indexes. The experimental design and model building were constructed by Design Expert 8.06 software to optimize the response surface data analysis and validate the optimal prescription composition. The quality of microemulsion was evaluated by observing appearance and stability as well as measuring particle size and potential. Results The optimum formulation was oleic acid-Labrasol-propylene glycol-water (5.303:29.336:7.334:58.027). The prepared microemulsion was clear in appearance with good yellowish color and stable property. The average particle size was (118.77 ± 0.37) nm, PDI was 0.282 ± 0.02 and Zeta potential was (0.346 ± 0.05) mV. Conclusion The results indicated that the multicomponent microemulsion of CMM with different logP values is optimized and the drug loading was high. The multicomponents microemulsion of CMM with different logP values (-1.01-3.85) is established and optimized, providing a feasible microemulsion carrier for the multicomponent CMM to simplify its prescription screening work.
RESUMO
Objective: To prepare Lingyi Formula multicomponent microemulsion and evaluate its anti-lung cancer activity. Methods: Lingyi Formula multicomponent microemulsion was prepared by aqueous titration method using polysaccharides solution of Ganoderma lucidum and Coix lachryma-jobi var. ma-yuen as aqueous phase and coix seed oil as oil phase, loading ganoderma triterpenes. The average particle size, Zeta potential, and stability were detected. The results of antitumor efficacy including tumor inhibitory rate, body weight change, immune organ index, and concentration of TNF-α and IL-6 were investigated. Besides, pathological section of tumor tissue and TUNEL labeling were conducted subsequently. Results: The prepared microemulsion displayed spherical surface with mean droplet size of (69.92 ± 8.43) nm, polydispersity (PDI) of 0.060 ± 0.008, and Zeta potential of (-11.30 ± 1.34) mV. Tumor inhibitory rate of microemulsion (57.25%) was significantly higher than that of suspension (45.89%), immune tissue index as well as the concentration of TNF-α and IL-6 were increased significantly. TUNEL labeling and pathological section of tumor tissue showed that the antitumor activity of microemulsion was significantly effective compared with that of suspensions. Conclusion: Lingyi Formula multicomponent microemulsion has a good anti-lung cancer activity.