Encapsulation of berberine into liquid crystalline nanoparticles to enhance its solubility and anticancer activity in MCF7 human breast cancer cells

Abstract

Berberine, an isoquinoline alkaloid derived from Berberis vulgaris and plants of the Ranunculaceae family, elicits a broad range of pharmacological effects, including anticancer properties. However, poor solubility and low bioavailability limit its therapeutic use. In this study, we developed lyotropic liquid crystalline nanoparticles (LCNs) to enhance the solubility of berberine. LCNs were prepared by the ultrasonication method using monoolein, poloxamer 407, polyethylene glycol-400, and Transcutol® HP. The nanoparticles were characterized for size, surface charge, in vitro release, cytotoxicity, and cellular uptake. The average particle size ranged from 186 to 190 nm with cubical shape, and the polydispersity index was lower than 0.2. The zeta potential ranged between −9.3 and −21.9 mV with high drug entrapment efficiency (≥73.8%). The cell viability assay in MCF7 human breast cancer cells revealed that formulations prepared with polyethylene glycol-400 and Transcutol® HP exhibited significantly lower half-maximal inhibitory concentration compared with pure berberine. In cellular uptake assay, berberine concentration in Caco-2 cells was higher for LCNs prepared with Transcutol® HP. In conclusion, LCNs could be a potential carrier for enhancing the solubility and thus improving the anticancer effect of berberine against breast cancer.