Abstract
Chitosan oleate (CS-OA), a chitosan salt with amphiphilic properties, has demonstrated the ability to self-assemble in aqueous environment to give polymeric micelles useful to load poorly soluble drugs. More recently, CS-OA was proposed to stabilize nanoemulsions during the preparation by emulsification and solvent evaporation of poly lactic-glycolic acid (PLGA) nanoparticles (NPs) loaded with curcumin. Positive mucoadhesive behavior and internalization properties were demonstrated for these NPs attributable to the presence of positive charge at the NP surface. In the present paper, two CS-OA-based nanosystems, micelles and PLGA NPs, were compared with the aim of elucidating their physico-chemical characteristics, and especially their interaction with cell substrates. The two systems were loaded with resveratrol (RSV), a hydrophobic polyphenol endowed with anti-cancerogenic, anti-inflammatory, and heart/brain protective effects, but with low bioavailability mainly due to poor aqueous solubility. Calorimetric analysis and X-ray spectra demonstrated amorphization of RSV, confirming its affinity for hydrophobic domains of polymeric micelles and PLGA core of NPs. TGA decomposition patterns suggest higher stability of PLGA-NPs compared with polymeric micelles, that anyway resulted more stable than expected, considering the RSV release profiles, and the cell line interaction results.
Highlights
Many reports have been focused on the preparation and on the possible exploitation of amphiphilic derivatives of chitosan [1]
The relevance of chitosan oleate (CS-oleic acid (OA)) concentration on particle size was investigated for poly lactic-glycolic acid (PLGA)-NPs
The results presented in this paper confirm that CS-OA, for its ability to self-assemble and to stabilize emulsions, is suitable for preparing both micelles and PLGA-NPs containing RSV as lipophilic model drug
Summary
Many reports have been focused on the preparation and on the possible exploitation of amphiphilic derivatives of chitosan [1]. Chitosan (CS) and chitosan derivatives have been hydrophobically modified by interaction with different hydrophobic pendant groups, usually by covalent derivatization [2,3,4,5,6]. Amphiphilic polymers are known for their ability to self-assemble into nanoparticles with a hydrophobic core or inner hydrophobic domains and outer shell layers made by the chains of the polymer hydrophilic portions. This mechanism, common to polymeric micelles, was previously shown for chitosan oleate (CS-OA), a chitosan salt with amphiphilic properties and whose self-assembling in aqueous environment resulted suitable to efficiently load hydrophobic poorly soluble molecules [7,9].
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