Enhancement in brain uptake of vitamin D₃ nanoemulsion for treatment of cerebral ischemia: formulation, gamma scintigraphy and efficacy study in transient middle cerebral artery occlusion rat models

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.

Keywords:

• Gamma scintigraphy
• ischaemia
• MRI
• nanoemulsion
• vitamin D₃

Acknowledgments

The authors would like to thank Dr. AK Singh, former Director, Institute of Nuclear Medicine and Allied Sciences (INMAS) Delhi and Dr.Tarun Sekhri, current Director, INMAS for providing all necessary facilities as well as a conducive environment to carry out this research work. The authors are also grateful to All India Institute of Medical Sciences, New Delhi, for providing technical guidance.

Disclosure statement

No potential conflict of interest was reported by the author(s).