Nanobiolab, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, Brazil.
Nanostructured Systems for Overcoming Biological Barriers group of iMed, ULisboa (Research Institute for Medicines), Faculdade de Farmacia, Universidade de Lisboa, Lisboa, Portugal.
Colloids Surf B Biointerfaces. 2018 Apr 1;164:281-290. doi: 10.1016/j.colsurfb.2018.01.053. Epub 2018 Jan 31.
Wound healing involves the integration of biological and molecular events and, in case of chronic wounds, the use of drugs can be associated to side effects. Therefore, there is a search for alternatives therapeutics that encompass minimal toxicity. The use of natural compounds is an attractive approach for treating inflammatory disorders, wounds and burns. In this context, thymol has antimicrobial, antioxidant and antiseptic properties and is a promising compound in wound healing and inflammation management. However, essential oils and their constituents such as thymol present high volatility and can also easily decompose, thereby the encapsulation of these compounds into nanoparticles may be an efficient approach to modulate the release of the active ingredient, to increase the physical stability and to eventually reduce the toxicity. The aims of this work were to encapsulate thymol in nanostructured lipid carriers (NLCs) composed of natural lipids and assess its in vivo anti-inflammatory and antipsoriatic activity. The carrier containing thymol was produced by sonication method and showed 107.7 (±3.8) nm of size, zeta potential of -11.6 (±2.9) mV and entrapment efficiency of 89.1 (±4.2)%. Thymol-NLCs were incorporated into a gel and the final formulation presented rheological characteristics and pH suitable for topic application. In addition, the gel containing thymol-NLCs was tested in vivo on two different mouse models of skin inflammation, showing anti-inflammatory activity. Finally, this formulation was tested in an imiquimod-induced psoriasis mouse model and showed improved healing, compared to negative control. Therefore, thymol-NLCs is an interesting formulation for future treatment of inflammatory skin diseases.
伤口愈合涉及生物和分子事件的整合,在慢性伤口的情况下,药物的使用可能会带来副作用。因此,人们一直在寻找毒性较小的替代治疗方法。使用天然化合物是治疗炎症性疾病、伤口和烧伤的一种有吸引力的方法。在这种情况下,百里酚具有抗菌、抗氧化和防腐性能,是治疗伤口愈合和炎症管理的有前途的化合物。然而,精油及其成分(如百里酚)具有高挥发性,并且容易分解,因此将这些化合物包封在纳米颗粒中可能是一种有效的方法,可以调节活性成分的释放,提高物理稳定性,并最终降低毒性。本工作的目的是将百里酚包封在由天然脂质组成的纳米结构脂质载体(NLC)中,并评估其体内抗炎和抗银屑病活性。含有百里酚的载体通过超声法制备,粒径为 107.7(±3.8)nm,zeta 电位为-11.6(±2.9)mV,包封效率为 89.1(±4.2)%。百里酚-NLC 被掺入凝胶中,最终制剂具有适合局部应用的流变学特性和 pH 值。此外,含有百里酚-NLC 的凝胶在两种不同的皮肤炎症小鼠模型中进行了体内测试,显示出抗炎活性。最后,该制剂在咪喹莫特诱导的银屑病小鼠模型中进行了测试,与阴性对照相比,显示出更好的愈合效果。因此,百里酚-NLC 是一种有前途的治疗炎症性皮肤病的制剂。