The Preparation and In Vitro Studies of Phytantriol-Based Cubosomes Containing Oridonin
SHI Xuan1, PENG Ting-ting2, WU Chuan-bin2*
1. Department of Pharmacy, Hospital Affiliated with Tongji Medical College, Huazhong University of Science and Technology,Wuhan 430030, China; 2. School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China
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.
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2018, Vol. 53 
