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基于微乳的黏膜黏附型颊片:颊片成型、体外释放和离体评价。

Microemulsion-Based Mucoadhesive Buccal Wafers: Wafer Formation, In Vitro Release, and Ex Vivo Evaluation.

机构信息

Pharmaceutical Engineering Laboratory, Biomedical Engineering Department, International University, Vietnam National University, Ho Chi Minh City, Vietnam.

Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, Vietnam.

出版信息

AAPS PharmSciTech. 2017 Oct;18(7):2727-2736. doi: 10.1208/s12249-017-0754-9. Epub 2017 Mar 15.

Abstract

Microemulsion has the potentials to enhance dissolution as well as facilitate absorption and permeation of poorly water-soluble drugs through biological membranes. However, its application to govern a controlled release buccal delivery for local treatment has not been discovered. The aim of this study is to develop microemulsion-based mucoadhesive wafers for buccal delivery based on an incorporation of the microemulsion with mucoadhesive agents and mannitol. Ratio of oil to surfactant to water in the microemulsion significantly impacted quality of the wafers. Furthermore, the combination of carbopol and mannitol played a key role in forming the desired buccal wafers. The addition of an extra 50% of water to the formulation was suitable for wafer formation by freeze-drying, which affected the appearance and distribution of carbopol in the wafers. The amount of carbopol was critical for the enhancement of mucoadhesive properties and the sustained drug release patterns. Release study presented a significant improvement of the drug release profile following sustained release for 6 h. Ex vivo mucoadhesive studies provided decisive evidence to the increased retention time of wafers along with the increased carbopol content. The success of this study indicates an encouraging strategy to formulate a controlled drug delivery system by incorporating microemulsions into mucoadhesive wafers.

摘要

微乳液具有提高难溶性药物溶解性能以及促进其透过生物膜吸收和渗透的潜力。然而,将其应用于控制局部治疗的口腔释放尚未被发现。本研究旨在开发基于微乳液的粘膜粘附型口腔贴片,将微乳液与粘膜粘附剂和甘露醇结合使用。微乳液中油、表面活性剂和水的比例对贴片的质量有显著影响。此外,卡波姆和甘露醇的组合在形成所需的口腔贴片方面起着关键作用。制剂中额外添加 50%的水适合冷冻干燥形成贴片,这会影响卡波姆在贴片中的外观和分布。卡波姆的用量对于增强粘膜粘附性能和持续释放药物模式至关重要。释放研究表明,药物释放曲线在持续释放 6 小时后得到显著改善。离体粘膜粘附研究提供了决定性的证据,表明随着卡波姆含量的增加,贴片的滞留时间延长。这项研究的成功表明,通过将微乳液纳入粘膜粘附贴片来构建控制药物释放系统是一种很有前途的策略。

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