Xiuling Tang,Huanhuan Zhao,Wei Jiang,Song Zhang,Shun Guo,Xiaobo Gao,Peng Yang,Lei Shi,Linna Liu
Dry citrus peel (Chenpi) is not only consumed as a dietary supplement, but also used for the treatment of respiratory diseases. Pinelliae Rhizoma Praeparatum (Banxia) is always used with Chenpi for the treatment of respiratory diseases, but β-sitosterol, the main active component in Banxia, as a food additive, shows no respiratory system activity. In the present study, the pharmacokinetic characters showed that the absorption of the active components of Chenpi was accelerated under pathological conditions combined with Banxia. Although the bioavailability of active components did not significantly change, the distribution of active components in tissues increased, particularly in the target organ. These results are consistent with the combination of Chenpi with β-sitosterol. Furthermore, the pharmacodynamics result also indicated that Chenpi combined with Banxia or β-sitosterol was able to ameliorate histopathologic damage and decrease the levels of inflammatory factors. The results suggest that pharmacokinetic interactions improve the pharmacological activity of Chenpi in respiratory diseases.
Ulcerative colitis is an inflammatory disease that primarily involves intestinal inflammation and epithelial damage. The nano-targeted drug delivery system delivers drugs to the disease site, exerting effects such as inhibiting inflammatory response and reducing reactive oxygen species expression, thereby promoting recovery from ulcerative colitis. In this experiment, dextran sulfate-coated curcumin nanocrystals (NBD) were prepared for the oral treatment of ulcerative colitis (UC). NBD not only significantly enhances the water solubility and stability of curcumin but also possesses the ability of sustained release and targeting inflammatory macrophages. The sustained release effect of NBD was demonstrated by in vitro release experiments. In simulated gastric fluid, the cumulative release amount of NBD at 2 h was 21.99 ± 1.93 %, while in simulated colonic fluid, the cumulative release amount of NBD at 12 h was 84.98 ± 2.02 %. The ability of NBD to target inflammatory macrophages was verified through the transwell system, rat one-way intestinal perfusion experiment and in vivo imaging system. The in vitro and in vivo (mice) anti-inflammatory and antioxidant capacities of NBD were validated using immunofluorescence experiment, ELISA kits and reactive oxygen species-related detection kits. The results indicated that NBD could reduce inflammatory responses, promote macrophage polarization and inhibit oxidative stress. In addition, the therapeutic effect of NBD was further confirmed in this experiment by the clostridium perfringens-induced necrotizing enteritis model in chickens. In conclusion, NBD might be a potential pharmaceutical preparation for the treatment of UC.
In this study, we developed calcium alginate-coated nanovesicles derived from macrophage membranes loaded with berberine (Ber@MVs-CA) for the oral treatment of ulcerative colitis (UC). Ber@MVs-CA demonstrates resistance to gastric acid and controlled drug release in the colonic pH environment, while actively targeting sites of ulcerative colitis injury. pH-responsive release of Ber in Ber@MVs-CA was confirmed through in vitro release experiments. The results indicated a total of 19.35 ± 1.61 % of Ber was cumulatively released from Ber@MVs-CA in SGF and SIF at 4 h, and approximately 87.14 ± 2.33 % release in simulated colonic fluid (pH 7.4) after 24 h. The targeting ability of Ber@MVs-CA was confirmed using laser confocal microscopy (CLSM), Transwell™ system, and in vivo imaging. Results demonstrated effective targeting of inflammatory macrophages and sustained retention in the colon. In vitro and in vivo (mice) assessments via immunofluorescence, ELISA kit, and reactive oxygen species (ROS) assays demonstrated that Ber@MVs-CA effectively attenuated inflammatory responses, modulated macrophage polarization, and inhibited oxidative stress. Additionally, we evaluated the therapeutic efficacy of Ber@MVs-CA in a Clostridium perfringens -induced enteritis model in chickens, demonstrating its effectiveness in alleviating enteritis. Consequently, Ber@MVs-CA exhibits great potential as an oral nano-formulation for the treatment of enteritis. Thus, Ber@MVs-CA shows great potential as an oral nano-formulation for the treatment of enteritis.
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