Co-Delivery of Berberine Chloride and Tariquidar in Nanoliposomes Enhanced Intracellular Berberine Chloride in a Doxorubicin-Resistant K562 Cell Line Due to P-gp Overexpression

Abstract

The MDR phenomenon has become a major obstacle in the treatment of cancers, and among the strategies to reverse it, the inhibition of P-gp function and expression is essential to increase for effective anticancer drugs. In the present paper, the co-delivery of berberine chloride and tariquidar loaded nanoliposomes was investigated with the aim of enhancing solubility and improving desired effects for the antineoplastic drug and the P-gp inhibitor. Developed nanoliposomes were loaded with the electron-dense enzyme horseradish peroxidase, and analyzed by TEM to investigate their ability to enter in both K562 and K562/DOXO cell lines. Receptor-mediated endocytosis was evidenced for both cell lines. Nanoliposomes were loaded with tariquidar, berberine chloride, or both, maintaining chemical and physical characteristics—i.e., size, homogeneity, and encapsulation efficiency—and high suitability for parenteral administration. Tariquidar was able to reverse the MDR in the K562/DOXO cell line. Tariquidar- and berberine chloride-loaded nanoliposomes showed a significant increase of berberine chloride accumulation in tumor cells, which could be correlated with resensitization of the resistant cells to the antitumor agent. These results suggest that the co-delivery of the P-gp inhibitor, tariquidar, and the cytotoxicity inducer, berberine chloride, looks like a promising approach to overcome the MDR.

The Anti-Arthritic Efficacy of Khellin Loaded in Ascorbyl Decanoate Nanovesicles after an Intra-Articular Administration

“…The cumulant method was used with the aid of Zetasizer software version 7.02 (Malvern Panalytical Ltd., Almelo, The Netherlands). Electrophoretic light scattering (ELS), using the same apparatus and the same operating conditions as DLS, gave the ζ-potential (mV) [ 13 ]. A Henry correction to Smoluchowski’s equation was used for the calculation of the electrophoretic mobility.…”

Apoptosis Induction, a Sharp Edge of Berberine to Exert Anti-Cancer Effects, Focus on Breast, Lung, and Liver Cancer

“…Nano-co-delivery can further improve these effects. Nanoliposomes loaded with P-gp inhibitors and BBR chloride significantly increased BBR chloride content in cells ( Vanti et al, 2021 ). Nano-co-delivery of BBR and Dox using poly lactic-co-glycolic acid NPs resulted in an almost 14-fold increase in half-life and an increased plasma concentration in rats ( Khan et al, 2019 ), while BBR and zinc oxide-based NPs provided safe chemo-photothermal therapy for lung cancers ( Kim et al, 2018b ).…”

Recent strategies in nanodelivery systems for natural products: a review

“…Analysis by transmission electron microscopy also evidenced the ability of developed nanoliposomes to enter in both cell lines by receptor-mediated endocytosis, with significant increase in berberine chloride uptake by K562/DOXO cell line. Moreover, formulated tariquidar had less toxic effects (lower cell death by necrosis) than free molecule, as nanoliposomes controlled tariquidar release, with a potential benefit in clinical therapy (Vanti et al 2021b).…”