Purpose: In the present work we report on the preparation of nanoparticulate systems N-trimethyl chitosan (TMC) based, in which a titrated extract of Boswellia serrata (Boswellin®- BSW) has been enclosed, to be used as model drug for a colon specific drug delivery system. Methods: The synthesis of TMC has been performed through methylation reaction with Methyl iodide in basic medium, carefully modifying reaction steps and conditions in order to reach the desired Degree of Quaternization (DQ). The obtained polymers have been characterized by means of spectroscopic methods (FTIR, NMR and XRD). Water dispersions of TMC have also been submitted to physical- chemical analyses, such as determination of pH, rheological, evaporation-freezing assays and stability studies. TMC nanoparticles loaded BSW (BSW NP) have been prepared through ionotropic gelation method using tripolyphoshate (TPP). Results: TMC dispersions showed to be much stable overtime if compared with the corresponding Chitosan ones. Moreover TMC have been used for the preparation of BSW NP. The obtained BSW NP showed good polydispersity index (PDI), potential and are stable overtime. Particles size, drug loading capacity and efficiency were determined. BSW preliminary release in vitro tests were performed by HPLC. Data showed that BSW has been released from the polymer matrix in a prolonged and controlled manner. Conclusion: TMC could be considered a more promising derivative than chitosan itself for the preparation of NP. Opportunely varying the DQ, nanoparticulate drug delivery systems have been obtained, suitable for the preparation of colon specific drug delivery systems.
Preparation and characterization of TMC nanoparticles for colon specific drug delivery
CARDIA, MARIA CRISTINA;MACCIONI, ANNA MARIA;MARCI, LUISA;
2013-01-01
Abstract
Purpose: In the present work we report on the preparation of nanoparticulate systems N-trimethyl chitosan (TMC) based, in which a titrated extract of Boswellia serrata (Boswellin®- BSW) has been enclosed, to be used as model drug for a colon specific drug delivery system. Methods: The synthesis of TMC has been performed through methylation reaction with Methyl iodide in basic medium, carefully modifying reaction steps and conditions in order to reach the desired Degree of Quaternization (DQ). The obtained polymers have been characterized by means of spectroscopic methods (FTIR, NMR and XRD). Water dispersions of TMC have also been submitted to physical- chemical analyses, such as determination of pH, rheological, evaporation-freezing assays and stability studies. TMC nanoparticles loaded BSW (BSW NP) have been prepared through ionotropic gelation method using tripolyphoshate (TPP). Results: TMC dispersions showed to be much stable overtime if compared with the corresponding Chitosan ones. Moreover TMC have been used for the preparation of BSW NP. The obtained BSW NP showed good polydispersity index (PDI), potential and are stable overtime. Particles size, drug loading capacity and efficiency were determined. BSW preliminary release in vitro tests were performed by HPLC. Data showed that BSW has been released from the polymer matrix in a prolonged and controlled manner. Conclusion: TMC could be considered a more promising derivative than chitosan itself for the preparation of NP. Opportunely varying the DQ, nanoparticulate drug delivery systems have been obtained, suitable for the preparation of colon specific drug delivery systems.
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