Enhancement in brain uptake of vitamin D<sub>3</sub> nanoemulsion for treatment of cerebral ischemia: formulation, gamma scintigraphy and efficacy study in transient middle cerebral artery occlusion rat models
Mukesh Kumar, Dhruv Kumar Nishad, Anoop Kumar, Aseem Bhatnagar, Ritu Karwasra, Kushagra Khanna, S. Keerthana, Deeksha Sharma, Kamal Dua, Vijaybabu Mudaliyar, Nitin Sharma
Abstract
Aim For the treatment of cerebral ischaemia, vitamin-D3 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 various in-vitro parameters. Targeting efficiency was investigated through radiometry, gamma scintigraphy and efficacy was studied in transient middle cerebral artery occlusion (MCAo) rat model.Result Vitamin D3-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 99mTc-vitamin D3-nanoemulsion through nasal route compared to IV administered 99mTc-vitamin D3 solution (0.79 ± 0.03%). Magnetic Resonance Imaging (MRI) of the ischaemic model confirmed better efficacy of vitamin D3-nanoemulsion.Conclusion This work demonstrated better permeation, deposition, and efficacy of vitaminD3-nanoemulsion through the intranasal route.