Exploring the mechanism through which berberine (Ber) reverses the multidrug resistance (MDR) of breast cancer is of great importance. Herein, we used the methyl thiazolyl tetrazolium assay to determine the drug resistance and cytotoxicity of Ber and doxorubicin (DOX) alone or in combination on the breast cancer cell line MCF-7/DOX Fluc . The results showed that Ber could synergistically enhance the inhibitory effect of DOX on tumor cell proliferation in vitro , and the optimal combination ratio was Ber/DOX = 2:1. Using a luciferase reporter assay system combined with the bioluminescence imaging technology, the efflux kinetics of d -luciferin potassium salt in MCF-7/DOX Fluc cells treated with Ber in vivo was investigated. The results showed that Ber could significantly reduce the efflux of d -luciferin potassium salt in MCF-7/DOX Fluc cells. In addition, western blot and immunohistochemistry experiments showed that the expression of P-glycoprotein (P-gp/ABCB1) and multidrug resistance protein 1 (MRP1/ABCC1) in MCF-7/DOX Fluc cells was downregulated upon Ber treatment. Finally, high-performance liquid chromatography was used to investigate the effect of Ber on DOX tissue distribution in vivo , and the results showed that the uptake of DOX in tumor tissues increased significantly when combined with Ber ( P < 0.05). Thus, the results illustrated that Ber can reverse MDR by inhibiting the efflux function of ATP-binding cassette transporters and downregulating their expression levels.

: Chemometrics is an important emerging discipline with unique charm formed by the intersection of mathematics, statistics, chemistry and computer science. The application of chemometrics in the field of pharmacy has injected fresh blood into the scientific research and clinical practice of medicine, and has provided sufficient scientific basis for drug analysis and content determination to solve the problem of cancer treatment with combined therapy in different ranges. This paper introduces the basic principles, advantages and disadvantages of several commonly used pattern recognition and multidimensional correction methods of chemometrics, reviews the application of chemometrics for efficiency enhancement and toxicity reduction in cancer treatment with combined therapy, and summarizes its development and prospects in the future.

Objective: To improve solubility of Honokiol (HNK), Honokiol nanoparticles (HNK-NPs) were prepared by using a new biodegradable polysaccharide polymer as its carrier. Methods: HNK-NPs were prepared by hydrophilic polymer coagulation method, and the processing parameters were optimized according to average particle size and PDI by single factor experiment. The morphology of the optimized nanoparticles was investigated by TEM and the in vitro release was carried out to evaluate the optimized HNK-NPs. Results: The encapsulation efficiency and drug loading of the HNK-NPs were 77.75 ± 2.63% and 13.46 ± 0.39%. The obtained nanoparticles of HNK-NPs were spherical-like under the electron microscope with a mean particle size of 198.50 ± 0.01 nm and Zeta potential of −52.60 ± 1.00 mV, respectively. The in vitro release results showed that the cumulative release rates of nanoparticles were 48.28 ± 9.80% and 81.12 ± 4.35% within 2 h and 8 h, respectively which showed a stable release behavior. The average particle size and PDI of HNK-NPs solution prepared by hydrophilic polymer condensation method had no obvious change at 72h. Conclusion: HNK-NPs were successfully prepared by phase separation method. This new polysaccharide polymer should be an ideal carrier to help improving the solubility of HNK.

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