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载利多卡因薄膜中的硝酸咪康唑微粒用于治疗口腔念珠菌病

Miconazole Nitrate Microparticles in Lidocaine Loaded Films as a Treatment for Oropharyngeal Candidiasis.

作者信息

Tejada Guillermo, Calvo Natalia L, Morri Mauro, Sortino Maximiliano, Lamas Celina, Álvarez Vera A, Leonardi Darío

机构信息

Grupo Materiales Compuestos Termoplásticos, Instituto de Investigaciones en Ciencia y Tecnología de Materiales, Av. Colón 10850, Mar Del Plata 7600, Argentina.

Instituto de Química Rosario, Suipacha 570, Rosario 2000, Argentina.

出版信息

Materials (Basel). 2023 May 7;16(9):3586. doi: 10.3390/ma16093586.

Abstract

Oral candidiasis is an opportunistic infection that affects mainly individuals with weakened immune system. Devices used in the oral area to treat this condition include buccal films, which present advantages over both oral tablets and gels. Since candidiasis causes pain, burning, and itching, the purpose of this work was to develop buccal films loaded with both lidocaine (anesthetic) and miconazole nitrate (MN, antifungal) to treat this pathology topically. MN was loaded in microparticles based on different natural polymers, and then, these microparticles were loaded in hydroxypropyl methylcellulose-gelatin-based films containing lidocaine. All developed films showed adequate adhesiveness and thickness. DSC and XRD tests suggested that the drugs were in an amorphous state in the therapeutic systems. Microparticles based on chitosan-alginate showed the highest MN encapsulation. Among the films, those containing the mentioned microparticles presented the highest tensile strength and the lowest elongation at break, possibly due to the strong interactions between both polymers. These films allowed a fast release of lidocaine and a controlled release of MN. Due to the latter, these systems showed antifungal activity for 24 h. Therefore, the treatment of oropharyngeal candidiasis with these films could reduce the number of daily applications with respect to conventional treatments.

摘要

口腔念珠菌病是一种机会性感染,主要影响免疫系统较弱的个体。用于口腔治疗这种病症的器械包括口腔贴膜,其相对于口服片剂和凝胶剂具有优势。由于念珠菌病会引起疼痛、灼烧感和瘙痒,本研究的目的是开发同时负载利多卡因(麻醉剂)和硝酸咪康唑(MN,抗真菌剂)的口腔贴膜,以局部治疗这种病症。MN被负载于基于不同天然聚合物的微粒中,然后将这些微粒负载于含有利多卡因的羟丙基甲基纤维素-明胶基薄膜中。所有制备的薄膜均表现出足够的粘附性和厚度。差示扫描量热法(DSC)和X射线衍射(XRD)测试表明,药物在治疗体系中呈无定形状态。基于壳聚糖-海藻酸盐的微粒显示出最高的MN包封率。在这些薄膜中,含有上述微粒的薄膜具有最高的拉伸强度和最低的断裂伸长率,这可能是由于两种聚合物之间的强相互作用。这些薄膜可实现利多卡因的快速释放和MN的控释。由于后者,这些体系显示出24小时的抗真菌活性。因此,用这些薄膜治疗口腔念珠菌病相对于传统治疗方法可减少每日用药次数。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d621/10180309/a461294dff14/materials-16-03586-g001.jpg

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