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Recently, Fei Tan of Tongji University School of Medicine, in collaboration with Prof. Xiangliang Yang and Qing Du of Huazhong University of Science and Technology (HUST), successfully developed a three-fluid electrostatic spinning process to prepare three-compartmental composite Electrospun Nanofbers.The aim of this study is to develop a novel drug delivery system to improve oral bioavailability and synergistic anticancer action of drugs. The related research results were published under the title “Improved synergistic anticancer action of quercetin and tamoxifen citrate supported by an electrospun complex nanostructure “The results were published in the journal Materials & Design.
1.This study prepared a complex nanostructure by three-fluid electrospinning technique for improving the synergistic anticancer effect of quercetin and tamoxifenate.
2.The complex Electrospun Nanofbers have a three-compartmental structure with a center-shell microstructure and a Janus primary structure that helps in controlled drug release and oral bioavailability.
3.Scanning electron microscopy, transmission electron microscopy and confocal fluorescence microscopy image results demonstrated the complex structure of Electrospun Nanofbers.
4.In vitro release studies demonstrated that the three-compartment Electrospun Nanofbers promoted rapid release of quercetin (90% vs 38%) and delayed and sustained release of tamoxifen citrate over the same time interval (1.88) times less). The results of in vivo experiments showed that this composite nanostructure had a significant inhibitory effect on tumor growth.
In the present study, the core-shell and Janus structures of the composite nanofibers helped to increase the oral bioavailability of quercetin and tamoxifenate. The rapid release of quercetin in the stomach increased its systemic utilization, whereas tamoxifenate achieved delayed and sustained release in the intestine, leading to an increased drug concentration gradient and blood circulation, thus enhancing its efficacy. In addition, the inhibition of the P-gp efflux pump by quercetin selectively promoted the intestinal absorption of tamoxifenate, reducing its first-pass effect and increasing its blood concentration and efficacy.
Overall, the binding of the nucleus-shell and Janus structures in the composite Electrospun Nanofbers contributed to the controlled and differential release of the drugs, which ultimately enhanced their oral bioavailability and synergistic anticancer effects.
Key findings and insights from this paper include:
1. A three-fluid electrospinning process was developed for the preparation of three-compartment Electrospun Nanofbers with the core-shell structure embedded on one side of the main Janus structure, which provided a controlled dual, temporal and target-specific delivery system for tamoxifenate and quercetin.
2. The complex structure of Electrospun Nanofbers was demonstrated by SEM, TEM and confocal microscopy images showing the core-shell structure embedded on one side of the main Janus structure.
3. The amorphous state and good component compatibility of the model drug in the three-compartment Electrospun Nanofbers were characterized by XRD and FTIR analyses, suggesting that Electrospun Nanofbers are suitable for drug delivery.
4. In vitro release studies demonstrated that the three-compartment Electrospun Nanofbers provided a release system in which quercetin was rapidly released in the stomach, while tamoxifenate achieved a delayed and sustained release in the intestines, resulting in improved bioavailability and anticancer properties.
5. Higher cytotoxicity of the combined drug in the three-compartment Electrospun Nanofbers as compared to the original drug alone, suggesting a synergistic anticancer effect of quercetin and tamoxifenate in the complex nanostructures.
6. The potential of the three-fluid electrospinning process and the complex nanostructures it produces to advance functional nanomaterials in the field of drug delivery, providing insights into the design of novel advanced functional nanomaterials.
These findings and insights contribute to the understanding of how the three-fluid electrospinning process and the complex nanostructures it generates can be utilized to enhance the anticancer effects of quercetin and tamoxifenates and to advance the development of functional nanomaterials in the field of drug delivery.
Originallink: https://doi.org/10.1016/j.matdes.2024.11265
