Novel amphiphilic chitosan micelles as carriers for hydrophobic anticancer drugs
- Almeida, A.
- Araújo, Marco
- Novoa-Carvallal, Ramon
- Andrade, Fernanda
- Gonçalves, Hugo
- Reis, R. L.
- Lúcio, Marlene
- Schwartz Jr, Simó
- Sarmento, Bruno
DOIAbstract
Chitosan was grafted with O-methyl-O⠲-succinylpolyethylene glycol and oleic acid after a two-step carbodiimide coupling. The structural and physicochemical characterization of the compounds confirmed the successful conjugation of the hydrophilic and hydrophobic moieties to the chitosan backbone. The amphiphilic chitosan derivative obtained allowed the formation of polymeric micelles with an average size of 140 nm, a polydispersity index <0.234, and a positive superficial charge. Camptothecin, used as a model hydrophobic drug, was successfully carried into the polymeric micelles with an encapsulation efficiency of 78%. The in vitro drug release was evaluated in simulated gastrointestinal fluids, exhibiting a low release of camptothecin...
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