Résumé
Objective: To prepare baicalin-loaded TPGS nanomicells (BCN-TPGS-PMs) and to evaluate its physicochemical properties, in vitro release behavior, and antitumor activity against MCF-7 cells. Methods: BCN-TPGS-PMs were prepared by film-thin hydration method. The preparation methods and formulations were optimized and screened based on particle size and encapsulation efficiency (EE) of micelles. The transmission electron microscope (TEM) was used to observe the particle appearance, zetasizer instrument was used to detect the diameter and Zeta potential, and ultracentrifugation was utilized to determine the EE and drug-loading rate. Dynamic dialysis method was used to study the in vitro release behavior of BCN-TPGS-PMs, and the antitumor activity against MCF-7 cells was determined by MTT method. Results: The optimal BCN-TPGS-PMs were round with the nanometric size of (11.91 ± 0.14) nm, high EE rate of (95.83 ± 7.34)%, and drug-loading rate of (5.42 ± 0.04)%. The in vitro release behavior showed that BCN-TPGS-PMs had a slow release. Compared with free BCN, BCN-TPGS-PMs showed stronger cytotoxicity and inhibition against MCF-7 cells (P < 0.05). Conclusion: The prepared BCN-TPGS-PMs have small particle size, high drug-loading rate, and good stability, and could obviously increase the in vitro inhibitory effect of BCN.
Résumé
With polyethylene glycol vitamin E succinate (TPGS) as the carrier materials, and berberine hydrochloride ( BER) as model drug, we formed berberine hydrochloride (BER) -loaded TPGS nanomicells (BER-PMs) using filming-rehydration method to improve its solubility and in vitro anti-tumor effect. The transmission electron microscope (TEM) was used to observe the particle appearance; particle detector was used to detect the diameter and Zeta potential; and ultracentrifugation was utilized to determine the encapsulation efficiency (EE) and drug-loading (DD); dynamic dialysis method was used to study the in vitro release behavior of BER-PMs, and the anti-tumor activity against MCF-7 cells was determined by MTT method. Results showed that the average particle size of BER-PMs was (12.45 ± 1.46) nm; particle size was uniform and spherical; drug loading and encapsulation efficiency were (5.7 ± 0.22)% and (95.67 ± 5.35)%, respectively. Zeta potential was (-1.12 ± 0.23) mV; release rate within 24 h was 37.20% and 41.14% respectively in pH 7.4 and pH 6.5 phosphate buffer in vitro; compared with BER, BER-PMs can significantly inhibit MCF-7 cell proliferation (P < 0.05), promote cell apoptosis and improve the anti-tumor activity of BER in vitro. Therefore, the formed berberine hydrochloride micelle can more effectively promote the apoptosis of MCF-7 cell, and improve the drug's in vitro anti-tumor effect.