Self-nanoemulsifying drug delivery system of bruceine D: a new approach for anti-ulcerative colitis

Abstract

Background

Bruceine D (BD) is a major bioactive component isolated from the traditional Chinese medicinal plant Brucea javanica which has been widely utilized to treat dysentery (also known as ulcerative colitis [UC]).

Methods

To improve the water solubility and absolute bioavailability of BD, we developed a self-nanoemulsifying drug delivery system (SNEDDS) composing of MCT (oil), Solutol HS-15 (surfactant), propylene glycol (co-surfactant) and BD. The physicochemical properties and pharmacokinetics of BD-SNEDDS were characterized, and its anti-UC activity and potential mechanism were evaluated in TNBS-induced UC rat model.

Results

The prepared nanoemulsion has multiple beneficial aspects including small mean droplet size, low polydispersity index (PDI), high zeta potential (ZP) and excellent stability. Transmission electron microscopy showed that nanoemulsion droplets contained uniform shape and size of globules. Pharmacokinetic studies demonstrated that BD-SNEDDS exhibited enhanced pharmacokinetic parameters as compared with BD-suspension. Moreover, BD-SNEDDS significantly restored the colon length and body weight, reduced disease activity index (DAI) and colon pathology, decreased histological scores, diminished oxidative stress, and suppressed TLR4, MyD88, TRAF6, NF-κB p65 protein expressions in TNBS-induced UC rat model.

Conclusion

These results demonstrated that BD-SNEDDS exhibited highly improved oral bioavailability and advanced anti-UC efficacy. In conclusion, our current results provided a foundation for further research of BD-SNEDDS as a potential complementary therapeutic agent for UC treatment.

Keywords:

• bruceine D
• self-nanoemulsifying drug delivery system
• physicochemical properties
• pharmacokinetics
• anti-inflammation
• anti-colitis activity

Supplementary materials

Figure S1 ¹H-NMR spectrum of bruceine D.

Figure S2 ¹³C-NMR spectrum of bruceine D.

Acknowledgments

This work was supported by Science and Technology Planning Project of Guangdong Province, China (grant no 2017A050506044), Science and Technology Planning Project of Guangzhou, Guangdong, China (grant no 201704030028), and Natural Science Foundation of Guangdong Province, China (grant no 2018A030313408).

Disclosure

The authors report no conflicts of interest in this work.