1. Anhui University of Chinese Medicine, Hefei 230012, China; 2. Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei 230012, China; 3. Engineering Technology Research Center of Modernized Pharmaceutics, Education Office of Anhui Province, Hefei 230012, China
Abstract��OBJECTIVE To prepare and characterize triptolide cubic liquidcrystal,study the rheological properties and in vitro transdermal properties. METHODS Cubic liquid crystal (V2) was prepared by using phytantriol-carbitol-water three-component system. Using the ternary phase diagram method to optimize the target area. V2 was characterized by small-angle X-ray scattering, infrared spectroscopy and differential scanning calorimetry. Rheological properties of V2 was studied by a DHR-2 rheometer. In vitro drug release studies were conducted by using improved Franz diffusion cell method. RESULTS SAXS is shown as double-diamond lattice cubic liquid crystal; rheological parameters are good; DSC results show V2 can be converted into a hexagonal phase at 65.5 �� and converted into a layered liquid crystal at 90 ��, and the addition of the drug does not change the liquid crystal structure. In vitro transdermal cumulative permeation amount is about 1.54 times that of the gel, and the sustained release of triptolide can be as long as 48 h. CONCLUSION The prepared triptolide liquid crystal has good appearance and suitable rheology, and its cumulative permeation amount and infiltration rate of V2 are superior to the hydrophilic gel, which provides theoretical reference for triptolide percutaneous administration.
FAN D, GUO Q, SHEN J, et al. The effect of triptolide in rheumatoid arthritis: from basic research towards clinical translation. Int J Mol Sci, 2018, 19(2):376-392.
[2]
BAO J, DAI S M. A Chinese herb Tripterygium wilfordii Hook F in the treatment of rheumatoid arthritis: mechanism, efficacy, and safety. Rheumatol Int, 2011, 31(9):1123-1129.
[3]
ZHU X, ZHANG J, HUO R, et al. Evaluation of the efficacy and safety of different tripterygium preparations on collagen-induced arthritis in rats. J Ethnopharmacol, 2014, 158:283-290.
[4]
ZHOU Z L, YANG Y X, DING J, et al. Triptolide: structural modifications, structure-activity relationships, bioactivities, clinical development and mechanisms. Nat Prod Rep, 2012, 29(4):457-475.
[5]
LI L, JIANG Z, JING L, et al. Sex differences in subacute toxicity and hepatic microsomal metabolism of triptolide in rats. Toxicology, 2010, 271(1-2):57-63.
[6]
MARTIEL I, BAUMANN N, VALLOORAN J J, et al. Oil and drug control the release rate from lyotropic liquid crystals. J Controlled Release, 2015, 204:78-84.
[7]
ZABARA A, MEZZENGA R. Controlling molecular transport and sustained drug release in lipid-based liquid crystalline mesophases. J Controlled Release, 2014, 188(6):31-43.
[8]
LOPES L B, COLLETT J H, BENTLEY M V. Topical delivery of cyclosporin A: an in vitro study using monoolein as a penetration enhancer. Eur J Pharm Biopharm, 2005, 60(1):25-30.
[9]
ELREFAIE W M,ELNAGGAR Y S,ELMASSIK M A. Novel self-assembled,gelcorehyaluosomes for non-invasive management of osteoarthritis: in vitro optimization,ex-vivo and in vivo permeation. Pharm Res,2015,32(9):2901-2911.
[10]
ELREFAIE W M,ELNAGGAR Y S,ELMASSIK M A. Novel curcumin-loaded gel-core hyaluosomes with promising burn-wound healing potential: development,in vitro appraisal and in vivo studies. Int J Pharm,2015,486(1-2):88-98.
[11]
GUAN Y M. Design and evaluation of transdermal drug delivery system for Tripterygium wilfordii microemulsion. Chengdu: Chengdu University of Chinese Medicine,2008.
[12]
LI Y. The studie on triptolidegels. Chongqing: Chong Qing Medical University,2008.
[13]
YU Y T, ZHU W F, CHEN L H. Preparation of triptolide microemulsion-based gel and investigation of its in vitro percutaneous permeability. Chin Hosp Pharm J(�й�ҽԺҩѧ��־), 2016, 36(13):1087-1091.
[14]
ZHANG J. Study on lipid cubic liquid crystal and imidazole ionic liquid liquidcrystal. Jinan:Shandong University, 2008.
[15]
DONG Y D, BOYD B J. Applications of X-ray scattering in pharmaceutical science . Int J Pharm, 2011, 417 ( 1-2 ):101-111.
[16]
MULET X, BOYD B J, DRUMMOND C J. Advances in drug delivery and medical imaging using colloidal lyotropic liquid crystalline dispersions . J Colloid Interface Sci, 2013, 393(1):1-20.
[17]
BARAUSKAS J, LAND H T. Phase behavior of the phytantriol/water system . Langmuir, 2003, 19(23):9562-9565.
[18]
MEZZENGA R, MEYER C, SERVAIS C, et al. Shear rheology of lyotropic liquid crystals: a case study. Langmuir Acs J Surfaces Colloids, 2005, 21(8):3322-3333.
[19]
RIZWAN S B, BOYD B J, RADES T, et al. Bicontinuous cubic liquid crystals as sustained delivery systems for peptides and proteins. Expert Opin Drug Deliv, 2010, 7(10):1133-1144.
2019, Vol. 54 
