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使用载有辣椒素的纳米凝胶对成牙本质细胞样细胞中TRPV1的调节

Modulation of TRPV1 on Odontoblast-like Cells Using Capsazepine-Loaded Nanogels.

作者信息

Bernal-Cepeda Lilia Jadith, Jiménez Ronald Andrés, Velandia-Romero Myriam L, Acosta-Guzmán Paola, Castellanos Jaime E

机构信息

IBAPO Group, School of Dentistry, Universidad Nacional de Colombia, Bogota 111321, Colombia.

INQA Group, Pharmaceutical Chemistry Program, Department of Chemistry, Universidad El Bosque, Bogota 110121, Colombia.

出版信息

Pharmaceutics. 2024 Mar 3;16(3):355. doi: 10.3390/pharmaceutics16030355.

Abstract

The modulation of TRPV1 emerges as a promising strategy for dental pain management. This study aimed to assess TRPV1 modulation in a human odontoblast-like cell model using Capsazepine (CZP) loaded in a nanogel delivery system. Gelatin nanogels, synthesized via the emulsification-gelation technique, were characterized and loaded with the TRPV1 antagonist, CZP. HPLC determined a remarkable 67.5 ± 0.04% CZP loading efficiency, with 71.7% of nanogels falling within the 300-950 nm size range, as evidenced by light microscopy. Moreover, CZP-loaded nanogels had a low cytotoxicity. An FTIR analysis showed no adverse chemical interactions, ensuring stability and active release. When examining biological responses, TRPV1 expression and channel activity were assessed in odontoblast-like cells. On the fifth day post-treatment, cells treated with CZP-loaded nanogels exhibited an increased TRPV1 expression and a reduction in calcium fluxes after agonist stimulus (F/F0 ratio 1.18 ± 0.18), resembling the response in free CZP-treated cells (1.28 ± 0.15). A two-way analysis of variance and the Tukey's test were used to determine statistical significance ( < 0.05). This delivery system, proven to be economical and straightforward, holds promise for dental pain management and potential local use. Local administration minimizes systemic adverse effects, making it a practical solution for releasing molecules in the oral cavity.

摘要

TRPV1的调节成为一种有前景的牙科疼痛管理策略。本研究旨在使用负载于纳米凝胶递送系统中的辣椒素(CZP),在人成牙本质细胞样细胞模型中评估TRPV1的调节作用。通过乳化-凝胶技术合成的明胶纳米凝胶进行了表征,并负载了TRPV1拮抗剂CZP。高效液相色谱法测定CZP的负载效率显著,为67.5±0.04%,光学显微镜显示71.7%的纳米凝胶粒径在300 - 950 nm范围内。此外,负载CZP的纳米凝胶具有低细胞毒性。傅里叶变换红外光谱分析表明不存在不良化学相互作用,确保了稳定性和活性释放。在检查生物学反应时,评估了成牙本质细胞样细胞中的TRPV1表达和通道活性。在处理后的第五天,用负载CZP的纳米凝胶处理的细胞在激动剂刺激后表现出TRPV1表达增加和钙通量降低(F/F0比值为1.18±0.18),类似于游离CZP处理细胞的反应(1.28±0.15)。采用双向方差分析和Tukey检验确定统计学显著性(<0.05)。这种递送系统经证明经济且简便,在牙科疼痛管理和潜在局部应用方面具有前景。局部给药可将全身不良反应降至最低,使其成为在口腔中释放分子的实用解决方案。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c15/10975074/1703224b268e/pharmaceutics-16-00355-g001.jpg

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