Oral administration of Huanglian-Houpo herbal nanoemulsion loading multiple phytochemicals for ulcerative colitis therapy in mice

Abstract

How to achieve stable co-delivery of multiple phytochemicals is a common problem. This study focuses on the development, optimization and characterization of Huanglian-HouPo extract nanoemulsion (HLHPEN), with multiple components co-delivery, to enhance the anti-ulcerative colitis (UC) effects. The formulation of HLHPEN was optimized by pseudo-ternary phase diagram combined with Box-Behnken design. The physicochemical properties of HLHPEN were characterized, and its anti-UC activity was evaluated in DSS-induced UC mice model. Based on preparation process optimization, the herbal nanoemulsion HLHPEN was obtained, with the droplet size, PDI value, encapsulation efficiency (EE) for 6 phytochemicals (berberine, epiberberine, coptisine, bamatine, magnolol and honokiol) of 65.21 ± 0.82 nm, 0.182 ± 0.016, and 90.71 ± 0.21%, respectively. The TEM morphology of HLHPEN shows the nearly spheroidal shape of particles. The optimized HLHPEN showed a brownish yellow milky single-phase and optimal physical stability at 25 °C for 90 days. HLHPEN exhibited the good particle stability and gradual release of phytochemicals in SGF and SIF, to resist the destruction of simulated stomach and small intestine environment. Importantly, the oral administration of HLHPEN significantly restored the shrunk colon tissue length and reduced body weight, ameliorated DAI value and colon histological pathology, decreased the levels of inflammatory factors in DSS-induced UC mice model. These results demonstrated that HLHPEN had a significant therapeutic effect on DSS-induced UC mice, as a potential alternative UC therapeutic agent.

Keywords:

• Nanoemulsion
• multi-component
• co-delivery
• Huanglian-Houpo
• anti-ulcerative colitis

Disclosure statement

No potential conflict of interest was reported by the authors.

Ethical approval statement

All institutional and national guidelines for the care and use of laboratory animals were followed. The ethics committee: the State Committee of Science and Technology of China and the Institutional Animal Care and Use Committee (IACUC) of Sichuan Province.

The number or ID of the ethics approval: SYXK (Chuan) 2020-124.

The mice were used to study the anti-UC effect of the preparation. All mice were under the conditions of room temperature (20 ± 0.5° C,), humidity (50 ± 10%), light (12 h light/dark cycle) and were free access to diet. At the end of study, the animals were sacrificed following anesthesia with pentobarbital sodium (80 mg/kg).

Additional information

Funding

The authors would like to thank the National Interdisciplinary Innovation Team of Traditional Chinese Medicine, for funding this project under the project number ZYYCXTD-D-202209.