Synthesis and characterization of chitosan quaternary ammonium salt and its application as drug carrier for ribavirin.
N-(2-hydroxyl) propyl-3-trimethyl ammonium chitosan chloride (HTCC) is hydro-soluble chitosan (CS) derivative, which can be obtained by the reaction between epoxypropyl trimethyl ammonium chloride (ETA) and CS. The preparation parameters for the synthesis of HTCC were optimized by orthogonal experimental design. ETA was successfully grafted into the free amino group of CS. Grafting of ETA with CS had great effect on the crystal structure of HTCC, which was confirmed by the XRD results. HTCC displayed higher capability to form nanoparticles by crosslinking with negatively charged sodium tripolyphosphate (TPP). Ribavrin- (RIV-) loaded HTCC nanoparticles were positively charged and were spherical in shape with average particle size of 200 nm. More efficient drug encapsulation efficiency and loading capacity were obtained for HTCC in comparison with CS, however, HTCC nanoparticles displayed faster release rate due to its hydro-soluble properties. The results suggest that HTCC is a promising CS derivative for the encapsulation of hydrophilic drugs in obtaining sustained release of drugs.
College of Science, Guangdong Ocean University , Zhanjiang , P. R. China .
Si-Dong
SD
Li
Pu-Wang
PW
Li
Zi-Ming
ZM
Yang
Zheng
Z
Peng
Wei-Yan
WY
Quan
Xi-Hong
XH
Yang
Lei
L
Yang
Jing-Jing
JJ
Dong
D000998:Antiviral Agents / Q000008:administration & dosage / Q000138:chemical synthesis; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D048271:Chitosan / Q000008:administration & dosage / Q000138:chemical synthesis*; D004337:Drug Carriers / Q000008:administration & dosage / Q000138:chemical synthesis*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D012254:Ribavirin / Q000008:administration & dosage / Q000138:chemical synthesis*; D014961:X-Ray Diffraction
D000998:Antiviral Agents; D004337:Drug Carriers; C118071:N-trimethyl chitosan chloride; D012254:Ribavirin; D048271:Chitosan
Chemical modification; chitosan; drug delivery system; nanoparticles; ribavirin