Inhomogeneous lignin from a canola (rapeseed) straw was isolated and valorized as regularly shaped spherical microparticles for drug delivery formulations. Lignin with a purity of 83% and broad molecular weight distribution (<SIC> > 5.0) was extracted by alkali pulping and acetylated to increase spheronization ability. Lignins with high degrees of acetylation (0.76 and 0.89) were successfully assembled into microparticles with uniform sizes (approximately 2 mu m) and smooth spherical surfaces via solvent-antisolvent precipitation. Hydrophobic coumarin 153 and positively charged ciprofloxacin were used as model drugs to assess the encapsulation and release performance of lignin microparticles. Highly acetylated lignin microparticles displayed encapsulation efficiencies of 89.6% for coumarin 153% and 90.6% for ciprofloxacin. Scanning electron microscope images showed that coumarin 153 was encapsulated in the hydrophobic core, while ciprofloxacin was adsorbed on the less hydrophobic shell. The synthesis of lignin microcarriers not only provides a facile approach to utilizing waste canola straw lignin for drug delivery matrices but also has the potential to serve as an alternative lignin powder feedstock for bio-based materials.