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.
Pharmacology group of the Institute of Academy of Medical Sciences in Henan Province, Chemistry and research group of Medical College in Henan Province, Laboratory of phytochemistry, Institute of Botany Institute in Yunnan province, etc. The study of chemical and pharmacological effects of oridonin [J]. Chin Tradit Herb Drugs(�в�ҩ), 1977, 2 (10):5-7.
[2]
Pharmacology group of the Institute of Academy of Medical Sciences in Henan Province, Chemistry and research group of Medical College in Henan Province, Laboratory of phytochemistry, Institute of Botany Institute in Yunnan province, etc. A new kind of antitumor substances rubescensin [J]. Chin Sci Bull(��ѧͨ��), 1978, 23 (1):53-56.
[3]
YANG R, HUANG X, DOU J, et al. Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid:design and evaluation[J]. Int J Nanomed, 2013, 8:2917-2926.
[4]
JI C R, FENG W S, HU R Z, et al. Determination of oridonin in Rabdosia rubescens terpenoids buccal tablets by HPLC[J]. Chin J Mod Appl Pharm(�й��ִ�Ӧ��ҩѧ), 1999, 16(5):35-36.
[5]
LI M R, LU Y H,ZHOU M, et al. Determination of oridonin in Rabdosia rubescens syrup by RP-HPLC[J]. China J Chin Mater Med(�й���ҩ��־),2001, 26(11):786-787.
[6]
DIAN L, YANG Z, LI F, et al. Cubic phase nanoparticles for sustained release of ibuprofen:formulation, characterization, and enhanced biovailability study[J]. Int J Nanomed, 2013,8:845-854.
[7]
NAI J, WU W, CHEN Y P, et al. Preparation of cyclosporin A cubic crystal nanoparticles and determination of encapsulation efficiency [J]. West China J Pharm Sci(����ҩѧ��־), 2009,24(6):579-582.
[8]
YANG Z W, PENG X S, TAN Y H, et al. Optimization of the preparation process for an oral phytantriol-based amphotericin B cubosomes [J]. J Nanomater, 2011,10(7):1155-1164.