Preliminary studies for the development of intranasal nanoemulsion containing CNS agent: emphasizing the utilization...

The selection of excipients and preformulation strategy plays a vital role for the development of nanoemulsion, due to anatomical and physiological challenges posed by nasal cavity.

This attempt is focused on the selection and optimization of excipients for the development of a nanoemulsion system for intranasal delivery.

Excipients were selected on the basis of solubility of active drug, compatibility interactions and nasal irritancy. Surfactant and co-surfactant combination and their ratio were finalized on the basis of nanoemulsion region obtained from constructed phase diagrams with Capmul MCM as oil phase. A validated cut and weigh method was employed for the optimization of different phase diagrams with respect to nanoemulsion region.

The solubility of drug in Capmul MCM, Labrasol, and Transcutol-P was found to be superior with numeric values of 79.50 ± 1.68 mg/ml, 51.10 ± 1.39 mg/ml, and 36.60 ± 0.85 mg/ml, respectively. On the basis of phase diagram analysis, Labrasol and Transcutol-P in 3:1 ratio provides greater nanoemulsion region of 65.28 ± 0.18%. The validation of cut and weigh method revealed that there was no significant statistical difference (P > 0.05) with a %RSD value of 2.38 for intersheet variation.

The results of validation studies for cut and weigh method suggests that it can be effectively used as an optimization method for the selection of nanoemulsion composition.