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.

中文翻译：

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增强维生素D3纳米乳剂在脑中的摄取以治疗脑缺血：配方，γ闪烁显像和在短暂性中脑动脉阻塞大鼠模型中的功效研究。

摘要

目标

为了治疗脑缺血，开发了负载维生素D _3的纳米乳剂。

方法

选择吐温20和聚乙二醇作为表面活性剂/助表面活性剂，而油酸作为油相。针对各种体外参数表征制剂。通过放射线照相法，γ闪烁显像法研究了靶向效率，并在短暂性大脑中动脉阻塞（MCAo）大鼠模型中研究了功效。

结果

维生素D _3-纳米乳液的平均粒径范围为49.29±10.28 nm，多分散指数为0.17±0.04，ζ电位为13.77 mV。在热力学稳定性研究中发现该制剂稳定，并在180分钟内透过羊鼻粘膜渗透（渗透系数7.873±0.884 cm / h）。与静脉内施用^99m Tc-维生素D ₃溶液（0.79±0.03％）相比，伽玛闪烁显像和放射线测定法证实^99m Tc-维生素D _3-纳米乳剂通过鼻腔途径的沉积百分比更高（2.53±0.17 ％）。缺血模型的磁共振成像（MRI）证实了维生素D _3-纳米乳剂的更好疗效。

结论

这项工作通过鼻内途径证明了维生素D _3-纳米乳剂的更好的渗透，沉积和功效。