Bonetti Flávia Monique Rocha, de Paula Eneida, Fonseca Belchiolina Beatriz, da Silva Gabriela Ribeiro, da Silva Leandro Santana Soares, de Moura Ludmilla David, Breitkreitz Márcia Cristina, Rodrigues da Silva Gustavo Henrique, de Morais Ribeiro Lígia Nunes
Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas-UNICAMP, Campinas 13083-862, SP, Brazil.
School of Veterinary Medicine, Federal University of Uberlândia-UFU, Uberlândia 38410-337, MG, Brazil.
Pharmaceutics. 2022 Mar 8;14(3):583. doi: 10.3390/pharmaceutics14030583.
The oral administration of the anti-inflammatory indomethacin (INDO) causes severe gastrointestinal side effects, which are intensified in chronic inflammatory conditions when a continuous treatment is mandatory. The development of hybrid delivery systems associates the benefits of different (nano) carriers in a single system, designed to improve the efficacy and/or minimize the toxicity of drugs. This work describes the preparation of hybrid nanobeads composed of nanostructured lipid carriers (NLC) loading INDO (2%; w/v) and chitosan, coated by xanthan. NLC formulations were monitored in a long-term stability study (25 °C). After one year, they showed suitable physicochemical properties (size < 250 nm, polydispersity < 0.2, zeta potential of −30 mV and spherical morphology) and an INDO encapsulation efficiency of 99%. The hybrid (lipid-biopolymers) nanobeads exhibited excellent compatibility between the biomaterials, as revealed by structural and thermodynamic properties, monodisperse size distribution, desirable in vitro water uptake and prolonged in vitro INDO release (26 h). The in vivo safety of hybrid nanobeads was confirmed by the chicken embryo (CE) toxicity test, considering the embryos viability, weights of CE and annexes and changes in the biochemical markers. The results point out a safe gastro-resistant pharmaceutical form for further efficacy assays.
口服抗炎药吲哚美辛（INDO）会引起严重的胃肠道副作用，在慢性炎症状态下，当必须进行持续治疗时，这些副作用会加剧。混合递送系统的开发将不同（纳米）载体的优点结合在一个单一系统中，旨在提高药物疗效和/或使药物毒性最小化。本文描述了由负载2%（w/v）INDO的纳米结构脂质载体（NLC）和壳聚糖组成、并由黄原胶包衣的混合纳米珠的制备。在长期稳定性研究（25℃）中对NLC制剂进行了监测。一年后，它们表现出合适的物理化学性质（粒径<250nm，多分散性<0.2，ζ电位为-30mV，呈球形形态）以及99%的INDO包封率。混合（脂质-生物聚合物）纳米珠在生物材料之间表现出优异的相容性，这通过结构和热力学性质、单分散尺寸分布、理想的体外吸水性以及延长的体外INDO释放（26小时）得以体现。通过鸡胚（CE）毒性试验证实了混合纳米珠的体内安全性，该试验考虑了胚胎活力、CE及其附件的重量以及生化标志物的变化。结果指出了一种安全的抗胃药物剂型，可用于进一步的疗效测定。
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