Formulation, Optimization and Evaluation of Non-aerosol Topical Spray of Lidocaine for Pain Management

Abstract

Background: The optimization study was conducted in an attempt to develop a non-pressurized topical spray of Lidocaine without propellant. Methods: Central composite design was selected to determine the best conditions for the formulation of sprays with two independent factors were prepared (pH adjuster i.e sodium citrate and penetration enhancer i.e. propylene glycol). Concentration of propylene glycol (X1) of (5-25 ml) and sodium citrate (X2) of (0.5-2.0 ml) was the value range of the variables. F5 was ideally suited for use by spraying the container of a pump spray. Results: The drug content of F5 was 98.8% which indicates that the drug is distributed almost uniformly throughout the formulation and that there was no loss of drug in the formulation. Evaporation time and total number of delivery of F5 batch was about 2 min and 487. Drug content per actuation, diffusion study of F5 and marketed formulation were 97.64, 98.88 (at 6hr) and 68.64 (at 6 hr) respectively. The best fitted model for the drug content and evaporation time was quadric fit provided the value of r2 (0.9070 and 0.974) respectively. Conclusion: The research work concludes about the successful preparation of non-pressurized Lidocaine spray with local anesthetic action.