Modified mixed nanomicelles with collagen peptides enhanced oral absorption of Cucurbitacin B: preparation and evaluation

Abstract

Polymer nanoparticles modified with collagen peptides (CPs) are an attractive strategy for the oral delivery of active ingredients from Chinese medicine. Thus, in the present study, collagen cationic CPs were simply separated using ion-exchange resin from bovine CPs, to modify mixed nanomicelles (MMs) on the surface to improve the oral bioavailability of Cucurbitacin B (CuB). The physicochemical property of micelles was characterized, which confirmed the successful modification of the nanomicelles. CPs-modified nanomicelles in vitro were found to significantly increase cellular uptake and transportation. Compared to unmodified micelles, the quantity of CPs-modified micelles internalized by Caco-2 cells were 3.74 times greater and the cumulative transportation flux (AP-BL) was 2.81 times greater. The membrane transportation process of CuB-MMs-CPs was found to be associated with energy consumption and clathrin- and caveolin-mediated endocytosis. In vivo studies performed on rats indicated that in comparison to CuB and CuB-MMs, the relative bioavailability of CuB-MMs-CPs increased by 3.43 times and 2.14 times, respectively. In addition, the tumor inhibition caused by CuB-MMs-CPs was increased significantly. Therefore, the nanomicelles co-modified with isolated CPs could act as attractive carriers for oral delivery of CuB.

Naturally occurring anti-cancer compounds: shining from Chinese herbal medicine

“…In addition, some other strategies have been applied to accelerate the clinical use of cucurbitacin B. The collagen peptide-modified nanomicelles with cucurbitacin B were synthesized to enhance the oral availability of cucurbitacin B, and these nanomicelles show a higher bioavailability and better tumor inhibition [497].…”

Preparation, Characterization, and In Vivo Evaluation of an Oral Multiple Nanoemulsive System for Co-Delivery of Pemetrexed and Quercetin

“…Complex formation of FITC-PMX with DCK and incorporation of FITC-PMX/DCK into the NE system resulted in significantly greater cellular uptake into Caco-2 cells compared with that observed with FITC-PMX ( Figure 4 A). This result was attributed to the increased lipophilicity of PMX by the permeation enhancer (DCK), which was also shown to be able to alter the membrane structure and fluidity, resulting in enhanced cellular uptake [ 51 ]. Similarly, the intracellular uptake of QCN-NE was also significantly increased compared with that of QCN in 0.3% NaCMC ( Figure 4 A).…”

In Vitro and In Situ Characterization of the Intestinal Absorption of Capilliposide B and Capilliposide C from Lysimachia capillipes Hemsl

“…The oral delivery route for the therapeutic administration of drugs remains one of the most desirable and important routes in drug delivery. With a combination of increased patient compliance, safety and ease of administration, orally-delivered drugs often offer greater clinical efficacy than other options, particularly in minimizing potential infections [1]. However, many therapeutics are unable to utilize this sought-after delivery route due to the poor solubility and instability of many compounds in gastrointestinal fluids.…”