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Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis.
International Journal of Nanomedicine ( IF 6.6 ) Pub Date : 2020-06-03 , DOI: 10.2147/ijn.s247406 Jianping Deng 1, 2 , Zicong Wu 1, 2 , Zhenling Zhao 2, 3 , Chaoxi Wu 2, 3 , Min Yuan 1 , Zhengquan Su 1 , Yifei Wang 2, 3 , Zhiping Wang 1, 2
International Journal of Nanomedicine ( IF 6.6 ) Pub Date : 2020-06-03 , DOI: 10.2147/ijn.s247406 Jianping Deng 1, 2 , Zicong Wu 1, 2 , Zhenling Zhao 2, 3 , Chaoxi Wu 2, 3 , Min Yuan 1 , Zhengquan Su 1 , Yifei Wang 2, 3 , Zhiping Wang 1, 2
Affiliation
Purpose: Berberine (BBR), a major ingredient extracted from Coptis chinensis, is a natural drug with limited oral bioavailability. We developed nanostructured lipid carriers (NLCs) as a delivery system for enhanced anti-inflammatory activity of BBR against ulcerative colitis (UC).
Methods: BBR-loaded nanostructured lipid carriers (BBR-NLCs) prepared via high-pressure homogenization were evaluated for particle size, zeta potential, drug entrapment efficiency, drug loading, drug release, toxicity, and cellular uptake. The anti-UC activities of free and encapsulated BBR were evaluated in a DSS-induced acute model of UC in mice.
Results: Spherical BBR-NLCs were prepared with a particle size of 63.96± 0.31 nm, a zeta potential of +3.16 ± 0.05 mV, an entrapment efficiency of 101.97± 6.34%, and a drug loading of 6.00± 0.09%. BBR-NLCs showed excellent biocompatibility in vivo. Cellular uptake experiments showed that BBR-NLCs improved uptake of BBR by RAW 264.7 cells and Caco-2 cells. Oral administration of BBR-NLCs significantly alleviated colitis symptoms (DAI, colon length, spleen swelling, MPO activity) through inhibition of NF-κB nuclear translocation, decreased expression of pro-inflammatory cytokines (IL-1β, IL-6, MMP-9, CX3CR1, COX-2, TERT), and increased expression of the tight junction protein ZO-1.
Conclusion: BBR-loaded NLCs improved colitis symptoms, which suggested that this may be a novel formulation for treatment of UC.
Keywords: berberine, nanostructured lipid carriers, anti-inflammatory, ulcerative colitis
中文翻译：
负载小檗碱的纳米结构脂质载体增强溃疡性结肠炎的治疗。
用途：小檗碱（BBR）是从黄连中提取的主要成分，是一种口服生物利用度有限的天然药物。我们开发了纳米结构脂质载体 (NLC) 作为增强 BBR 对溃疡性结肠炎 (UC) 的抗炎活性的递送系统。
方法：评估通过高压均质制备的负载 BBR 的纳米结构脂质载体 (BBR-NLC) 的粒径、zeta 电位、药物包埋效率、药物负载、药物释放、毒性和细胞摄取。在 DSS 诱导的小鼠急性 UC 模型中评估了游离和封装 BBR 的抗 UC 活性。
结果：制备的球形BBR-NLCs粒径为63.96±0.31 nm，zeta电位为+3.16±0.05 mV，包封率为101.97±6.34%，载药率为6.00±0.09%。BBR-NLC在体内表现出优异的生物相容性。细胞摄取实验表明，BBR-NLCs 提高了 RAW 264.7 细胞和 Caco-2 细胞对 BBR 的摄取。口服 BBR-NLCs 通过抑制 NF-κB 核转位、降低促炎细胞因子（IL-1β、IL-6、MMP-9）的表达，显着缓解结肠炎症状（DAI、结肠长度、脾肿胀、MPO 活性） 、CX3CR1、COX-2、TERT）和紧密连接蛋白 ZO-1 的表达增加。
结论：负载 BBR 的 NLC 改善了结肠炎症状，这表明这可能是一种治疗 UC 的新剂型。
关键词：小檗碱，纳米结构脂质载体，抗炎，溃疡性结肠炎
更新日期：2020-06-03
Methods: BBR-loaded nanostructured lipid carriers (BBR-NLCs) prepared via high-pressure homogenization were evaluated for particle size, zeta potential, drug entrapment efficiency, drug loading, drug release, toxicity, and cellular uptake. The anti-UC activities of free and encapsulated BBR were evaluated in a DSS-induced acute model of UC in mice.
Results: Spherical BBR-NLCs were prepared with a particle size of 63.96± 0.31 nm, a zeta potential of +3.16 ± 0.05 mV, an entrapment efficiency of 101.97± 6.34%, and a drug loading of 6.00± 0.09%. BBR-NLCs showed excellent biocompatibility in vivo. Cellular uptake experiments showed that BBR-NLCs improved uptake of BBR by RAW 264.7 cells and Caco-2 cells. Oral administration of BBR-NLCs significantly alleviated colitis symptoms (DAI, colon length, spleen swelling, MPO activity) through inhibition of NF-κB nuclear translocation, decreased expression of pro-inflammatory cytokines (IL-1β, IL-6, MMP-9, CX3CR1, COX-2, TERT), and increased expression of the tight junction protein ZO-1.
Conclusion: BBR-loaded NLCs improved colitis symptoms, which suggested that this may be a novel formulation for treatment of UC.
Keywords: berberine, nanostructured lipid carriers, anti-inflammatory, ulcerative colitis
中文翻译：
负载小檗碱的纳米结构脂质载体增强溃疡性结肠炎的治疗。
用途：小檗碱（BBR）是从黄连中提取的主要成分，是一种口服生物利用度有限的天然药物。我们开发了纳米结构脂质载体 (NLC) 作为增强 BBR 对溃疡性结肠炎 (UC) 的抗炎活性的递送系统。
方法：评估通过高压均质制备的负载 BBR 的纳米结构脂质载体 (BBR-NLC) 的粒径、zeta 电位、药物包埋效率、药物负载、药物释放、毒性和细胞摄取。在 DSS 诱导的小鼠急性 UC 模型中评估了游离和封装 BBR 的抗 UC 活性。
结果：制备的球形BBR-NLCs粒径为63.96±0.31 nm，zeta电位为+3.16±0.05 mV，包封率为101.97±6.34%，载药率为6.00±0.09%。BBR-NLC在体内表现出优异的生物相容性。细胞摄取实验表明，BBR-NLCs 提高了 RAW 264.7 细胞和 Caco-2 细胞对 BBR 的摄取。口服 BBR-NLCs 通过抑制 NF-κB 核转位、降低促炎细胞因子（IL-1β、IL-6、MMP-9）的表达，显着缓解结肠炎症状（DAI、结肠长度、脾肿胀、MPO 活性） 、CX3CR1、COX-2、TERT）和紧密连接蛋白 ZO-1 的表达增加。
结论：负载 BBR 的 NLC 改善了结肠炎症状，这表明这可能是一种治疗 UC 的新剂型。
关键词：小檗碱，纳米结构脂质载体，抗炎，溃疡性结肠炎
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