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首页> 外文期刊>Journal of Young Pharmacists >Development and Characterization of Thermosensitive intranasal Gel Containing Paliperidone Loaded Microspheres
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Development and Characterization of Thermosensitive intranasal Gel Containing Paliperidone Loaded Microspheres

机译：含帕潘立酮微球的热敏鼻内凝胶的研制与表征

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Purpose: The objective of the present investigation was to fabricate a thermosensitive gel containing paliperidone loaded microspheres for the treatment of schizophrenia for brain delivery through nasal route. Incorporation of drug in to microspheres and then in to gel should increase the duration of release and nasal duration time respectively. Material and Method: Ethyl cellulose microspheres containing paliperidone palmitate were prepared by emulsification of ethyl acetate dispersion containing polymer and drug with aqueous external phase containing polysorbate 80. Amount of ethyl cellulose and polysorbate 80 were identified as critical formulation variables influencing the drug release at critical time points, percentage yield and particle size. These factors were studied using 2 factors and 3 level face centered factorial design using Design Expert?. Drug-excipient compatibility was ascertained using FTIR analysis. The paliperidone microspheres were then incorporated in to Pluronic F127 and HPMC gel having required thermo sensitive and muco adhesive properties. Gel containing microspheres was subjected to Ex vivo permeation study, irritation study using sheep nasal mucosa and pharmacodynamic study (spontaneous motor activity in mice). Results: Microspheres that could sustain the drug release up to 8 hours were developed. Thermoreversible gel having required thermo sensitive and muco adhesive properties was developed. The Ex vivo permeation study and pharm a codynamic study of the drug loaded microsphere containing gel confirmed the release up to 8 hours. The histopathology study showed absence of irritation on sheep nasal mucosa. Conclusion: Paliperidone palmitate loaded microspheres containing gel could prolong and target the drug release to brain and therefore give prolonged and intense action.
机译：目的：本研究的目的是制造一种含有帕潘立酮负载的微球的热敏凝胶，用于治疗精神分裂症，经鼻途径向大脑输送。将药物混入微球体，然后混入凝胶中，应分别增加释放时间和鼻腔持续时间。材料和方法：通过将含有聚合物和药物的乙酸乙酯分散液与含有聚山梨酯80的水外相乳化来制备含有帕潘立酮棕榈酸酯的乙基纤维素微球。确定了乙基纤维素和聚山梨酯80的量是影响关键时刻药物释放的关键配方变量。点，百分产率和粒度。使用Design Expert ？使用2个因子和3个以面部为中心的析因设计来研究这些因子。使用FTIR分析确定了药物-赋形剂的相容性。然后将帕潘立酮微球掺入具有所需的热敏和粘膜粘合特性的Pluronic F127和HPMC凝胶中。对含凝胶的微球体进行离体渗透研究，使用绵羊鼻黏膜的刺激性研究和药效学研究（小鼠的自发运动活性）。结果：开发了可以维持长达8小时药物释放的微球。开发了具有所需的热敏性和粘膜粘合性的热可逆凝胶。含有凝胶的载药微球的离体渗透研究和药物动力学研究证实了长达8小时的释放。组织病理学研究表明对绵羊鼻粘膜无刺激。结论：棕榈油中含有帕潘立酮棕榈酸酯的微球含有凝胶，可以延长和靶向药物释放到大脑，因此可以发挥长期而强烈的作用。

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