Abstract：OBJECTIVE To optimize the preparation technology of iguratimod ethosomal and evaluate its preparations performance and characteristics of the in vitro transdermal penetration. METHODS The iguratimod ethosomes were prepared with injection method. The formulation and the preparation method of ethosomes were optimized by orthogonal experiment. Their physicochemical properties including particle size, morphology and encapsulation efficiency were characterized,and the carbomer was added as the base for the preparation of the ethosomal gel. The penetration of iguratimod ethosomal gel through mouse skin were performed by Franz′s cell. The cumulative penetration amount was calculated. RESULTS The color of iguratimod ethosome prepared under optimum conditions was light blue, the sizes were (97.60±5.9) nm. The entrapment efficiency of iguratimod in ethosomes was (95.39±1.06)%. Accumulative permeation amount of iguratimod ethosomal gel within 24 h was 51.15 μg·cm-2, which was about 3.43 times of normal gel. CONCLUSION The iguratimod ethosomes have a suitable size, a high entrapment efficiency and the gel is feasible in preparation technique, controllable in quality and can improve transdermal penetration of iguratimod.
金银秀, 陶雪芬, 王玉新, 张明涛, 王金朝, 周逸轩, 杨芳芳, 罗俊杰. 艾拉莫德醇质体凝胶的制备及其经皮渗透特性研究[J]. 中国药学杂志, 2020, 55(21): 1807-1811.
JIN Yin-xiu, TAO Xue-fen, WANG Yu-xin, ZHANG Ming-tao, WANG Jin-zhao, ZHOU Yi-xuan, YANG Fang-fang, LUO Jun-jie. Preparation and Transdermal Permeation of Iguratimod Ethosomal Gel in Vitro. Chinese Pharmaceutical Journal, 2020, 55(21): 1807-1811.
MUCKE H A. Iguratimod: a new disease-modifying antirheumatic drug[J]. Drugs Today (Barc), 2012, 48(9):577-586.
TANAKA K, YAMAGUCHI T, HARA M. Iguratimod for the treatment of rheumatoid arthritis in Japan[J]. Expert Rev Clin Immunol, 2015, 11(5):565-573.
OKAMURA K, YONEMOTO Y, SUTO T, et al. Efficacy at 52 weeks of daily clinical use of iguratimod in patients with rheumatoid arthritis[J]. Mod Rheumatol, 2015, 25(4):534-539.
MIMORI T, HARIGAI M, ATSUMI T, et al. Safety and effectiveness of iguratimod in patients with rheumatoid arthritis: final report of a 52-week, multicenter postmarketing surveillance study[J]. Mod Rheumatol, 2019, 29(2):314-323.
LI X L, LIU X C, SONG Y L, et al. Suspected drug-induced liver injury associated with iguratimod: a case report and review of the literature[J]. BMC Gastroenterol, 2018, 18(1):130-135.
SHI B W, LIN Q P, LI X Q, et al. Preparation of iguratimod sustained-release pellets[J]. Chin J Pharm(中国医药工业杂志), 2016, 47(6):717-722.
MA Z Z, TAO C, SUN L, et al. In situ forming injectable hydrogel for encapsulation of nanoiguratimod and sustained release of therapeutics[J]. Int J Nanomed, 2019, 14: 8725-8738.
XIA Y F, CHU K D, LI H, et al. Overview of traditional Chinese medicine transdermal drug delivery preparations for rheumatoid arthritis[J]. J Extern Ther Tradit Chin Med(中医外治杂志), 2012, 21(1):44-46.
SHI X Q, ZHAO J H, WANG Z D, et al. Application of ethosomes as carriers in dermal and transdermal drug delivery[J]. Chin J Exp Tradit Med Form(中国实验方剂学杂志), 2013, 19(12):352-355.
JIN Y X, WANG Y X, TAO X F, et al. Study on preparation and transdermal permeation of ropivacaine ethosomal gel in vitro[J]. Chin Pharrm J(中国药学杂志), 2016,51(23):2041-2044.
JIN Y X, WANG Y X,SHI L, et al. Determination of entrapment efficiency of oxcarbazepine nanostructured lipid carriers [J]. Sci Technol Chem Ind(化工科技), 2016, 24(2):50-53.
FU X L, SHI Y B, WANG H,et al. Ethosomal gel for improving transdermal delivery of thymosin β-4[J]. Int J Nanomed, 2019, 14(11):9275-9284.
WANG X N, FENG S M, ZHANG C L. Preparation and characterization of ketoprofen ethosomes and the transdermal penetration in vitro[J]. Appl Chem Ind(应用化工), 2015, 44(8):1461-1467.
NIE Y, HE S J, CHEN L L, et al. Preparation and in vitro transdermal penetration of nisoldipine ethosomes[J]. Chin J Hosp Pharm (中国医院药学杂志), 2013, 33(20):1677-1681.