Zolmitriptan brain targeting via intranasal route using solid lipid nanoparticles for migraine therapy: Formulation, characterization, in-vitro and in-vivo assessment

dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorMostafa, D.A.E
dc.contributor.authorKhalifa, M.K.A
dc.contributor.authorGad, S.S
dc.date.accessioned2020-03-19T07:21:54Z
dc.date.available2020-03-19T07:21:54Z
dc.date.issued2020-04
dc.descriptionScopusen_US
dc.description.abstractObjective: Zolmitriptan, a class of antidepressant drugs with poor bioavailability due to its first-pass metabolism. The aim of this study was to improve systemic bioavailability and explore the brain targeting impact of nasal Zolmitriptan (Zol) solid lipid nanoparticles (SLNs) gel for migraine treatment. Methods: Stearic acid and cholesterol used as solid lipid and lecithin as a surfactant, emulsion solvent evaporation technique was used to produce Zolmitriptan SLNs. (Zol) SLNs were characterized for particle size, percent entrapment efficiency and in vitro drug release. Formula S6 showed greater percent entrapment efficiency (PEE), adequate particle size and sustained drug release behavior. Formula S6 was integrated into HPMC gel (3%) to prepare nasal gel. Zol SLN nasal gel was subjected to histopathological study to ensure brain targeting. Results: It was observed that all prepared Zol SLNs were in the nano-sized range with a polydispersity index of<0.5. In the cholesterol/lecithin combination, higher PEE%, better stability, and less agglomeration inclination were discovered. Results of the release profiles showed that developed Zol-SLNs were able to release Zolmitriptan in a sustained manner. Histopathological study of the brain tissues showed that Zolmitriptan SLN nasal gel can reach brain cells and localized for 24 h although the hydrophobicity of the target drug. Conclusion: Intranasal administration of Solid lipid nanostructure of Zolmitriptan through the olfactory pathway in which it travels from the nasal cavity to brain tissue achieved drug targeting potential of about 90% compared with conventional Zolmitriptan tablets. The small particle size helped them to squeeze themselves through the small opening in the olfactory neurons to the brain via different endo-cystic pathways of neuronal cells in nasal tissue membranes. © 2020 The Authors.en_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=19900192174&tip=sid&clean=0
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dc.identifier.doihttps://doi.org/10.22159/ijap.2020v12i2.36812
dc.identifier.issn9757058
dc.identifier.otherhttps://doi.org/10.22159/ijap.2020v12i2.36812
dc.identifier.urihttps://t.ly/MROwZ
dc.language.isoen_USen_US
dc.publisherInnovare Academics Sciences Pvt. Ltden_US
dc.relation.ispartofseriesInternational Journal of Applied Pharmaceutics;Volume 12, Issue 2, March-April 2020, Pages 86-93
dc.subjectuniversity of Brain targetingen_US
dc.subjectHistopathological examinationen_US
dc.subjectMigraineen_US
dc.subjectSolid lipid nanoparticles (SLNs)en_US
dc.subjectZolmitriptanen_US
dc.titleZolmitriptan brain targeting via intranasal route using solid lipid nanoparticles for migraine therapy: Formulation, characterization, in-vitro and in-vivo assessmenten_US
dc.typeArticleen_US

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