BBD assisted in-situ nanoliposomes of esculin hydrate via intranasal delivery for the amelioration of Parkinson's disease

The objective of this research was to develop and optimise esculin Hydrate loaded nanoliposomes (ESH-NLs). The nanoliposomes were prepared by solvent evaporation method and optimised using a three-factor, three-level Box-Behnken design. Phospholipid 90G (X1), cholesterol (X2), and sonication time (X3) were used as independent variables, and their effects on vesicle size (Y1), entrapment efficiency (Y2), and Polydispersity index (Y3) were observed. The opt-ESH-NLs were further characterised for in-vitro drug release, DPPH assay, confocal laser scanning microscopy, and ex-vivo permeation. Opt-ESH-NLs had a vesicle size of 88.36 nm, a PDI of 0.06, an entrapment efficiency of 94.22±0.93%, and a drug release of 76.776±1.127%. Compared to standard ascorbic acid, the antioxidant activity was found to be 78.52±0.148%. Ex-vivo permeation studies revealed that opt-ESH-NLs had significantly enhanced permeation (79.484± 0.754 %) compared to ESH suspension (38.326± 1.279 %). Pharmacokinetic study revealed that opt-ESH-NLs when compared with Oral ESH suspension had a significant bioavailability in Brain as compared to plasma. The stability study of nanoliposomes at 4 °C reveals there is no significant change in the formulation. It was concluded that opt-ESH-NLs is a promising and effective formulation for intranasal administration for direct delivery of drug in the brain for amelioration of PD.