The Preparation and In Vitro Studies of Phytantriol-Based Cubosomes Containing Oridonin / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare oridonin-loaded cubosomes, and encapsulate oridonin(ORI) for the purpose of enhancing the solubility and prolonging the action time. METHODS: Phytantriol (PYT) was firstly used to cooperate with Poloxamer 407-propylene glycol-water system to improve the solubility of ORI for developing ORI-loaded cubosomes. Polarizing microscope, small angel X-ray scattering (SAXS) and cryogenic transmission electron microscopy(cryo-TEM) were used to study the characters of cubosomes. RESULTS: Under homogenization conditions of 1 200 bar for 9 cycles, the obtained PYT-based cubosomes had narrow particle size distribution with a mean particle size of (225.9 ± 5.6) nm. The internal structures of cubosomes were revealed by small-angle X-ray scattering as a bicontinuous cubic liquid crystalline phase with Pn3m geometry. The encapsulation efficiency and drug loading determined by ultrafiltration centrifugation were (86.6 ± 1.5)% and (3.69 ± 0.06) mg•g-1, the solubility of ORI had been increased by 5.20 times. CONCLUSION: The optimized formulas of cubosomes show obvious 24 h-sustained release, and the in vitro release profiles fitt the Higuchi release model well, implying diffusion-control as main release mechanism.