Formulation, characterization and pharmacokinetics of Morin hydrate niosomes prepared from various non-ionic surfactants

• Three differently optimized Morin hydrate (MH) niosomes were prepared as a result of the analysis of Taguchi orthogonal array (TOA).
• MH Tween 60 Niosomes found to be the most one with greater efficiency of entrapment, stability and AUC.
• The molecular modeling simulation study showed hydrogen bonding interaction between MH and human serum albumin (HSA).
• The in vivo imaging study revealed the capability of MH Tween 60 Niosomes to cross the blood brain barrier (BBB).

Morin hydrate (MH), a bioflavonoid with antioxidant and anticancer activity as well as the ability to improve the bioavailability of other drugs on their concurrent use. Three differently optimized niosomal formulations using three different non-ionic surfactants (Span 60, Span 80 and Tween 60) were achieved by (L9 (34)) Taguchi orthogonal array (TOA). The analysis of TOA revealed that Tween 60 Niosomes had the highest entrapment efficiency (93.4%) compared to other optimized Niosomal formulations (71–79%). In terms of MH remaining %, Tween 60 Niosomes were found to be the most stable (89%) at 4 °C over one month compared to Span 60 (56%) and Span 80 (57%) Niosomes. The release pattern in all Niosomal formulations was found to follow the Weibull model and Tween 60 Niosomes had the highest release rate. The molecular modeling simulation explained the binding of MH to the human serum albumin (HSA) by hydrogen bonds during the in vitro release process. As for the bioavailability, the AUC0–8 showed 1.3–2.7 fold increase compared to the MH solution. Ex vivo images of the excised organs showed that MH could accumulate in brain which indicates that MH-Tween 60 Niosomes might be a possible candidate to deliver hydrophobic drugs and overcome the blood–brain barrier (BBB) penetration.

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