Journal of Microencapsulation, Vol.37, No.7, 492-501, 2020
Enhancement in brain uptake of vitamin D(3)nanoemulsion for treatment of cerebral ischemia: formulation, gamma scintigraphy and efficacy study in transient middle cerebral artery occlusion rat models
Aim For the treatment of cerebral ischaemia, vitamin-D(3)loaded nanoemulsions were developed. Method Tween 20 and polyethylene glycol were chosen as surfactant/co-surfactant, while oleic acid as the oil phase. The formulation was characterised for variousin-vitroparameters. Targeting efficiency was investigated through radiometry, gamma scintigraphy and efficacy was studied in transient middle cerebral artery occlusion (MCAo) rat model. Result Vitamin D-3-nanoemulsion showed a mean size range of 49.29 +/- 10.28 nm with polydispersity index 0.17 +/- 0.04 and zeta potential 13.77 mV. The formulation was found stable during thermodynamic stability study and permeated within 180 min through sheep nasal mucosa (permeation coefficient 7.873 +/- 0.884 cm/h). Gamma scintigraphy and radiometry assay confirmed better percentage deposition (2.53 +/- 0.17%) of(99m)Tc-vitamin D-3-nanoemulsion through nasal route compared to IV administered(99m)Tc-vitamin D(3)solution (0.79 +/- 0.03%). Magnetic Resonance Imaging (MRI) of the ischaemic model confirmed better efficacy of vitamin D-3-nanoemulsion. Conclusion This work demonstrated better permeation, deposition, and efficacy of vitaminD(3)-nanoemulsion through the intranasal route.