Divya G, Panonnummal Rajitha, Gupta Swati, Jayakumar R, Sabitha M
Amrita School of Pharmacy, Amrita Institute of Medical Sciences and Research Centre, Amrita Vishwa Vidyapeetham, Amrita University, Kochi 682041, India.
Amrita Centre for Nanosciences and Molecular Medicine, Amrita Institute of Medical Sciences and Research Centre, Amrita Vishwa Vidyapeetham, Amrita University, Kochi 682041, India.
Eur J Pharm Biopharm. 2016 Oct;107:97-109. doi: 10.1016/j.ejpb.2016.06.019. Epub 2016 Jun 28.
The present study focuses on the development of an effective topical nanogel formulation of two anti-psoriatic drugs; Acitretin (Act) and Aloe-emodin (AE) using natural polymer chitin. Simple regeneration chemistry was used to prepare Chitin Nanogel Systems (CNGs). The developed control chitin (CNGs) nanogels, acitretin loaded chitin nanogels (ActCNGs) and aloe-emodin loaded chitin nanogels (AECNGs) were characterized by DLS, SEM, FTIR, XRD and TG-DTA. The systems were found to be spherical in shape with a size range of 98±10, 138±8 and 238±6nm having zeta potential values of +28±3, +27±3 and +25±6mV for CNGs, ActCNGs and AECNGs respectively. The in vitro haemolysis assay revealed that all the nanogel systems are blood compatible. The systems exhibited higher swelling and release at acidic pH. The ex vivo skin permeation studies using porcine skin confirmed the higher deposition of the systems at epidermal and dermal layers, which was confirmed further by fluorescent imaging. The in vivo anti-psoriatic activity study using Perry's mouse tail model and skin safety studies confirmed the potential benefit of the system for topical delivery of acitretin and aloe-emodin in psoriasis.
本研究聚焦于使用天然聚合物几丁质开发两种抗银屑病药物阿维A(Act)和芦荟大黄素(AE)的有效局部纳米凝胶制剂。采用简单的再生化学方法制备几丁质纳米凝胶系统(CNGs)。通过动态光散射(DLS)、扫描电子显微镜(SEM)、傅里叶变换红外光谱(FTIR)、X射线衍射(XRD)和热重-差示热分析(TG-DTA)对所开发的对照几丁质(CNGs)纳米凝胶、载阿维A几丁质纳米凝胶(ActCNGs)和载芦荟大黄素几丁质纳米凝胶(AECNGs)进行了表征。发现这些系统呈球形,尺寸范围分别为98±10、138±8和238±6nm,CNGs、ActCNGs和AECNGs的zeta电位值分别为+28±3、+27±3和+25±6mV。体外溶血试验表明,所有纳米凝胶系统都具有血液相容性。这些系统在酸性pH下表现出更高的溶胀和释放。使用猪皮进行的离体皮肤渗透研究证实了这些系统在表皮和真皮层有更高的沉积,荧光成像进一步证实了这一点。使用佩里小鼠尾巴模型进行的体内抗银屑病活性研究和皮肤安全性研究证实了该系统在银屑病中局部递送阿维A和芦荟大黄素的潜在益处。