In vitro transdermal permeation of fenoterol hydrobromide

被引:16
作者
Elshafeey, Ahmed H. [1 ,2 ]
Hamza, Yassin E. [2 ]
Amin, Soad Y. [2 ]
Zia, Hossein [1 ]
机构
[1] Univ Rhode Isl, Coll Pharm, Appl Pharmaceut Sci, Kingston, RI 02881 USA
[2] Cairo Univ, Coll Pharm, Dept Pharmaceut, Giza, Egypt
关键词
Fenoterol; Transdermal; Patches; Enhancers; Duro-Tak;
D O I
10.1016/j.jare.2011.05.009
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
The aim of this study was to determine if transdermal penetration of fenoterol, a beta-agonist drug, could be enhanced and controlled by formulation modification and formulation of transdermal patches. Pre-formulation studies were performed to determine the feasibility of a transdermal dosage form of fenoterol. Penetration of fenoterol was determined using the hairless guinea pig skin with unjacketed Franz diffusion cell. Transdermal patches were formulated using drug in-adhesive technique. Several enhancers were investigated for fenoterol skin penetration. Transcutol-oleic acid co-solvent gives the highest drug flux among all tested liquid formulations. Pretreatment of the skin with oleic acid 2 h before patch application significantly increases drug diffusion. Cis-oleic acid gives best results compared to oleic acid. Azone derivative (1-dodecyl-2-pyrrolidinone) gives the highest drug diffusion amongst all tested enhancers. Results of this study show the feasibility of using fenoterol formulated in transdermal delivery system in the treatment of chronic asthma to improve patient compliance, bioavailability and reduce the inter-subject variability. (C) 2011 Cairo University. Production and hosting by Elsevier B.V. All rights reserved.
引用
收藏
页码:125 / 132
页数:8
相关论文
共 29 条
[1]  
Davis S.S., Illum L., Tamlinson E., Enzymatic barriers to peptide and protein absorption and the use of penetration enhancers to modify its absorption, Delivery Systems for Peptide Drugs, pp. 389-416, (1986)
[2]  
Wohlrab J., Kreft B., Tamke B., Skin tolerability of transdermal patches, Expert Opin Drug Deliv, (2011)
[3]  
Burkoth T., Bellhouse B., Hewson G., Transdermal and transmucosal powdered drug delivery, Crit Rev Ther Drug Carrier Syst, 16, 4, pp. 331-384, (1999)
[4]  
Squillante E., Nanda A., Needham T.E., Zia H., Transdermal delivery of calcium channel blockers such as nifedipine, 6, 106, (2000)
[5]  
Mitragorti S., Kost J., Low frequency sonophoresis. A non-invasive method of drug delivery and diagnostics, Biotechnol Prog, 16, pp. 448-492, (2000)
[6]  
Sears M.R., The evolution of beta2-agonists, Respir Med, 95, (2001)
[7]  
Hochhaus G., Schmidt E.W., Rominger K.L., Mollmann H., Pharmacokinetic/dynamic correlation of pulmonary and cardiac effect of fenoterol in asthmatic patients after different routes of administration, Pharm Res, 9, pp. 291-297, (1992)
[8]  
Lin W J., Wu T.L., Modification of the initial release of a highly water-soluble drug from ethyl cellulose microspheres, J Microencapsul, 16, 5, pp. 639-646, (1999)
[9]  
Almirall M., Montana J., Escribano E., Obach R., Berrozpe J., Effect of d-limonene, alpha-pinene and cineole on in vitro transdermal human skin penetration of chloropromazine and haloperidol, Arzneim-Forsch Drug Res, 46, 7, pp. 678-680, (1996)
[10]  
Obata Y., Takayania K., Maitani Y., Machida Y., Nagai T., Effect of pretreatment of skin with cyclic monoterpenes on penetration of diclofenac in hairless rat, Biol Pharm Bull, 3, (1993)