Department of Biochemistry, Faculty of Medicine, Medical University of Lodz, Lodz, Poland.
Department of Gastroenterological Surgery, Tenth People's Hospital of Shanghai, School of Medicine, Tongji University, Shanghai, China.
J Physiol Pharmacol. 2019 Apr;70(2). doi: 10.26402/jpp.2019.2.10. Epub 2019 Aug 20.
Crohn's Disease (CD), one of the types of inflammatory bowel disease, poses a significant challenge to modern healthcare. This condition severely impacts patients' quality of life, and its incidence is continuously rising. Despite constant research, current treatment options are limited and largely unsuccessful and result in serious side effects, therefore new therapy alternatives are needed. Liposomal formulation provides a new hope for disease management. In our study, we characterized the anti-inflammatory activity of mesalazine (5-ASA) and chlorogenic acid (CGA) encapsulated in liposomal formulation in the animal model of CD. Liposomes were obtained by thin film hydration method and characterized in terms of suspension stability and particle size and distribution. Colitis was induced in mice by intracolonic (i.c.) administration of 2,4,6-trinitrobenzenesulfonic acid (TNBS). The effect of treatment with liposomal suspensions of 5-ASA and CGA was evaluated macroscopically and by measuring myeloperoxidase (MPO) activity. We observed that liposome-encapsulated 5-ASA (5 mg/kg), but not CGA (20 mg/kg) attenuated colitis as evidenced by a decreased macroscopic and microscopic scores. It may be hypothesized that the composition of liposomal lipid bilayer as well as the switch in macrophage populations leading to unfavorable accumulation of anti-inflammatory agents in the cells may underly the efficiency of obtained liposomes and need to be taken into consideration in further studies on drug delivery.
克罗恩病（CD）是炎症性肠病的一种类型，对现代医疗保健构成重大挑战。这种疾病严重影响患者的生活质量，其发病率不断上升。尽管不断进行研究，但目前的治疗选择有限且大多不成功，并导致严重的副作用，因此需要新的治疗选择。脂质体制剂为疾病管理提供了新的希望。在我们的研究中，我们研究了包裹在脂质体中的美沙拉嗪（5-ASA）和绿原酸（CGA）在 CD 动物模型中的抗炎活性。通过薄膜水化法获得脂质体，并根据悬浮稳定性、粒径和分布对其进行了表征。通过向结肠内给予 2,4,6-三硝基苯磺酸（TNBS）诱导小鼠结肠炎。通过测量髓过氧化物酶（MPO）活性评估脂质体混悬液中 5-ASA 和 CGA 的治疗效果。我们观察到，包封在脂质体中的 5-ASA（5mg/kg），而不是 CGA（20mg/kg）减轻了结肠炎，这表现在宏观和微观评分降低。可以假设脂质体双层脂质的组成以及巨噬细胞群体的转变导致抗炎剂在细胞中的不利积累可能是所获得的脂质体的效率的基础，在进一步的药物输送研究中需要考虑这一点。
