Novel quaternized chitosan and polymeric micelles with cross-linked ionic cores for prolonged release of minocycline.
Novel multifunctional octadecyl quaternized carboxymethyl chitosans (OQCMCs) with varying degree of quaternary substitution (DS) and molecular mass were prepared and compared with quaternized chitosan. OQCMCs exhibited excellent solubility both in water and organic solvents. Nanoparticles of OQCMCs offered many advantages, such as easier fabrication and modulation of their size and degree of positive charge, and a lower cytotoxic effect compared with PEI (25 kDa). DNA can be successfully adsorbed on its surface. Electrostatic attraction of carboxymethyl and quaternary groups in OQCMCs was utilized as micellar template for the synthesis of cross-linked micelles. Formation and characteristics of OQCMC polymeric micelles were studied by fluorescence spectroscopy, tensiometry, SEM, TEM and particle size analysis. Self-assembled OQCMC micelles were evaluated as carrier of the lipophilic drug, minocycline hydrochloride (MH). MH was incorporated into cross-linked ionic cores of micelles with remarkably high efficiency (22.7%, w/w). MH-loaded OQCMC polymeric micelles exhibited a slow steady release profile over a 1-week period at 37 degrees C. The OQCMC micelles are potentially useful for gene and lipophilic drug delivery applications.
Liang
Xiaofei
X
Institute of Nanobiotechnology, School of Materials Science and Engineering, Tianjin University, Tianjin 300072, P. R. China.
Tian
Hui
H
Luo
Hao
H
Wang
Hanjie
H
Chang
Jin
J
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000378:metabolism; D001672:Biocompatible Materials / Q000737:chemistry / Q000378:metabolism; D002460:Cell Line; D048271:Chitosan / Q000031:analogs & derivatives* / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D008422:Materials Testing; D051379:Mice; D008823:Micelles; D008911:Minocycline / Q000737:chemistry / Q000378:metabolism; D015394:Molecular Structure; D010316:Particle Size; D011108:Polymers / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D001672:Biocompatible Materials; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; C514968:carboxymethyl-chitosan; D048271:Chitosan; D008911:Minocycline