DSPE-PEG polymer enhanced berberine absorption specifically in the small intestine of rats through paracellular passway.

OBJECTIVES: This study focuses on investigating the potential impact of DSPE-PEG polymers on intestinal absorption and related mechanism of berberine in rats. METHODS: Effect of DSPE-PEG polymer on intestinal absorption of berberine was investigated with an in situ closed-loop method in rats. To confirm the safety of DSPE-PEG polymer, morphological observation of rat intestine and measurement of biological markers in the intestinal perfusion of rats was performed. Underling mechanism behind promoting action of DSPE-PEG polymer was explored from its impact on the P-gp function and tight junction using in vitro diffusion chamber system, Caco-2 monolayer cells and western blot. KEY FINDINGS: DSPE-PEG polymer demonstrated significant enhancement action on the berberine absorption in rats without any obvious membrane toxicity. DSPE-PEG polymer (1.0%, w/v) induced the most significant promoting effect on berberine absorption specifically in the small intestine of rats. Results of mechanistic studies revealed that DSPE-PEG polymer might not regulate intestinal P-gp function, but significantly down-regulated the expression of tight junction-related proteins, which accordingly led to loosening the tight junctions of intestinal epithelium cells, and consequently increased paracellular absorption of berberine in rats. CONCLUSIONS: DSPE-PEG polymer, as an excellent absorption enhancer, seems very promising in increasing oral bioavailability of berberine.

Growth and Development Responses of the Rhizome-Root System in Pleioblastus pygmaeus to Light Intensity.

Light, as a primary source of energy, directly or indirectly influences virtually all morphological modifications occurring in both shoots and roots. A pot experiment was conducted to assess the growth patterns of one-year-old Pleioblastus pygmaeus plants' rhizome-root systems and their responses to different light intensities from 11 March to 26 December 2016. The experiment design scheme was 3.87% (L1), 11.25% (L2), 20.25% (L3), 38.76% (L4), 60.70% (L5), and 100% full sunlight (control CK). The results indicated that along the growing period from March to December, eight of the eleven studied parameters of the rhizome-root system showed significant variability and diverse growth patterns. In addition, light intensity is a key factor for determining P. pygmaeus plants' rhizome and root growth. Specifically, the light intensity had a significant, positive, and linear/or almost linear impact on the number of old and new rhizomes, old rhizome length, new rhizome diameter, as well as the culm root diameter. A nonlinear and positive relationship was found between light intensity and the listed three parameters, i.e., new rhizome length, new rhizome internode length, and rhizome root length. The value of the above-mentioned three parameters significantly increased when affected from 0% to 40-60% of full sunlight and then gradually increased until 100% of full sunlight. The ratio of aboveground dry weight to underground dry weight (A/U ratio) showed a single peak curve with increasing light intensity and presented the highest value under ca. 55% full sunlight. Furthermore, 40% full sunlight (equal to an average light of 2232 lux) might be the threshold for P. pygmaeus rhizome-root system growth. When the light intensity was below 40%, the generalized additive models (GAMs) predicted value of most studied parameters decreased to lower than zero. In conclusion, current study provides a solid basis for understanding the dynamic growth and development of P. pygmaeus rhizome-root system, and its responses to different light conditions, which could be used as inputs to P. pygmaeus plant cultivation.

Efficacy of SPM-NONOate following intrapulmonary delivery in promoting absorptions of poorly absorbed macromolecules in rats and the underling mechanism.

This research aims to investigate the potential of N-[4-[1-(3-Aminopropyl)-2-hydroxy-2-nitrosohydrazino]butyl]-1,3-propanediamine (SPM-NONOate) for promoting the absorption of poorly absorbed macromolecules delivered by intrapulmonary route. Influence of SPM-NONOate on the drug absorption was characterized by using a series of fluorescein isothiocyanate-labeled dextrans (FDs) as affordable models of hydrophilic macromolecules with established tools for quantitative analysis. SPM-NONOate increased concentration-dependently within 1-10 mM the pulmonary absorptions of FDs in rats. Moreover, this promoting effect varied with the molecular weight of FDs, and the largest absorption enhancement effect was obtained for FD70. SPM-NONOate also showed promising enhancement potential on the absorption of some therapeutic peptides, where obvious hypoglycemic and hypocalcemic effects were observed after intrapulmonary delivery of insulin and calcitionin, respectively, with SPM-NONOate to rats. The safety of SPM-NONOate was confirmed based on measurement of some biological markers in bronchoalveolar lavage fluid (BALF) of rats. Additionally, mechanism underling the absorption enhancement action of SPM-NONOate was explored by combinatorial administration of FD4 and SPM-NONOate with various scavengers and generator to rat lungs. Results indicated that NO released from SPM-NONOate induced the enhancement in the drug absorption, and peroxynitrate, a NO metabolite, possibly participated in the absorption enhancing action of SPM-NONOate.

SDS-assisted solvothermal synthesis of rose-like BiOBr partially enclosed by {111} facets and enhanced visible-light photocatalytic activity.

Rose-like BiOBr nanostructures with exposed {111} facets were firstly synthesized with the assistance of an anionic surfactant, sodium dodecyl sulfate (SDS), via a facile solvothermal route. The 2D nanosheets, which self-assembled to form the 3D structures, were achieved with the thickness decreasing from average 120 nm to 20 nm. Specially, the nanosheets were partially enclosed by {111} facets due to the effect of SDS. The as-prepared BiOBr with {111} facets exhibited excellent electrochemical behavior and photocatalytic activity under both visible light (λ≥ 420 nm) and monochromatic light (λ = 420 nm) irradiation.