Laboratory of Neurobiology, Department of Biology, Faculty of Chemistry and Biology, University of Santiago of Chile, Santiago, Chile.
Vicerrectory of Research, Development and Innovation, University of Santiago of Chile, Santiago, Chile.
PLoS One. 2018 Apr 12;13(4):e0187473. doi: 10.1371/journal.pone.0187473. eCollection 2018.
Pain is a sensory experience of a complex physiological nature in which is not only involved the nervous system. Among its many features is the development of chronic pain that is more complicated to treat because of the central somatization processes involved, becoming inefficient treatments used in other forms of pain. Among them is the role of glial cells, whose participation is such that some authors have proposed to chronic pain as a gliopathy. Because of this, the drug target of possible treatments focuses on modulating nociceptive response affecting transduction into the central nervous system through affecting synapses in the dorsal horn of the spinal cord. Solid lipid nanoparticles enter the central nervous system, protecting the drug, and in addition to the advantage of having greater absorption surface, all factors that improve drug activity. This work is based on the development and characterization of lipid nanoparticles of solid phase incorporating two antibiotics, minocycline, and ciprofloxacin with antinociceptive properties and challenged them with a rat monoarthritis model using Sprague-Dawley adult male rats. The solid lipid nanoparticles were prepared to modify the lipid, and surfactant amounts to obtain the best encapsulation capacity of the antibiotics, size and z potential. By using the Randall-Selitto test, we measured its pharmacological efficiency as an anti-inflammatory and measuring the time span the antibiotics are active. The encapsulated antibiotics were at least 50% more efficient than the antibiotic alone, and that is possible to measure anti-inflammatory activity up to seven days after the antibiotic application. The former is important for example, in the veterinary field, since a single application of the antibiotic will be necessary for the complete treatment, avoiding excessive stress for the animals. We can conclude that antinociceptive antibiotics encapsulation is a very effective, environmentally safe and inexpensive method for improving the pharmacological efficiency and time span the antibiotics are acting. Since these antibiotics are both anti-microbial and antinociceptive, his use in the field of veterinary presents the advantage of being adequate in single doses, with the saving of time and stress to the animals under treatment.
疼痛是一种复杂的生理感觉体验，不仅涉及神经系统。其众多特征之一是慢性疼痛的发展，由于涉及中枢躯体化过程，这种疼痛更难治疗，成为治疗其他形式疼痛无效的方法。其中涉及神经胶质细胞的作用，一些作者已经提出将慢性疼痛视为神经胶质病。正因为如此，可能的治疗药物靶点集中在调节伤害感受反应上，通过影响脊髓背角中的突触来影响传入中枢神经系统。固体脂质纳米粒进入中枢神经系统，保护药物，此外还具有更大的吸收表面的优势，所有这些因素都提高了药物的活性。这项工作基于开发和表征包含两种具有镇痛特性的抗生素米诺环素和环丙沙星的固相固体脂质纳米粒，并使用 Sprague-Dawley 成年雄性大鼠的单关节炎模型对其进行了挑战。固体脂质纳米粒的制备是为了修饰脂质和表面活性剂的用量，以获得抗生素的最佳包封能力、粒径和 z 电位。通过使用 Randall-Selitto 测试，我们测量了其作为抗炎药的药理效率，并测量了抗生素的作用时间。包封的抗生素的效率至少比单独使用抗生素高 50%，并且可以在抗生素应用后长达七天测量抗炎活性。这在兽医领域很重要，因为单次应用抗生素将是完全治疗的必要条件，避免了动物的过度应激。我们可以得出结论，镇痛抗生素的包封是一种非常有效、环保且廉价的方法，可以提高抗生素的药理效率和作用时间。由于这些抗生素既有抗菌作用又有镇痛作用，因此在兽医领域的使用具有单次剂量足够、节省时间和减少治疗动物压力的优势。
