Novel combination of non-invasive morphological and solid-state characterisation of drug-loaded core-shell electrospun fibres

Abstract

In recent years, core-shell nanofibrous drug delivery systems have received increasing attention due to their ability to incorporate two or more active pharmaceutical ingredients (APIs) individually into the desired layer (either core or sheath) and thereby finely tune the release profiles of even incompatible drugs in one system. This study aims to perform formulation and solid-state characterisation of levofloxacin-loaded polylactic acid (PLA) - naproxen-sodium-loaded polyvinyl pyrrolidone (PVP) bicomponent core-shell fibrous sheets and examine the electro spinnability of the precursor combinations. The selected drugs have potential therapeutic relevance in similar systems intended for wound healing; however, in this study, they are used as model drugs to understand the physicochemical properties of a drug loaded system. In order to determine the best core- and shell-solution combination, a full factorial experimental design is used. A combination of various morphological (scanning electron microscopy and transmission electron microscopy) and microstructural characterisation techniques (X-ray photoelectron spectroscopy and Raman spectroscopy) was applied to non-invasively obtain information about the structure of the fibres and the embedded drugs. The results indicate that core-shell fibres of different compositions could be successfully prepared with various structural homogeneities. The best core-shell structure was obtained using a combination of 15% (w/w) shell concentration and 8% (w/w) PLA solution concentration. In addition to the conventional core-shell structural verification methods, the Raman spectroscopy method was implemented to reveal not only the core-shell structure of the PLA/PVP nanofibers but also the form of the embedded drugs. The Raman mapping of the fibres confirm the above results, and it is shown that an amorphous solid dispersion is formed as a result of the coaxial electrospinning process.

Keywords: Chloroform (PubChem CID: 6212); Coaxial electrospinning; Core-shell electrospun fibres; Drug delivery; Ethanol (PubChem CID: 702); Hydroxypropyl-beta-cyclodextrin (PubChem CID:14049689); Levofloxacin (PubChem CID: 149096); N,N-dimethylformamide (PubChem CID: 6228); Naproxen-sodium (PubChem CID: 23681059); Polylactic acid (PubChem CID: 612); Polysorbate 80 (PubChem CID: 5284448); Polyvinyl pyrrolidone (PubChem CID: 131751496); Raman spectroscopy; Transmission electron microscopy.