Fabrication and application of a dual drug-loaded nanoniosomes encapsulating rutin and berberine: optimization, in vitro and ex vivo evaluation.

AbstractRutin and berberine are naturally occurring polyphenols but their usefulness is restricted by their low bioavailability and poor solubility. Thus, by delivering rutin–berberine in the form of niosomes simultaneously and hoped to enhance the permeability through nasal route for the treatment of depression. Thin-film hydration approach was used to generate dual drug-loaded niosomes (rutin–berberine) encapsulating rutin and berberine. Various analytical techniques were used to characterize the morphology, size, compatibility, and leakage of the particles. These techniques included transmission electron microscopy, dynamic light scattering, UV spectrophotometry, and differential scanning calorimetry. The optimized formulation (rutin–berberine optimized niosomal formulation) was subjected to additional characterization for drug release, ex-vivo penetration investigation, confocal laser scanning microscopy, and 2,2-diphenyl-1-picrylhydrazyl assay. The rutin–berberine optimized niosomal formulation analysis showed that the drug release was 76.66 ± 1.24% at 24 hours, the entrapment efficiency was 74.8 ± 2.13% (rutin), and 79.0 ± 3.47% (berberine) and the vesicle size was 72.6 nm with a polydispersion index of 0.208. The antioxidant activity showed 73.67 ± 2.5% which is close to regular ascorbic acid. Studies on permeation ex-vivo revealed that rutin–berberine optimized niosomal formulation had considerably higher permeation (84.89 ± 3.15%) compared to rutin–berberine suspension (37.28 ± 2.33%). Furthermore, rhodamine B-loaded rutin–berberine optimized niosomal formulation appeared to have higher penetration than the control (rhodamine B-solution) according to the confocal laser scanning microscope results of the nasal mucosa. Based on all the experimental data, rutin–berberine optimized niosomal formulations were determined to be a viable and successful intranasal delivery formulation. [ABSTRACT FROM AUTHOR]