Polymeric Micelles for Enhanced Solubility of Meloxicam in Oral Drug Delivery

摘要

N-arylsuccinyl chitosan was successfully synthesized by introducing hydrophobic and hydrophilic moieties into the chitosan backbone. Incorporation efficiency of the drug-loaded micelles, particle size, in vitro cytotoxicity, and in vitro drug release were investigated. Meloxicam (MX) as a model drug was loaded into the inner core of the micelles by solvent evaporation method. The critical micelle concentration (CMC) of micelles was found to be 0.0385 mg/ml. N-arylsuccinyl chitosan micelles were able to entrap hydrophobic drug (MX) and have particle sizes in the range of 342.1- 444.2 nm. The micelles could enhance solubility of MX with high incorporation efficiency (32.72%). The cytotoxicity in Caco-2 cells to be dependent on the concentration of N-arylsuccinyl chitosan with the IC50 value of 3.23 +/- 0.08 mg/ml. Therefore, N-arylsuccinyl chitosan polymeric micelle presents interest to improve solubility of hydrophobic drug for oral drug delivery.