de Oliveira Maísa Soares, Oshiro-Junior João Augusto, Sato Mariana Rillo, Conceição Marta Maria, Medeiros Ana Cláudia Dantas
Laboratório de Desenvolvimento e Ensaios de Medicamentos, Centro de Ciências Biológicas e da Saúde, Universidade Estadual da Paraíba, R. Baraúnas, 351, Cidade Universitária, 58429-500 Campina Grande, Paraíba, Brasil.
Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista Júlio de Mesquita Filho, Araraquara-Jaú, 14.800-903 Km 1 Araraquara, São Paulo, Brazil.
Pharmaceutics. 2020 Jul 23;12(8):695. doi: 10.3390/pharmaceutics12080695.
Bacterial resistance has become an important public health problem. Bacteria have been acquiring mechanisms to resist the action of antimicrobial active pharmaceutical ingredients (API). Based on this, a promising alternative is the use of nanotechnology, since when the systems are presented in nanometric size, there is an increase in the interaction and concentration of the action at the target site improving the activity. Thus, this study aims to develop a polymeric nanoparticle (PN) composed of chitosan and hydroxypropylmethylcellulose, as an innovative strategy for the administration of an association between ceftriaxone and extract of , for the treatment of Enterobacteriaceae. From a Box-Behnken design, nanoparticles were obtained and evaluated using the DLS technique, obtaining the particle size between 440 and 1660 nm, IPD from 0.42 to 0.92, and positive charges. Morphological characteristics of PN by SEM revealed spherical morphology and sizes similar to DLS. Infrared spectroscopy showed no chemical interaction between the components of the formulation. The broth microdilution technique evaluated their antimicrobial activity, and a considerable improvement in the activity of the extract and the API compared to the free compounds was found, reaching an improvement of 133 times in the minimum inhibitory activity CRO.
细菌耐药性已成为一个重要的公共卫生问题。细菌一直在获得抵抗抗菌活性药物成分（API）作用的机制。基于此，一个有前景的替代方法是使用纳米技术，因为当系统呈现纳米尺寸时，在靶位点的相互作用和作用浓度会增加，从而提高活性。因此，本研究旨在开发一种由壳聚糖和羟丙基甲基纤维素组成的聚合物纳米颗粒（PN），作为一种创新策略，用于联合给药头孢曲松和[提取物名称缺失]提取物，以治疗肠杆菌科细菌。通过Box-Behnken设计获得纳米颗粒，并使用DLS技术进行评估，得到的粒径在440至1660nm之间，IPD为0.42至0.92，且带正电荷。通过扫描电子显微镜（SEM）观察PN的形态特征，显示出球形形态且尺寸与DLS结果相似。红外光谱表明制剂各成分之间没有化学相互作用。采用肉汤微量稀释技术评估其抗菌活性，结果发现与游离化合物相比，提取物和API的活性有显著提高，头孢曲松的最低抑菌活性提高了133倍。
