Study on paclitaxel-oleic acid and Brucea javanica oil core-matched nanoemulsions drug delivery / 中草药
Chinese Traditional and Herbal Drugs
; (24): 1544-1552, 2017.
Article
en Zh
| WPRIM
| ID: wpr-852840
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WPRO
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.
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WPRIM
Idioma:
Zh
Revista:
Chinese Traditional and Herbal Drugs
Año:
2017
Tipo del documento:
Article