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Abstract
The delivery of biopharmaceuticals to the oral mucosa offers a range of potential applications including antimicrobial peptides to treat resistant infections, growth factors for tissue regeneration, or as an alternative to injections for systemic delivery. Existing formulations targeting this site are typically non-specific and provide little control over dose. To address this, an electrospun dual-layer mucoadhesive patch was investigated for protein delivery to the oral mucosa. Lysozyme was used as a model antimicrobial protein and incorporated into poly(vinylpyrrolidone)/Eudragit RS100 polymer nanofibers using electrospinning from an ethanol/water mixture. The resulting fibrous membranes released the protein at a clinically desirable rate, reaching 90±13% cumulative release after 2h. Dual fluorescent fibre labelling and confocal microscopy demonstrated the homogeneity of lysozyme and polymer distribution. High encapsulation efficiency and preservation of enzyme activity were achieved (93.4±7.0% and 96.1±3.3% respectively). The released lysozyme inhibited the growth of the oral bacterium Streptococcus ratti, providing further evidence of retention of biological activity and illustrating a potential application for treating and preventing oral infections. An additional protective poly(caprolactone) backing layer was introduced to promote unidirectional delivery, without loss of enzyme activity, and the resulting dual-layer patches displayed long residence times using an in vitro test, showing that the adhesive properties were maintained. This study demonstrates that the drug delivery system has great potential for the delivery of therapeutic proteins to the oral mucosa.
Highlights
Due to advances in protein synthesis in recent decades, proteins and peptides represent one of the fastest growing classes of pharmaceuticals [1]
A typical dose of a therapeutic peptide is in the order of micrograms [27,28,29], a loading of 1% lysozyme by dry mass was used to simulate a loading that may be suitable for mucosal peptide or protein delivery
Further investigation would be required to elucidate the mechanism of this effect. This mucoadhesive system enabled the encapsulation of an enzyme into polymer fibres with superior encapsulation efficiency and biological activity preservation compared to what has previously been accomplished with uniaxial electrospinning
Summary
Due to advances in protein synthesis in recent decades, proteins and peptides represent one of the fastest growing classes of pharmaceuticals [1]. A variety of potential applications for biopharmaceutical delivery to the oral mucosa have been identified. These include antimicrobial peptides as a treatment for bacterial [3] and fungal [4] infections, such as in periodontal disease or oral candidiasis, with resistance to traditional antimicrobials. Topical recombinant cytokines such as epidermal growth factor and basic fibroblast growth factor have shown potential in vivo for regenerating oral wounds or ulcers caused by oral mucositis [5,6]. The oral mucosa is of interest for systemic delivery, circumventing proteolytic degradation in the gastrointestinal tract and offering the potential for controlled release and needleless delivery
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