基于不同电荷β-环糊精的美洛昔康钾鼻用粉剂的配制与研究

IF 4.3 3区 医学 Q1 PHARMACOLOGY & PHARMACY European Journal of Pharmaceutical Sciences Pub Date : 2024-08-16 DOI:10.1016/j.ejps.2024.106879
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引用次数: 0

摘要

鼻腔给药是替代肠外给药或口服给药的一种简便方法,但辅料在鼻腔制剂中具有重要作用,可增加粘膜的渗透性并延长药物的停留时间。在这项研究中,我们的目标是利用纳米喷雾干燥器,以中性、阴离子和阳离子β-环糊精作为渗透促进剂,以(聚乙烯醇)作为水溶性聚合物,生产出含有一水美洛昔康钾(MXP)的鼻腔粉剂。为了研究辅料对配方鼻腔适用性的影响,我们进行了以下检查:激光散射、扫描电子显微镜测量、XRPD、DSC 和傅立叶变换红外光谱测量、粘附性、体外药物释放和通过人工膜和 RPMI 2650 细胞的渗透性测试。根据我们的研究结果,制备出了尺寸为 1.89-2.21 微米的球形颗粒,其中 MXP 以无定形状态存在。辅料与药物之间形成了次级相互作用。无论是否存在 PVA,带电的环糊精制剂都显示出明显更高的粘附力值。药物释放快速而完全。MXP 的被动扩散不仅受到环糊精电荷的影响,还受到 PVA 存在的影响。在 RPMI 2650 细胞模型上测试发现,阴离子环糊精的存在增强了药物的渗透性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Formulation and investigation of differently charged β-cyclodextrin-based meloxicam potassium containing nasal powders

Nasal systemic drug delivery may provide an easy way to substitute parenteral or oral dosing, however, the excipients have an important role in nasal formulations to increase the permeability of the mucosa and prolong the residence time of the drug. In this work, we aimed to produce meloxicam potassium monohydrate (MXP) containing nasal powders by a nano spray drier with the use of a neutral, an anionic and a cationic β-cyclodextrin as permeation enhancers, and (polyvinyl)alcohol (PVA) as a water soluble polymer. The following examinations were performed in order to study the effect of the applied excipients on the nasal applicability of the formulations: laser scattering, scanning electron microscope measurement, XRPD, DSC and FTIR measurements, adhesivity, in vitro drug release and permeability tests through an artificial membrane and RPMI 2650 cells. Based on our results, spherical particles were prepared with a size of 1.89–2.21 µm in which MXP was present in an amorphous state. Secondary interactions were formed between the excipients and the drug. The charged cyclodextrin-based formulations showed significantly higher adhesive force values regardless of the presence of PVA. The drug release was fast and complete. The passive diffusion of MXP was influenced not only by the charge of the cyclodextrin, but the presence of PVA, too. The permeation of the drug was enhanced in the presence of the anionic cyclodextrin testing it on RPMI 2650 cell model.

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来源期刊
CiteScore
9.60
自引率
2.20%
发文量
248
审稿时长
50 days
期刊介绍: The journal publishes research articles, review articles and scientific commentaries on all aspects of the pharmaceutical sciences with emphasis on conceptual novelty and scientific quality. The Editors welcome articles in this multidisciplinary field, with a focus on topics relevant for drug discovery and development. More specifically, the Journal publishes reports on medicinal chemistry, pharmacology, drug absorption and metabolism, pharmacokinetics and pharmacodynamics, pharmaceutical and biomedical analysis, drug delivery (including gene delivery), drug targeting, pharmaceutical technology, pharmaceutical biotechnology and clinical drug evaluation. The journal will typically not give priority to manuscripts focusing primarily on organic synthesis, natural products, adaptation of analytical approaches, or discussions pertaining to drug policy making. Scientific commentaries and review articles are generally by invitation only or by consent of the Editors. Proceedings of scientific meetings may be published as special issues or supplements to the Journal.
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