Institute of Nano Science and Technology, Habitat Centre, Phase - 10, Sector 64, Mohali, Punjab 160062, India.
Laboratory for Stem Cell and Restorative Neurology, Department of Biotechnology, Era's Lucknow Medical College Hospital, Sarfarazganj, Lucknow 226003, India.
Mater Sci Eng C Mater Biol Appl. 2020 Nov;116:111103. doi: 10.1016/j.msec.2020.111103. Epub 2020 May 20.
Ulcerative colitis is a chronic mucosal inflammatory condition that adversely affects colon and rectum. Celecoxib is a selective inhibitor of inducible cyclooxygenase-2 (COX-2) and is prescribed for the management of pain and other inflammatory disorders. The physicochemical properties of celecoxib limit its clinical potency. Here we developed nanostructured lipid carriers (NLCs) using Generally Recognized as Safe and US-FDA approved compounds for encapsulating celecoxib. Present study was aimed to evaluate efficacy of eudragit-S100-coated celecoxib-loaded NLCs against DSS-induced colitis in mice. NLCs were formulated by hot-melt method and possessed the average particle size of 250.90 nm and entrapment efficiency (%) was 59.89%. Furthermore, size, shape and morphology of NLCs were confirmed using TEM, SEM and AFM. The blank NLCs were cytocompatible against hTERT-BJ cells up to a dose of 200 μg/ml. Treatment with celecoxib-loaded NLCs alleviated severity of colitis as demonstrated by disease activity index, colon length, fecal occult blood test, and histopathological analysis. Moreover, treatment with celecoxib-loaded NLCs reduced disintegration of goblets cells and restores sulfomucin in colon. Celecoxib-nanoformulation markedly reduced colonic inflammation as evidenced by decreased immunohistochemical expression of COX-2 and iNOS. The observations of study suggest that lipid-based colon specific delivery of celecoxib may be used for management of colitis.
溃疡性结肠炎是一种慢性黏膜炎症性疾病，主要影响结肠和直肠。塞来昔布是一种诱导型环氧化酶-2（COX-2）的选择性抑制剂，用于治疗疼痛和其他炎症性疾病。塞来昔布的理化性质限制了其临床疗效。在这里，我们使用一般认为安全且美国食品和药物管理局批准的化合物开发了纳米结构脂质载体（NLC）来包封塞来昔布。本研究旨在评估载有塞来昔布的 Eudragit-S100 涂层纳米脂质载体（NLC）对 DSS 诱导的结肠炎小鼠的疗效。NLC 采用热熔法制备，平均粒径为 250.90nm，包封率（%）为 59.89%。此外，还使用 TEM、SEM 和 AFM 对 NLC 的大小、形状和形态进行了确认。空白 NLC 对 hTERT-BJ 细胞的细胞相容性高达 200μg/ml。载有塞来昔布的 NLC 治疗可减轻结肠炎的严重程度，表现在疾病活动指数、结肠长度、粪便潜血试验和组织病理学分析上。此外，载有塞来昔布的 NLC 治疗可减少杯状细胞的崩解，并恢复结肠中的硫酸粘蛋白。载有塞来昔布的纳米制剂可显著减轻结肠炎症，这可通过 COX-2 和 iNOS 的免疫组化表达减少来证明。研究结果表明，塞来昔布的基于脂质的结肠特异性给药可能用于结肠炎的治疗。
