Incorporation of functionalized carbon nanotubes into hydrophobic drug crystals for enhancing aqueous dissolution

We present for the first time the direct incorporation of carboxylated carbon nanotubes (f-CNTs) into hydrophobic drug particles during their formation via anti-solvent precipitation. The approach was tested using two drugs namely antifungal agent Griseofulvin (GF) and antibiotic Sulfamethoxazole (SMZ) that had very different aqueous solubility. It was observed that the f-CNTs dispersed in the water served as nucleating sites for crystallization and were readily incorporated into the drug particles without altering crystal structure or other properties. The results showed that the hydrophilic f-CNTs dramatically enhanced dissolution rate for both drugs, and the time necessary to reach 80% dissolution (t₈₀) reduced from 67 to 10 with the incorporation of 5.1% f-CNTs in SMZ, and from 66 to 18 min with 4.0% f-CNTs in GF. The enhanced dissolution is attributed to the fact that the hydrophilic f-CNTs served as conduits for bringing in water in close contact with the drug crystals.