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原位凝胶地塞米松口腔黏膜制剂:影响药物递送的物理特性

In Situ Gelling Dexamethasone Oromucosal Formulation: Physical Characteristics Influencing Drug Delivery.

作者信息

Krchňák Daniel, Balážová Ľudmila, Hanko Michal, Žigrayová Dominika, Špaglová Miroslava

机构信息

Department of Galenic Pharmacy, Faculty of Pharmacy, Comenius University Bratislava, Odbojárov 10, SK-832 32 Bratislava, Slovakia.

Department of Pharmaceutical Technology, Pharmacognosy and Botany, University of Veterinary Medicine and Pharmacy in Košice, Komenského 73, SK-041 81 Kosice, Slovakia.

出版信息

Gels. 2025 Jan 2;11(1):26. doi: 10.3390/gels11010026.

Abstract

The study focuses on the development of an in situ gelling dexamethasone (DEX) oromucosal formulation designed for the treatment of aphthous stomatitis. Three series of formulations were prepared; a first series containing DEX suspended, a second series containing DEX and, in addition, mint essential oil (EO), and a third series containing EO and DEX solubilized in propylene glycol (PG). In the composition, polymers in the role of mucoadhesive agent were interchanged (hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), hydroxyethyl cellulose (HEC), methyl cellulose (MC), carboxymethyl cellulose (CMC), and sodium carboxymethyl cellulose (NaCMC). Specifically, DEX was incorporated at a concentration of 0.1% (/) in each formulation. The influence of mint EO and DEX solubilization on the physical properties (pH measurements, rheological analysis, swelling ability, and texture analysis) and in vitro drug release was studied. Key findings revealed that HPMC-based formulation containing mint EO and PG exhibited best swelling properties (700 ± 46% after 5 h), adequate adhesiveness and in vitro drug release (34.7 ± 5.9%). Furthermore, the irritation potential assessed via the hen's egg test on the chorioallantoic membrane (HET-CAM) demonstrated low irritancy risk. Finally, Fourier-transform infrared spectroscopy (FT-IR) showed no incompatibility between DEX and excipients. Overall, the research highlights the potential of mucoadhesive systems in improving the therapeutic efficacy of oromucosal drug delivery for managing painful oral lesions.

摘要

该研究聚焦于开发一种用于治疗复发性口腔溃疡的原位凝胶地塞米松(DEX)口腔黏膜制剂。制备了三个系列的制剂:第一个系列含有悬浮的DEX,第二个系列含有DEX以及薄荷精油(EO),第三个系列含有溶解在丙二醇(PG)中的EO和DEX。在配方中,作为黏膜黏附剂的聚合物进行了互换(羟丙基甲基纤维素(HPMC)、羟丙基纤维素(HPC)、羟乙基纤维素(HEC)、甲基纤维素(MC)、羧甲基纤维素(CMC)和羧甲基纤维素钠(NaCMC))。具体而言,每个制剂中DEX的掺入浓度为0.1%(/)。研究了薄荷EO和DEX溶解对物理性质(pH测量、流变学分析、溶胀能力和质地分析)以及体外药物释放的影响。主要研究结果表明,含有薄荷EO和PG的基于HPMC的制剂表现出最佳的溶胀性能(5小时后为700±46%)、足够的黏附性和体外药物释放(34.7±5.9%)。此外,通过鸡胚绒毛尿囊膜试验(HET-CAM)评估的刺激潜力表明刺激风险较低。最后,傅里叶变换红外光谱(FT-IR)显示DEX与辅料之间不存在不相容性。总体而言,该研究突出了黏膜黏附系统在提高口腔黏膜给药治疗疼痛性口腔病变疗效方面的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2be6/11765448/fdcb9388e166/gels-11-00026-g001.jpg

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