Design of meloxicam and lornoxicam transdermal patches: Preparation, physical characterization, ex vivo and in vivo studies.
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.
Department of Pharmaceutical Technology, Istanbul University, Turkey. gulyen@superonline.com
Gülgün
G
Yener
Melike
M
Üner
Ümit
Ü
Gönüllü
Sinem
S
Yildirim
Pınar
P
Kiliç
Serap Sağlik
SS
Aslan
Aslı
A
Barla
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000627:therapeutic use; D002152:Calorimetry, Differential Scanning; D016503:Drug Delivery Systems / Q000295:instrumentation / Q000379:methods*; D004487:Edema / Q000188:drug therapy; D065347:Hypromellose Derivatives; D000077239:Meloxicam; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D010894:Piroxicam / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000378:metabolism; D017550:Spectroscopy, Fourier Transform Infrared; D013718:Tensile Strength; D013843:Thiazines / Q000008:administration & dosage* / Q000627:therapeutic use; D013844:Thiazoles / Q000008:administration & dosage* / Q000627:therapeutic use
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013843:Thiazines; D013844:Thiazoles; D010894:Piroxicam; D065347:Hypromellose Derivatives; D008747:Methylcellulose; C059451:lornoxicam; D000077239:Meloxicam