Abstract
The purpose of present study was to prepare transdermal therapeutic system that could enhance dissolution of poorly aqueous soluble drug Celecoxib and thus increase its skin permeation. Solubility studies screened triacetin as oil, cremophor RH 40 as surfactant and Polyethylene Glycol 400 as co-surfactant. Pseudoternary phase diagrams were constructed to find out microemulsion region. Independent variables (oil, Smix and water) concentration was used at high (+1) and low levels (-1) that would generate 17 different combinations of microemulsions. Microemulsions were characterized, optimized and evaluated. pH, viscosity, conductivities, refractive index, droplet size and poly-dispersity-index was investigated. Prepared microemulsions were oil in water, thermodynamically stable, isotropic, transparent, deflocculated and within narrow range of size. Mathematical equations and response surface plots related the independent and dependent variables. Optimum microemulsion ME6 was further incorporated with carbomer 940 gel base to produce microemulsion based gel. ME6 and its gel showed significant difference (p<0.05) from control gel. Stability studies showed prepared MEBG of celecoxib was stable during storage period. Skin irritation studies found the gel was safe and non-irritating to skin. Anti-inflammatory studies showed significant difference (p<0.05) compared to control gel. Thus, the therapeutic system was successfully developed and optimized using Box Behnken statistical design.
Highlights
The first synthesized non-steroidal antiinflammatory drug (NSAID) Celecoxib showed its effect by selectively inhibiting COX-2 activity
Triacetin, Cremophor RH 40, Polyethylene glycol-400 (PEG 400) and water were selected as microemulsion components because these showed comparatively high solubility and miscibility among themselves
Construction of pseudoternary phase diagrams The developed pseudo-ternary phase diagrams facilitated to find out area of microemulsion region and concentration ranges for microemulsion components
Summary
The first synthesized non-steroidal antiinflammatory drug (NSAID) Celecoxib showed its effect by selectively inhibiting COX-2 activity. Long term oral delivery of Celecoxib results in serious side effects like gastrointestinal toxicity, gastric mucosal ulceration, hemorrhage and currently, cardio-toxic effects which prohibit its oral usage and make this a suitable candidate for transdermal application. It has very poor aqueous solubility in water (4 mg/L) and skin barrier function limit its formulation for transdermal dosage forms and make it challenging. One of the main techniques to enhance the transdermal permeation of drugs is preparation of microemulsion (ME) which act as vehicles (Cevc & Vierl 2010, Shakeel & Ramadan 2010). Microemulsion is defined as an oil in water (o/w) or water in oil (w/o) showing a transparent
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