a Department of Pharmaceutics , National Institute of Pharmaceutical Education & Research (NIPER) , Hyderabad , India ;
b Department of Pharmacy, School of Chemical Sciences and Pharmacy , Central University of Rajasthan , Ajmer , India.
Drug Dev Ind Pharm. 2019 May;45(5):826-838. doi: 10.1080/03639045.2019.1576722. Epub 2019 Feb 14.
The aim of this study was to formulate nanostructured lipid carriers (NLCs) of dithranol-loaded in gel for ease of application and to evaluate its anti-psoriatic efficacy vis-a-vis conventional ointment formulation.
This study will provide an insight about the use of nanocarriers, esp. NLCs loaded with dithranol for the effective treatment of psoriasis.
Dithranol-loaded NLCs were prepared by hot melt homogenization method and characterized for particle size and percentage entrapment efficiency. The optimized NLCs were loaded into gel and evaluated for drug release, spreadability, rheological behavior, and staining. Anti-psoriatic efficacy of the NLC gel was evaluated in imiquimod (IMQ) induced psoriatic plaque model in comparison with prepared conventional ointment formulation (1.15% w/w dithranol).
NLCs were prepared with particle size below 300 nm, polydispersity index (PDI) below 0.3 and percentage entrapment efficiency of ∼100%. The prepared NLC gel was then compared with the ointment for drug release, staining property, and efficacy. Topical application of dithranol-loaded NLC gel on IMQ-induced psoriatic plaque model reduced the symptoms of psoriasis assessed by both Psoriasis area severity index (PASI) scoring and enzyme-linked immunosorbent assay. There was a significant reduction in disease severity and cytokines like Interleukins-17, 22, 23 and Tumor necrosis factor-α by the developed system in comparison to the negative control.
To conclude dithranol-loaded NLCs in gel base was efficacious in management of psoriasis at the same drug concentration and also offer less cloth staining to that of the ointment product.
本研究旨在制备载二羟蒽酮的纳米结构脂质载体（NLC）凝胶，以方便应用，并评估其与常规软膏制剂相比的抗银屑病疗效。
本研究将为纳米载体的应用提供一个见解，特别是载有二羟蒽酮的 NLC 用于有效治疗银屑病。
通过热熔匀化法制备载二羟蒽酮的 NLC，并对粒径和包封率进行了表征。将优化的 NLC 载入凝胶中，并对药物释放、铺展性、流变学行为和染色进行了评价。与制备的常规软膏制剂（1.15%w/w 二羟蒽酮）相比，在咪喹莫特（IMQ）诱导的银屑病斑块模型中评价了 NLC 凝胶的抗银屑病疗效。
NLC 的粒径低于 300nm，多分散指数（PDI）低于 0.3，包封效率约为 100%。然后将制备的 NLC 凝胶与软膏进行比较，以评价药物释放、染色性能和疗效。载二羟蒽酮的 NLC 凝胶局部应用于咪喹莫特诱导的银屑病斑块模型，通过银屑病面积严重程度指数（PASI）评分和酶联免疫吸附试验评估，可减轻银屑病的症状。与阴性对照组相比，该系统显著降低了疾病严重程度和细胞因子如白细胞介素-17、22、23 和肿瘤坏死因子-α的水平。
总之，载二羟蒽酮的 NLC 凝胶在相同药物浓度下对银屑病的治疗有效，并且与软膏产品相比，其对衣物的染色程度较低。
