Journal
INTERNATIONAL JOURNAL OF NANOMEDICINE
Volume 15, Issue -, Pages 3937-3951Publisher
DOVE MEDICAL PRESS LTD
DOI: 10.2147/IJN.S247406
Keywords
berberine; nanostructured lipid carriers; anti-inflammatory; ulcerative colitis
Funding
- Guangdong Provincial Engineering Center of Topical Precise Drug Delivery System [2016A040402033]
- science and technology projects of Guangdong Province [2016A040402033]
- National Engineering Research Center for Modernization of Traditional Chinese Medicine Moxa herb Branch
- Introduction of Leading Talents Program of Huizhou City
- Technology Innovation Team Program of Huizhou City [20170217013144015]
- Daya Bay Technology Project [2017008]
- Key Laboratory of Bioengineering Drugs of Guangdong Province of China
- Innovation Strong School Project of Department of Education of Guangdong Province
- Guangdong Pharmaceutical University, China
- Talent Training Program of Guangdong Province Joint Training Graduate Demonstration Base
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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 highpressure 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-kappa B nuclear translocation, decreased expression of pro-inflammatory cytokines (IL-1 beta, 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.
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