Application of DoE in polymers screening and optimization of in situ topical film-forming solution for spray formulation

Abstract

DoE is a structured and organised method to determine the relationship between the effect of change in the concentration of the independent variables and its impact on the formulation, through establishing a mathematical model. Since the acceptance of the QbD approach by the regulatory authorities across the world, DoE has been widely implemented in the areas of screening and optimisation of the formulations by the pharmaceutical industries. The topical delivery of API still posses’ limitations such as insufficient contact time, odd hours of application time, sticking to fabrics, formulation washing off, etc. To address these limitations, the researcher planned to develop an in situ polymeric sprays that will form a transparent and flexible film, & will not interfere with the applicant’s routine. Polymers such as HPMC, Eudragit RS100, PVP K30, PVP K90, Carbopol, Propylene glycol, Soluplus, and pullulan whereas the plasticisers selected were sorbitol. Voriconazole, a second-generation triazole, was used as a model drug. The article is a technological demonstration, in which the screening of polymers as well as the optimised concentration of the polymeric will be selected through 3² factorial design. The aim of the present article is also to establish the relationship between the software response and experimental values. The experiments were designed using 3² factorial design which resulted in 9 trial runs. Each run was evaluated for drying time, viscosity, and stickiness. The resultant response surface Later the optimisation, to yield an optimised polymeric solution that can deliver a desired in situ films. Based on ANOVA comparison of variability due to treatment, the significance of the regression model was evaluated. Other procedures such as DSC, FRIR, Stickiness, pH, diffusion studies were also performed on the selected formulation.