Miastkowska Małgorzata, Kulawik-Pióro Agnieszka, Lasoń Elwira, Śliwa Karolina, Malinowska Magdalena Anna, Sikora Elżbieta, Kantyka Tomasz, Bielecka Ewa, Maksylewicz Anna, Klimaszewska Emilia, Ogorzałek Marta, Tabaszewska Małgorzata, Skoczylas Łukasz, Nowak Krzysztof
Department of Organic Chemistry and Technology, Faculty of Chemical Engineering and Technology, Cracow University of Technology, Warszawska 24, 31-155 Cracow, Poland.
Malopolska Centre of Biotechnology, Jagiellonian University, 30-387 Cracow, Poland.
Pharmaceutics. 2023 Oct 31;15(11):2559. doi: 10.3390/pharmaceutics15112559.
is a chronic disorder that causes a rash with itchy, scaly patches. It affects nearly 2-5% of the worldwide population and has a negative effect on patient quality of life. A variety of therapeutic approaches, e.g., glucocorticoid topical therapy, have shown limited efficacy with systemic adverse reactions. Therefore, novel therapeutic agents and physicochemical formulations are in constant need and should be obtained and tested in terms of effectiveness and minimization of side effects. For that reason, the aim of our study was to design and obtain various hybrid systems, nanoemulgel-macroemulsion and nanoemulgel-oleogel (bigel), as vehicles for ursolic acid (UA) and to verify their potential as topical formulations used in psoriasis treatment. Obtained topical formulations were characterized by conducting morphological, rheological, texture, and stability analysis. To determine the safety and effectiveness of the prepared ursolic acid carriers, in vitro studies on human keratinocyte cell-like HaCaT cells were performed with cytotoxicity analysis for individual components and each formulation. Moreover, a kinetic study of ursolic acid release from the obtained systems was conducted. All of the studied UA-loaded systems were well tolerated by keratinocyte cells and had suitable pH values and stability over time. The obtained formulations exhibit an apparent viscosity, ensuring the appropriate time of contact with the skin, ease of spreading, soft consistency, and adherence to the skin, which was confirmed by texture tests. The release of ursolic acid from each of the formulations is followed by a slow, controlled release according to the Korsmeyer-Peppas and Higuchi models. The elaborated systems could be considered suitable vehicles to deliver triterpene to psoriatic skin.
是一种慢性疾病,会导致出现伴有瘙痒、鳞屑斑块的皮疹。它影响着全球近2% - 5%的人口,对患者的生活质量有负面影响。多种治疗方法,如糖皮质激素局部治疗,已显示出疗效有限且伴有全身不良反应。因此,一直需要新型治疗药物和物理化学制剂,并且应该根据有效性和副作用最小化来获取和测试它们。出于这个原因,我们研究的目的是设计并获得各种混合体系,即纳米乳凝胶 - 宏观乳液和纳米乳凝胶 - 油凝胶(双凝胶),作为熊果酸(UA)的载体,并验证它们作为用于银屑病治疗的局部制剂的潜力。通过进行形态学、流变学、质地和稳定性分析来表征所获得的局部制剂。为了确定所制备的熊果酸载体的安全性和有效性,对人角质形成细胞样HaCaT细胞进行了体外研究,并对各个成分和每种制剂进行了细胞毒性分析。此外,还对所获得体系中熊果酸的释放进行了动力学研究。所有研究的负载UA的体系均被角质形成细胞良好耐受,并且具有合适的pH值和随时间的稳定性。通过质地测试证实,所获得的制剂表现出表观粘度,确保了与皮肤接触的适当时间、易于铺展、质地柔软以及对皮肤的粘附性。根据Korsmeyer - Peppas和Higuchi模型,每种制剂中熊果酸的释放均呈现缓慢、可控的释放。所精心设计的体系可被认为是向银屑病皮肤递送三萜类化合物的合适载体。