Garcia Maíra Terra, Carmo Paulo Henrique Fonseca do, Figueiredo-Godoi Lívia Mara Alves, Gonçalves Natália Inês, Lima Patrícia Michelle Nagai de, Ramos Lucas de Paula, Oliveira Luciane Dias de, Borges Alexandre Luiz Souto, Shukla Anita, Junqueira Juliana Campos
Department of Biosciences and Oral Diagnosis, Institute of Science and Technology, São Paulo State University (UNESP), São José dos Campos 12245-000, SP, Brazil.
Department of Dental Materials and Prosthodontics, Institute of Science and Technology, São Paulo State University (UNESP), São José dos Campos 12245-000, SP, Brazil.
Pharmaceutics. 2024 Feb 20;16(3):298. doi: 10.3390/pharmaceutics16030298.
can cause various types of oral infections, mainly associated with denture stomatitis. Conventional therapy has been linked to high recurrence, toxicity, and fungal resistance, necessitating the search for new drugs and delivery systems. In this study, caffeic acid phenethyl ester (CAPE) and gellan gum (GG) were studied as an antifungal agent and carrier system, respectively. First, we observed that different GG formulations (0.6 to 1.0% wt/vol) were able to incorporate and release CAPE, reaching a controlled and prolonged release over 180 min at 1.0% of GG. CAPE-GG formulations exhibited antifungal activity at CAPE concentrations ranging from 128 to >512 µg/mL. Furthermore, CAPE-GG formulations significantly decreased the fungal viability of biofilms at short times (12 h), mainly at 1.0% of GG ( < 0.001). protease activity was also reduced after 12 h of treatment with CAPE-GG formulations ( < 0.001). Importantly, CAPE was not cytotoxic to human keratinocytes, and CAPE-GG formulations at 1.0% decreased the fungal burden ( = 0.0087) and suppressed inflammation in a rat model of denture stomatitis. Altogether, these results indicate that GG is a promising delivery system for CAPE, showing effective activity against and potential to be used in the treatment of denture stomatitis.
可引起多种类型的口腔感染，主要与义齿性口炎相关。传统疗法与高复发率、毒性和真菌耐药性有关，因此需要寻找新的药物和给药系统。在本研究中，分别研究了咖啡酸苯乙酯（CAPE）和结冷胶（GG）作为抗真菌剂和载体系统。首先，我们观察到不同的GG制剂（0.6至1.0%重量/体积）能够包载并释放CAPE，在1.0%的GG时在180分钟内实现控释和缓释。CAPE-GG制剂在CAPE浓度为128至>512 µg/mL范围内表现出抗真菌活性。此外，CAPE-GG制剂在短时间（12小时）内显著降低了生物膜的真菌活力，主要是在1.0%的GG时（<0.001）。用CAPE-GG制剂处理12小时后蛋白酶活性也降低了（<0.001）。重要的是，CAPE对人角质形成细胞无细胞毒性，1.0%的CAPE-GG制剂降低了真菌负荷（=0.0087）并抑制了义齿性口炎大鼠模型中的炎症。总之，这些结果表明GG是一种有前景的CAPE给药系统，对[此处原文缺失相关真菌名称]显示出有效活性并有潜力用于义齿性口炎的治疗。
