Abstract
Intranasal administration is a non-invasive and effective way for the delivery of drugs to brain that circumvents the blood– brain barrier (BBB). Taking this into account it was planned to formulate a thermodynamically stable and infinite dilutable nanoemulsion (o/w) encapsulating Ropinirole (rop), an anti-Parkinson drug, using a surfactant in a minimum concentration that could improve its solubility, stability and intransnasal flux. Various surfactants, co-surfactants and their mixtures were screened for their ability to emulsify the selected oil. Ternary phase diagrams were constructed to locate the area of nanoemulsion for. The optimized formulation contained 2 mg of Ropinirole along with Sefsol 218 (10% v/v), tween 80 (18% v/v), Transcutol (18% v/v) and water (54% v/v) as matrix, surfactant, cosurfactant and aqueous phase respectively. The optimized formulation showed adequate drug release (72.23±9.56%), globule size (58.61±5.18), polydispersity (0.201), viscosity (31.42±6.97 mpas), and infinite dispersion capability. The ex vivo study showed significant high (p<0.005) drug translocation in different parts of Wister rat brain. From in vitro, ex vivo and in vivo results conclude the promising approach of intranasal Ropinirole nanoemulsion as a better management option for Parkinson’s disease.
Keywords: Ropinirole, Nanoemulsion, Thermodynamic stability, Phase diagram, Intratracheal intubation model, transmission electron microscopy, matrix