Study on paclitaxel-oleic acid and Brucea javanica oil core-matched nanoemulsions drug delivery / 中草药

ABSTRACT

Objective: To optimize the preparation method of paclitaxel-oleic acid (PTX-OA)/Brucea javanica oil (BJO) core- matched nanoemulsions (CMNEs). Methods: PTX-OA/BJO was synthesized by esterification of PTX and OA, and determined by HPLC. Ultrasionic emulsification was used to prepare the PTX-OA/BJO CMNEs. The concentration of oil phase (A), quality of polysorbate 80 (B), and ultrasonic power (C) were selected as the significant factors after single-factor experiments and applied in L16(43) orthogonal array design with the average particle size as criterion. In addition, the physicochemical properties and cytotoxicity of PTX-OA/BJO CMNEs were tested. Results: Linear range of PTX-OA was 5-25 μg/mL, Y = 12.709 X + 6.252 0, r = 0.999 5. The optimized conditions of PTX-OA/BJO CMNEs were as follows The concentration of oil phase was 6.50 mg/mL, the mass ratio of polysorbate 80 to oil phase was 3.5 6.5 and the ultrasonic power was 120 W. The CMNEs prepared by the optimal conditions showed an entrapment efficiency of (100.6 ± 1.9)% and the nanoscale particle size was (108.7 ± 2.3) nm, PDI was 0.232 ± 0.038. The morphology of CMNEs examined by TEM exhibited a uniform and spherical shape. In vitro drug release was up to 67% after 48 h. After PTX-OA/BJO CMNEs sealed in a bottle were stored at 4 ℃ for 60 h, the average particle size and entrapment efficiency had no significant change. The cytotoxicity in vitro showed that the combined PTX-OA/BJO CMNEs could obviously inhibit the proliferation of HepG-2 cells. Conclusion: The current study demonstrates the feasibility of incorporating PTX-OA and BJO into a single CMNEs for the synergism in cancer therapy. Furthermore, the preparation of PTX-OA/BJO CMNEs has the advantages of practicability and simple operation, as well lays the foundation for the further mechanism research of the combined paclitaxel and BJO in oncotherapy.