Enhancing Buccal Drug Delivery: The Impact of Glycerol in Slot-Die-Coated Pectin Films.

IF 4.5 2区 医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL Molecular Pharmaceutics Pub Date : 2025-01-06 Epub Date: 2024-12-17 DOI:10.1021/acs.molpharmaceut.4c01051
Eleftheria Pantazoglou, Matteo Tollemeto, Nazanin Zanjanizadeh Ezazi, Tien-Jen Chang, Leticia Hosta Rigau, Jette Jacobsen, Line Hagner Nielsen
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Abstract

Buccal delivery offers a promising alternative to e.g., oral or parenteral drug administrations by leveraging the mucosal membranes of the mouth to enhance drug absorption and enhance patient compliance. Buccal films offer a promising approach for enhancing drug delivery by utilizing the mucoadhesive properties of the biopolymer pectin and glycerol's plasticizing effects. Designed to provide fast drug release, these films address the challenges of patient compliance, particularly among the elderly, children, and individuals with dysphagia. This study characterized the physicochemical properties of slot-die-coated films with pectin containing varying amounts of glycerol, including swelling behavior, disintegration rate, mechanical properties, mucoadhesion, and drug release profiles, using paracetamol as a model drug. Different methods such as quartz crystal microbalance with dissipation and open-source force analyzer were employed for the characterization. The results demonstrated that a high glycerol content in the films led to slower drug release with 95% paracetamol released for film without glycerol (GLY0) compared to only 74% released for film with 20% w/v glycerol (GLY20) after 60 min Additionally, higher glycerol levels resulted in enhanced mucoadhesive properties. Films containing 20% glycerol also showed superior permeability of paracetamol through ex vivo porcine buccal mucosa, with double the amount of paracetamol permeating in the first 120 min from GLY20 films compared to GLY0 films. These findings suggest that the pectin-glycerol buccal films, fabricated with slot-die coating as a novel technique, are user-friendly, exhibit interaction with the mucosa, and can be adjusted for specific disintegration and drug release rates, presenting a promising option for efficient, targeted drug delivery.

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加强口腔药物输送:甘油对开槽模涂覆果胶薄膜的影响。
口腔给药是口服或肠外给药的一种很有前途的替代方法,它利用口腔粘膜来增强药物吸收并提高患者的依从性。口腔膜利用生物聚合物果胶的黏附特性和甘油的塑化作用,为增强药物传递提供了一种很有前途的方法。这些影片旨在提供快速药物释放,解决患者依从性的挑战,特别是在老年人,儿童和吞咽困难的个体中。本研究以扑热息痛为模型药物,表征了含有不同数量甘油的果胶的槽模覆膜的物理化学性质,包括膨胀行为、崩解速率、机械性能、黏附性和药物释放谱。采用了石英晶体耗散微天平和开源力分析仪等不同的方法进行表征。结果表明,高甘油含量导致药物释放较慢,不含甘油(GLY0)的膜释放95%,而含20% w/v甘油(GLY20)的膜在60分钟后仅释放74%。此外,高甘油含量导致黏附性能增强。含20%甘油的膜对扑热息痛通过离体猪口腔粘膜的渗透性也较好,GLY20膜在前120分钟内对扑热息痛的渗透性是GLY0膜的两倍。这些发现表明,用槽模涂层制备的果胶-甘油口腔膜是一种新颖的技术,具有用户友好性,与粘膜相互作用,可以根据特定的崩解和药物释放率进行调整,为有效的靶向药物递送提供了一个有希望的选择。
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来源期刊
Molecular Pharmaceutics
Molecular Pharmaceutics 医学-药学
CiteScore
8.00
自引率
6.10%
发文量
391
审稿时长
2 months
期刊介绍: Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems. The journal encourages contributions describing research at the interface of drug discovery and drug development. Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. Mechanistic Drug Delivery and Drug Targeting research on modulating activity and efficacy of a drug or drug product is within the scope of Molecular Pharmaceutics. Theoretical and experimental peer-reviewed research articles, communications, reviews, and perspectives are welcomed.
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