Inhaling Vitamin D nanoemulsion through nose gets lots more to the brain (mice)

Created July 2020

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

Journal of Microencapsulation https://doi.org/10.1080/02652048.2020.1801870

Mukesh Kumar,Dhruv Kumar Nishad,Anoop kumar,Aseem Bhatnagar,Ritu Karwasra,Kushagra Khanna, show all

The study used radioactive Vitamin D

image

* Mucosal membranes (mouth, lungs, nose, intestines, etc) can activate Vitamin D – July 2020 Increased Vitamin D to the brain might help prevent/treat:     strokes, Alzheimer's, Parkinson's, Epilepsy, etc. Normally the blood-brain barrier somewaht restricts Vitamin D from getting to the brain The nose is directly connected to the brain – no blood-brain barrier Founder of VitaminDWiki has been inhailing Vitamin D nanoemulsion through his nose and mouth since 2017 Inhaled vitamin D help lungs - many studies Nanoemulsion Vitamin D may be a substantially better form image The nose, in addition to the lung, can activate Vitamin D locally. A nose, surprisingly, has MORE square meters of surface area than a lung --- 1. # 19+ VitaminDWiki pages with NANOEMULSION or EMULSION etc. in the title This list is automatically updated {LIST()}

📄 Download the PDF from sci-hub via VitaminDWiki

Aim: For the treatment of cerebral ischemia, Vitamin-D3 loaded nanoemulsion were developed.

Method: Tween 20 and polyethylene glycol were choosen as surfactant/co-surfactant, while oleic acid as oil phase. The formulation was characterized 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 13.77mV. 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 ischemic model confirmed better efficacy of Vitamin D3-Nanoemulsion.

Conclusion: This work demonstrated better permeation, deposition and efficacy of VitaminD3-Nanoemulsion through intranasal route.

Some of the References

  • Gupta, A., et al. 2016. Effect of Vitamin D and calcium supplementation on ischaemic stroke outcome: a randomized controlled open-label trial. ... ClinicalPractice. 70(9), 764-770.

  • Gupta, R., et al. 2018. Recent Advances in Formulation Strategies for Vitamin D. AAPS PharmSciTech. 20(1), 11.

  • Gupta, S., et al. 2017. Neuroprotective effect of lercanidipine in occlusion model of stroke in rats. Experimental Necrology. 288, 25-37 Guttoff, M., et al. 2015. Formation of vitamin D nanoemulsion-ba spontaneous emulsification: factors affecting 117-122.

  • Hossmann, K.A., 1994. Viability thresholds and the penumbra of focal Neurology. 36(4), 557-565.

  • Illum, L., 2003. Nasal drug delivery一possibilities, problems and solutions. Journal of Controlled Release. 87(1-3), 187-198.

  • Kumar, M., et al. 2008. Intranasal nanoemulsion based brain targeting drug delivery system of risperidone. International Journal of Pharmaceutics. 285-291.

  • Lakhan, S.E., Kirchgessner, A., Hofer, M., 2009. Inflammatory mechanisms in ischemic stroke: therapeutic approaches. Journal of Translational Medicine. 7(1), 97.

  • Lawrence, M. J. and Rees, G. D., 2000.Microemulsion-based media as novel drug delivery systems. Advance Drug Delivery Review. 45(1), 89-121.

  • Liu, W., et al. 2018. The anti -Inflammatory Effects of Vitamin D in Tumorigenesis. International Journal of Molecular Sciences. 19(9), 2136.

  • Li, J., et al. 2018. Preparation optimization and stirage stability of nanoemulsion based lutein delivery systems. Journal o/micoencapsulation. 35 (6), 570-583.

  • Majumdar, V., et al. 2015. Vitamin D status, hypertension and ischemic stroke: a clinical perspective. Journal of Human Hypertension. 29(11), 669-674.

  • Marklund, S. and Marklund, G., 19 autoxidation of pyrogallol and a conv of Biochemistry. 47 (3), 469-474.

  • Markisic, M., et al. 2017. The Impact of Homocysteine, Vitamin B12, and Vitamin D Levels on Functional Outcome after First-Ever Ischaemic Stroke. Biomed Research /nternational. 2017,1-6.

  • Md, S., et al. 2013. Bromocriptine loaded chitosan nanoparticles intended for direct nose to brain delivery: Pharmacodynamic, Pharmacokinetic and Scintigraphy study in mice model. European Journal of Pharmaceutical Science. 48 (3), 393-405.

  • Milanlioglu, A., et al. 2015. Serum antioxidant enzymes activities and oxidative stress levels in patients with acute ischemic stroke: influence on neurological status and outcome. Wien

  • Musa, S.H., et al. 2013. Formulation optimization of palm kernel oil esters nanoemulsion- loaded with chloramphenicol suitable for meningitis treatment.

  • Ohkawa, H., et al. 1979. Assay of lipid peroxides in animals tissue by thiobarbituric acid reaction. AnalyticalBiochemistr;y. 95 (2), 351-358.

  • Pangeni, R., et al. 2014. Vitamin E loaded resveratrol nanoemulsion for brain targeting for the treatment of Parkinson’s disease by reducing oxidative stress. Nanotechnology. 25(48), 485502.

    • Note: Resveratrol increases the activation of the Vitamin D Receptor

  • Punj, A., et al. 2017. Estimation of Antioxidant Levels in Saliva and Serum of Chronic Periodontitis Patients with and without Ischemic Heart Disease. International Journal of Dentistry. 1-9.

  • Sharma, N., et al. 2018. Development a] graecum (Fenugreek) polysaccharid 2571.

  • • Shi, Y., et al. 2015. Development optimization and evaluation of emodin loaded nanoemulsion prepared by ultrasonic emulsification. Journal of Drug Delivery Science and Technology. 27, 46-55.

  • Silva, H.D., et al.2011. Nanoemulsions for Food Applications: Development and Characterization. FoodBio ocess Technology. 5(3), 854-867.

  • Thakkar, H.P., et al. 2015. Formulation and evaluation of Itraconazole nanoemulsion for enhanced oral bioavailability. Journal of microencapsulation. 32 (6) 559-569.

  • Tran, T.H., et al. 2014. Quercetin -containing self-nanoemulsifying drug delivery system for improving oral bioavailability. Journal of Pharmaceutical Sciences. 103(3), 840-852.

    • Note: Quercetin increases the activation of the Vitamin D Receptor

  • Vyas, T., et al. 2005. Intranasal Drug Delivery for Brain Targeting. Current Drug Delivery.

  • Wei, Z.N. and Kuang, J.G., 2018. Vitamin D deficiency in relation to the poor functional outcomes in nondiabetic patients with ischemic stroke. Bioscience Reports. 38(2), 1-32.

  • Yu, H.L.et al. 2019. ESE1 expression correlates with neuronal apoptosis in the hippocampus after cerebralischemia/reperfusion injury. Neural Regeneration Research. 14(5), 41-849.

  • Zhou, R.et al. 2018. Lower Vitamin D Status Is Associated with an Increased Risk of Ischemic Stroke: A Systematic Review and Meta-Analysis. Nutrients. 10(3) 277.

Tags: Cognitive Forms Stroke