Enhanced topical delivery of tacrolimus by a carbomer hydrogel formulation with transcutol P

被引:31
作者
Lee, Sang Gon [1 ]
Kang, Jong Bu [1 ]
Kim, Sung Rae [1 ]
Kim, Chae Jin [1 ]
Yeom, Dong Woo [1 ]
Yoon, Ho Yub [1 ]
Kwak, Seong Shin [1 ]
Choi, Young Wook [1 ]
机构
[1] Chung Ang Univ, Coll Pharm, 221 Heuksuk Dong, Seoul 156756, South Korea
基金
新加坡国家研究基金会;
关键词
Carbomer gel; tacrolimus; topical delivery; transcutol P; skin permeation; TRANSDERMAL DELIVERY; IN-VITRO; ATOPIC-DERMATITIS; PERCUTANEOUS PENETRATION; SKIN PERMEABILITY; DERMAL DELIVERY; DRUG-DELIVERY; RAT SKIN; PERMEATION; MICROEMULSION;
D O I
10.3109/03639045.2016.1160107
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Tacrolimus (TAC), a non-steroidal anti-inflammatory and immunosuppressive agent, is used for the treatment of atopic dermatitis (AD) and skin immune diseases. TAC-loaded topical hydrogel formulations composed of carbomer, carnosine, transcutol P (diethylene glycol monoethyl ether) and humectant were prepared. For comparison, TAC-loaded topical cream-type formulations were also prepared and commercially available TAC ointment was used as a reference. A drug release study in vitro revealed that the total amount of TAC released from hydrogels over 24 h was approximately 30 times greater than that for the reference formulation. Compared to the reference ointment and creams, carbomer gel formulations showed higher skin permeation and retention of TAC (significantly different at p<0.05), especially those with more than 10% of transcutol P. Therefore, carbomer gel formulations with sufficient levels of transcutol P are good candidates for skin delivery of TAC and have potential as therapeutic agents for the treatment of AD or immune skin disorders.
引用
收藏
页码:1636 / 1642
页数:7
相关论文
共 40 条
[11]   Lecithin vesicular carriers for transdermal delivery of cyclosporin A [J].
Guo, JX ;
Ping, QN ;
Sun, GQ ;
Jiao, CH .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 194 (02) :201-207
[12]   Effect of poloxamer on physicochemical properties of tacrolimus solid dispersion improving water solubility and dissolution rate [J].
Ha J.-M. ;
Kang S.-Y. ;
Park C.-W. ;
Bin S.-A. ;
Rhee Y.-S. ;
Seo J.-W. ;
Kim S.-H. ;
Chi S.-C. ;
Park E.-S. .
Journal of Pharmaceutical Investigation, 2012, 42 (4) :171-176
[13]   Efficacy and safety of tacrolimus ointment treatment for up to 4 years in patients with atopic dermatitis [J].
Hanifin, JM ;
Paller, AS ;
Eichenfield, L ;
Clark, RA ;
Korman, N ;
Weinstein, G ;
Caro, I ;
Jaracz, E ;
Rico, MJ .
JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY, 2005, 53 (02) :S186-S194
[14]   POLYSACCHARIDES IN FUNGI .9. ANTI-INFLAMMATORY ACTIVITY AND CONFORMATIONAL BEHAVIOR OF A BRANCHED (1-]3)-BETA-D-GLUCAN FROM AN ALKALINE EXTRACT OF DICTYOPHORA-INDUSIATA FISCH [J].
HARA, C ;
KIHO, T ;
TANAKA, Y ;
UKAI, S .
CARBOHYDRATE RESEARCH, 1982, 110 (01) :77-87
[15]  
Hua L, 2004, PHARMAZIE, V59, P274
[16]   Rheological characterization of topical carbomer gels neutralized to different pH [J].
Islam, MT ;
Rodríguez-Hornedo, N ;
Ciotti, S ;
Ackermann, C .
PHARMACEUTICAL RESEARCH, 2004, 21 (07) :1192-1199
[17]   Nanoemulsions loaded Carbopol® 934 based gel for intranasal delivery of neuroprotective Centella asiatica extract: in–vitro and ex–vivo permeation study [J].
Jaiswal M. ;
Kumar A. ;
Sharma S. .
Journal of Pharmaceutical Investigation, 2016, 46 (1) :79-89
[18]   Influence of Liposome Type and Skin Model on Skin Permeation and Accumulation Properties of Genistein [J].
Kang, Kyoung Hoon ;
Kang, Myung Joo ;
Lee, Jaehwi ;
Choi, Young Wook .
JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY, 2010, 31 (08) :1061-1066
[19]   Effect of jet fuels on the skin morphology and irritation in hairless rats [J].
Kanikkannan, N ;
Locke, BR ;
Singh, M .
TOXICOLOGY, 2002, 175 (1-3) :35-47
[20]   Combined effect of oleic acid and propylene glycol on the percutaneous penetration of tenoxicam and its retention in the skin [J].
Larrucea, E ;
Arellano, A ;
Santoyo, S ;
Ygartua, P .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2001, 52 (02) :113-119