Effect of palmitic acid on the characteristics and release profiles of rotigotine-loaded microspheres

Abstract

Background: The initial burst release is a major obstacle to the development of microsphere-formulated drug products.

Purpose: To investigate the influence of palmitic acid on the characteristics and release profiles of rotigotine-loaded poly(d,l-lactide-co-glycolide) microspheres.

Materials and methods: Rotigotine-loaded microspheres (RMS) were prepared using the oil-in-water emulsion solvent evaporation technique. The in vitro characteristics of the RMS were evaluated with scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and a particle size analyzer. The in vitro drug release and in vivo pharmacokinetics of the RMS were investigated.

Results and discussion: The SEM results showed that the addition of palmitic acid changed the surface morphology of the microspheres from smooth to dimpled and then to non-smooth as the palmitic acid content increased. DSC revealed the existence of molecularly dispersed forms of palmitic acid in the microspheres. The in vitro and in vivo release profiles indicated that the addition of 5% and 8% palmitic acid significantly decreased the burst release of rotigotine from the microspheres, and the late-stage release was delayed as the palmitic acid content increased across the investigated range (5–15%).

Conclusion: The addition of palmitic acid to the microspheres significantly affects the release profile of rotigotine from RMS.

• Burst release
• characteristics
• palmitic acid
• rotigotine-loaded microspheres

Acknowledgements

The authors are grateful to the Taishan Scholar Project and to Zimei Wu for her valuable suggestions in this work.

Declaration of interest

The authors report no declarations of interest.

We gratefully acknowledge support from the National Science and Technology Foundation (2013ZX09402201) and the Natural Science Foundation of Shandong Province (ZR2013HQ009).