Niu Jiangxiu, Yuan Ming, Gao Panpan, Wang Liye, Qi Yueheng, Chen Jingjing, Bai Kaiyue, Fan Yanli, Liu Xianming
College of Food and Drug, Luoyang Normal University, Luoyang 471934, China.
Gels. 2023 Jul 21;9(7):587. doi: 10.3390/gels9070587.
Curcumin (Cur) is a kind of polyphenol with a variety of topical pharmacological properties including antioxidant, analgesic and anti-inflammatory activities. However, its low water solubility and poor skin bioavailability limit its effectiveness. In the current study, we aimed to develop microemulsion-based keratin-chitosan gel for the improvement of the topical activity of Cur. The curcumin-loaded microemulsion (CME) was formulated and then loaded into the keratin-chitosan (KCS) gel to form the CME-KCS gel. The formulated CME-KCS gel was evaluated for its characterization, in vitro release, in vitro skin permeation and in vivo activity. The results showed that the developed CME-KCS gel had an orange-yellow and gel-like appearance. The particle size and zeta potential of the CME-KCS gel were 186.45 ± 0.75 nm and 9.42 ± 0.86 mV, respectively. The CME-KCS gel showed desirable viscoelasticity, spreadability, bioadhesion and controlled drug release, which was suitable for topical application. The in vitro skin permeation and retention study showed that the CME-KCS gel had better in vitro skin penetration than the Cur solution and achieved maximum skin drug retention (3.75 ± 0.24 μg/cm). In vivo experimental results confirmed that the CME-KCS gel was more effective than curcumin-loaded microemulsion (Cur-ME) in analgesic and anti-inflammatory activities. In addition, the CME-KCS gel did not cause any erythema or edema based on a mice skin irritation test. These findings indicated that the developed CME-KCS gel could improve the skin penetration and retention of Cur and could become a promising formulation for topical delivery to treat local diseases.
姜黄素(Cur)是一种具有多种局部药理特性的多酚,包括抗氧化、镇痛和抗炎活性。然而,其低水溶性和较差的皮肤生物利用度限制了其有效性。在本研究中,我们旨在开发基于微乳液的角蛋白-壳聚糖凝胶,以提高姜黄素的局部活性。制备了负载姜黄素的微乳液(CME),然后将其负载到角蛋白-壳聚糖(KCS)凝胶中,形成CME-KCS凝胶。对制备的CME-KCS凝胶进行了表征、体外释放、体外皮肤渗透和体内活性评价。结果表明,所制备的CME-KCS凝胶呈橙黄色凝胶状外观。CME-KCS凝胶的粒径和zeta电位分别为186.45±0.75nm和9.42±0.86mV。CME-KCS凝胶具有理想的粘弹性、铺展性、生物粘附性和控释性,适用于局部应用。体外皮肤渗透和滞留研究表明,CME-KCS凝胶比姜黄素溶液具有更好的体外皮肤渗透性,并实现了最大的皮肤药物滞留量(3.75±0.24μg/cm)。体内实验结果证实,CME-KCS凝胶在镇痛和抗炎活性方面比负载姜黄素的微乳液(Cur-ME)更有效。此外,基于小鼠皮肤刺激性试验,CME-KCS凝胶未引起任何红斑或水肿。这些发现表明,所开发的CME-KCS凝胶可以提高姜黄素的皮肤渗透性和滞留性,并有望成为治疗局部疾病的局部给药制剂。