Bernal-Cepeda Lilia Jadith, Jiménez Ronald Andrés, Velandia-Romero Myriam L, Acosta-Guzmán Paola, Castellanos Jaime E
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.
Pharmaceutics. 2024 Mar 3;16(3):355. doi: 10.3390/pharmaceutics16030355.
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.
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。