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J Microencapsul ; 37(7): 492-501, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32715833

RESUMO

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.


Assuntos
Colecalciferol/administração & dosagem , Emulsões/química , Infarto da Artéria Cerebral Média/tratamento farmacológico , Vitaminas/administração & dosagem , Administração Intranasal , Animais , Encéfalo/irrigação sanguínea , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Infarto Cerebral/tratamento farmacológico , Infarto Cerebral/metabolismo , Colecalciferol/farmacocinética , Colecalciferol/uso terapêutico , Portadores de Fármacos/química , Infarto da Artéria Cerebral Média/metabolismo , Ratos Sprague-Dawley , Vitaminas/farmacocinética , Vitaminas/uso terapêutico
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