Physicochemical and drug diffusion analysis of rifampicin containing polyethylene glycol–poly(ɛ-caprolactone) networks designed for medical device applications

This study reports the physicochemical and drug diffusion properties of rifampicin containing poly(ɛ-caprolactone) (PCL)/polyethylene glycol (PEG) networks, designed as bioactive biomaterials. Uniquely, the effects of the states of both rifampicin and PEG and the interplay between these components on these properties are described. PCL matrices containing rifampicin (1–5%, w/w) and PEG 200 (0–15%, w/w) were prepared by casting from an organic solvent (dichloromethane). The films were subsequently characterized in terms of their thermal/thermorheological, surface and tensile properties, biodegradation and drug diffusion/release properties. Incorporation of PEG and/or rifampicin significantly affected the tensile and surface properties of PCL, lowering the ultimate tensile strength, % elongation at break, Young modulus and storage and loss moduli. Both in the absence and presence of PEG, solubilisation of rifampicin within the crystalline domains of PCL was observed. PEG was present as a dispersed liquid phase. The release of rifampicin (3% loading) was unaffected by the presence of PEG. Similarly the release of rifampicin (5%) was unaffected by low concentrations of PEG (5–10%) however, at higher loadings, the release rate of rifampicin was enhanced by the presence of PEG. Rifampicin release (10% loading) was enhanced by the presence of PEG in a concentration dependent fashion. These observations were accredited to enhanced porosity of the matrix. In all cases, diffusion-controlled release of rifampicin occurred which was unaffected by polymer degradation. This study has uniquely illustrated the effect of hydrophilic pore formers on the physicochemical properties of PCL. Interestingly, enhanced diffusion controlled release was only observed from biomaterials containing high loadings of PEG and rifampicin (5, 10%), concentrations that were shown to affect the mechanical properties of the biomaterials. Care should therefore be shown when adopting this strategy to enhance release of bioactive agents from biomaterials.

► We examined the physicochemical and drug diffusion properties of rifampicin containing poly(caprolactone)/PEG 200 films, prepared by solvent evaporation. ► The thermorheological, mechanical and surface properties of the films were quantified and observed to be dependent on the presence of drug and PEG 200. ► Solubilisation of rifampicin within the crystalline domains of PCL was observed. ► PEG 200 (5–10%) did not affect drug release from films containing 3 and 5% rifampicin although at higher drug loadings (10%) PEG did enhance drug release. ► The presence of pores due to dissolution of PEG did not necessarily promote drug diffusion, due to drug entrapment within the crystalline domains.