Abstract

The application of artemisinin (ART) in the treatment of malaria has been restricted to a certain degree due to its inherent limitations, such as short half-life, poor solubility, limited bioavailability, and re-crystallization. Electrospun nanofibers loaded with ART provide an excellent solution to these limitations and yield sustained drug release as well as inhibition of drug re-crystallization. In this study, ART-loaded polycaprolactone (PCL)/collagen (Col) nanofibers with different proportions of polymers were prepared. ART-loaded PCL/Col nanofibers were characterized, and further ART anti-crystallization and release behaviors were studied. SEM was used to observe the morphology of PCL/Col nanofibers. X-ray diffraction (XRD) was used to characterize the physical state of ART in ART-loaded PCL/Col nanofibers. Fourier transform infrared spectroscopy (FTIR), water contact angle measurement, weight loss, degree of swelling, and drug release experiments can verify the differences in performance of ART-loaded PCL/Col nanofibers due to different polymer ratios. The release curve was analyzed by kinetics, showing sustained release for up to 48 h, and followed the Fickian release mechanism, which was shown by the diffusion index value obtained from the Korsmeyer-Peppas equation.

Highlights

  • Malaria is a serious parasitic disease that has been spreading all over the world but mainly in Africa [1]

  • ART-loaded PCL/Col nanofibers with different polymer ratios were prepared by electrospinning technology

  • The morphology of the ART-loaded PCL/Col nanofibers was observed by Scanning Electron Microscopy (SEM), and the nanofiber diameter was determined

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Summary

Introduction

Malaria is a serious parasitic disease that has been spreading all over the world but mainly in Africa [1]. Artemisinin (ART), a peroxide-containing sesquiterpene lactone [2,3], is currently the most widely used and most effective anti-malarial drug [4,5]. It shows strong activity against malaria due to Plasmodium falciparum (a unicellular protozoan parasite that is the deadliest species of malaria-causing Plasmodium in humans) and plays a key role in the treatment and continuous control of malaria worldwide [6]. The problem of ART lies mainly in its re-crystallinity [15], which could reduce its bioavailability [16] and therapeutic effect on the human body. It is necessary to suppress ART crystallization to maintain its effectiveness and extend the shelf-life of its active ingredients [17]

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