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 intestinal delivery of hydrophobic drugs.



Amphiphilic chitosan derivative, Camptothecin, Chitosan, Oral drug delivery, Polymeric micelles

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Carbohydrate Polymers, v. 177, p. 178-186.