Abstract
Purpose: To investigate the in vitro permeation and drug release kinetics of flurbiprofen gel.Methods: Thirteen batches (G1, G2 … G13) of flurbiprofen gels were prepared using different ratios ofpermeation enhancers, i.e., propylene glycol (PG) and polyethylene glycol (PEG), by response surface methodology (RSM). Viscosity, pH, spreadability, consistency and drug content of the flurbiprofen gels were measured. Permeation experiments were conducted using silicone membrane in a modified Franz diffusion cell. Permeation parameters determined include diffusion coefficient (D), Flux (J), lag time (tLag), permeation coefficient (Kp), input rate (IR) and enhancement ratio (ER). Primary skin irritation test was performed for the optimized gel, G3, using 11 human volunteers.Results: Maximum solubility (72.15 ± 0.02 mg/mL) of flurbiprofen was observed in a mixture (2:1) of methanol and water. Partition coefficient (Ko/w) was determined as logP = 3.68 ± 0.11. The gels were stable under various storage conditions, and were homogenous, crystalline and transparent. Viscosity, pH, spreadability, consistency and drug content were in the range of 150 – 178 × 102 cps, 5.42 - 5.75, 5.0 - 7.0 g.cm/s, 3.0 - 9.0 mm, and 97.99 - 99.86 %, respectively. No irritation or lesions (erythma, redness and ulceration) occurred in human volunteers over a 30-day period. The optimized formulation, G3, showed maximum flux through silicone membrane.Conclusion: PG and PEG are effective enhancers of flurbiprofen from various formulations when used in various ratios.Keywords: Flurbiprofen, Gel, Diffusion, Permeation enhancers, Skin irritation, Silicone membrane
Highlights
The physicochemical, pharmacokinetic, and pharmacodynamic properties of flurbiprofen make it a worthy candidate for transdermal drug delivery [1,2]
Many in vitro studies have suggested that propylene glycol (PG) and polyethylene glycol (PEG) are capable of penetrating across the skin elaborating their role as skin penetration enhancers [9,10,11]
The solubility of flurbiprofen in water was 0.01 ± 0.01 mg/mL, in methanol 69.20 ± 0.01 mg/mL, in normal saline 0.27 ± 0.01 mg/mL, in PBS 17.62 ± 0.03 mg/ml, in PBS mixed with methanol 61.71 ± 0.15 mg/ml while in mixture of methanol and water (2:1), solubility was 72.15 ± 0.02 mg/ml
Summary
The physicochemical, pharmacokinetic, and pharmacodynamic properties of flurbiprofen make it a worthy candidate for transdermal drug delivery [1,2]. It has a molecular weight of 244.26 Daltons and value of log P (octanol/water, pH 7.4) is 3.80. Extensive research studies are being carried out to explore various approaches for promoting drug delivery across skin. Chemical enhancers are substances which temporarily reduce skin barrier features leading to increased drug absorption [6]. Some examples of these enhancers are essential oils, terpenes, and fatty acids. Many in vitro studies have suggested that propylene glycol (PG) and polyethylene glycol (PEG) are capable of penetrating across the skin elaborating their role as skin penetration enhancers [9,10,11]
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