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Formulation and Evaluation of Intranasal Microemulsion of Entacapone For Treatment of Parkinsonism
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| Author:
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ASHISH P.GORLE, RUTUJA S.SHENDE, JAYESH A.MAHIRRAO
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| Abstract:
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In the present study, the developed Entacapone (ENT) loaded microemulsion (ME) prone to increase the solubility of ENT by components of microemulsion including formulation concern, characterization, mucosal diffusion, stability and nasal ciliotoxicity of Entacapone microemulsion (EME). For nasal delivery of Entacapone, a challenge existing in formulation development is the solubilization of poorly water-soluble Entacapone. The purpose of this study was to improve the solubility and to enhance the brain uptake of Entacapone through an O/W microemulsion, with suitable intranasal delivery. The optimal microemulsion formulation consisted of Capmul MCM oil, Kolliphor EL: Transcutol HP (1:1) and water, with a maximum solubility of Entacapone and no ciliotoxicity, was developed and characterized. EME was characterized for % Transmittance, pH, viscosity, globule size, zeta potential, TEM, drug content with In-vitro release studies and Ex-vivo diffusion studies using Standard Franz Diffusion cell. The optimized microemulsion was found to be stable and transparent with average globule size 139.6 nm, PDI 0.272 and without showing any ciliotoxicity during its histopathological evaluation on goat nasal mucosa. The formulated Entacapone-loaded microemulsion was exhibited stable over period of 3 mo at room temperature, refrigeration temperature and elevated room temperature conditions.
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| Keyword:
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Entacapone, Intranasal Microemulsion, Ternary phase Diagram, Ex vivo diffusion
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| EOI:
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| DOI:
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https://doi.org/10.31838/ijpr/2022.14.04.002
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| Download:
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Request For Article
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