Design of Meloxicam and Lornoxicam Transdermal Patches: Preparation, Physical Characterization, ex Vivo and in Vivo Studies

被引:33
作者
Yener, Gulgun [1 ]
Uner, Melike [1 ]
Gonullu, Umit [1 ]
Yildirim, Sinem [1 ]
Kilic, Pinar [1 ]
Aslan, Serap Saglik [2 ]
Barla, Asli [3 ]
机构
[1] Istanbul Univ, Fac Pharm, Dept Pharmaceut Technol, TR-34116 Istanbul, Turkey
[2] Istanbul Univ, Fac Pharm, Dept Analyt Chem, TR-34116 Istanbul, Turkey
[3] Aromsa Besin Aroma & Katki Maddeleri Sanayi & Tic, TR-41480 Gebze, Kocaeli, Turkey
关键词
meloxicam; lornoxicam; transdermal delivery; transdermal patch; anti-inflammatory activity; PHYSICOCHEMICAL CHARACTERISTICS; PHARMACOKINETIC PROPERTIES; DELIVERY; RELEASE; DRUG; ABSORPTION; SYSTEMS; NSAIDS;
D O I
10.1248/cpb.58.1466
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Transdermal patches of meloxicam (MX) and lornoxicam (LX) were aimed to be prepared in order to overcome their side effects by oral application. The strategy was formulation of optimized films to prepare transdermal patches by determination of physical properties and investigation of drug-excipient compatibility. As the next step, in vitro drug release, assesment of anti-inflammatory effect on Wistar Albino rats, ex vivo skin penetration and investigation of factors on drug release from transdermal patches were studied. Hydroxypropyl methylcellulose (HPMC) was concluded to be suitable polymer for formulation of MX and LX transdermal films indicating pharmaceutical quality required. MX and LX transdermal patches gave satisfactory results regarding to the edema inhibition in the assessment of anti-inflammatory effect. MX was found out to be more effective compared to LX on relieving of edema and swelling. These results were supported by data obtained from ex vivo penetration experiments of drug through rat skin. indicative parameters like log P, molecular weight and solubility constraint on penetration rate of drugs also indicated good skin penetration. Transdermal patches of MX and LX can be suggested to be used especially for the immediate treatment of inflammated area since it displays anti-inflammatory effect, soon.
引用
收藏
页码:1466 / 1473
页数:8
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