Dual drug-loaded biodegradable Janus particles for simultaneousco-delivery of hydrophobic and hydrophilic compounds

摘要

Bicompartmental Janus particles have many advantages in drug delivery, includingco-delivery of two compounds with varying solubilities, differential releasekinetics, and two surfaces available for targeting ligands. We present a novelstrategy using the double emulsion method for the coencapsulation and staggeredrelease of a hydrophobic and hydrophilic drug from anisotropic PLGA/PCL Janusparticles, as well as a UV detection method to measure the release of twodifferent compounds from Janus particles. Curcumin and quercetin were chosen asthe model hydrophobic compounds for drug loading studies, while acetaminophen(APAP) and naproxen were chosen as the model hydrophilic–hydrophobic drug pairfor encapsulation methods and drug loading. Also, a similar double emulsionmethod was also applied for PLGA/Preicrol® Janus particles containingDoxorubicin and Curcumin. Hydrophobic drugs were encapsulated by the single O/Wemulsion technique. Hydrophilic compounds required special modifications due totheir poor oil solubility and tendency to escape to the outer aqueous phaseduring the emulsification and solvent evaporation steps. In total, threedifferent strategies for incorporating hydrophilic drugs were employed: (1) O/Wemulsion with partially water miscible solvent, (2) O/W emulsion with co-solvent(i.e. acetone, methanol, ethanol), or (3) W/O/W double emulsion. Theencapsulation efficiencies and drug loading percentages were measured usingUV/Vis spectroscopy and compared for the different synthesis methods. It wasfound that the double emulsion method resulted in the highest encapsulationefficiency and drug loading of the hydrophilic drug.