Self-aggregates of 3,6-O,O’-dimyristoylchitosan derivative are effective in enhancing the solubility and intestinal permeability of camptothecin


The aim of this work was to investigate the potential of a new 3,6-O,O’-dimyristoyl derivative amphiphilic chitosan (DMCh), in improving the solubility of camptothecin (CPT), a hydrophobic anticancer drug, and its potential oral delivery. FTIR, 1H NMR and solid-state 13C NMR spectroscopy were used to characterize DMCh and to determine its average degree of substitution (DS = 6.8%). DMCh/CPT micelles size ranged from (281–357 nm), zeta potential (+32–50 mV) of encapsulation efficiency of 42–100%. The in vitro cell viability showed that DMCh/CPT micelles were able to reduce the toxicity of CPT. The in vitro permeability of CPT through Caco-2 and Caco-2/HT29-MTX intestinal models was increased up to ten fold when formulated into DMCh micelles, underlining the mucoadhesive properties of the nanocarrier. DMCh/CPT micelles are able to enhance CPT solubility and bioavailability while reduce its cytotoxicity, showing the great potential for in- testinal delivery of hydrophobic drugs.


Silva, Daniella S.; Almeida, Andreia; Prezotti, Fabíola G.; Facchinatto, William M.; Colnago, Luiz A.; Campana-Filho, Sérgio P.; Sarmento, Bruno

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