Jianping Deng1,2, Zicong Wu1,2, Zhenling Zhao2,3, Chaoxi Wu2,3, Min Yuan1, Zhengquan Su1, Yifei Wang2,3, Zhiping Wang1,2. 1. Guangdong Provincial Engineering Center of Topical Precise Drug Delivery System, Department of Pharmaceutics, Guangdong Engineering Research Center of Natural Products and New Drugs, Guangdong Provincial University Engineering Technology Research Center of Natural Products and Drugs, Guangdong Pharmaceutical University, Guangzhou 510000, People's Republic of China. 2. Guangzhou (Jinan) Biomedical Research and Development Center, Guangzhou 510000, People's Republic of China. 3. College of Life Science and Technology, Jinan University, Guangzhou 510000, People's Republic of China.
Abstract
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.
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.
Authors: Quadri K Alabi; Rufus O Akomolafe; Joseph G Omole; Modinat A Adefisayo; Olaofe L Ogundipe; Ayodeji Aturamu; Joseph O Sanya Journal: Biomed Pharmacother Date: 2018-04-24 Impact factor: 6.529
Authors: Adel M Ahmad; Hamdoon A Mohammed; Tarek M Faris; Abeer S Hassan; Hebatallah B Mohamed; Mahmoud I El Dosoky; Esam M Aboubakr Journal: Molecules Date: 2021-12-10 Impact factor: 4.411