Optimization of the dose of penetration enhancers in celecoxib gel by factorial design / 中国药学杂志

ABSTRACT

OBJECTIVE: To optimize the formula of celecoxib gel by studying the effects of different doses of penetration enhancers on the penetration of celecoxib through skin in vitro. METHODS: With sodium alginate as the gel base, factorial design method was used to choose the optimal formula of penetration enhancers among four different formulas to prepare celecoxib gels. The release rate of celecoxib in the release media was detected by modified Franz diffusion cells method, and the steady percutaneous speed (J), permeability coefficient (Kp) and the accumulative permeation quantity (Q) in 12 h were calculated. RESULTS: The accumulative permeation quantity (Q) in 12 h of celecoxib from the gels made with the four different formulas were 27.93, 25.12, 18.79 and 19.35 μg·cm-2, respectively. The gel with 1% azone and 1% menthol as penetration enhancers had the maximum Q value, 27.93 μg· cm-2, its penetration process conformed to Higuchi equation, and the steady percutaneous speed (J) and permeability coefficient(Kp) were also higher than the other three experimental groups. CONCLUSION: With sodium alginate as the gel base, azone and menthol have a synergistic effect on the percutaneous penetration of celecoxib gels, and the best formula is 1% azone and 1% menthol.