Chitosan graft copolymer nanoparticles for oral protein drug delivery: preparation and characterization.
Several novel functionalized graft copolymer nanoparticles consisting of chitosan (CS) and the monomer methyl methacrylate (MMA), N-dimethylaminoethyl methacrylate hydrochloride (DMAEMC), and N-trimethylaminoethyl methacrylate chloride (TMAEMC), which show a higher solubility than chitosan in a broader pH range, have been prepared by free radical polymerization. The nanoparticles were characterized in terms of particle size, zeta potential, TEM, and FT-IR. These nanoparticles were 150-280 nm in size and carried obvious positive surface charges. Protein-loaded nanoparticles were prepared, and their maximal encapsulation efficiency was up to 100%. In vitro release showed that these nanoparticles provided an initial burst release followed by a slowly sustained release for more than 24 h. These graft copolymer nanoparticles enhanced the absorption and improved the bioavailability of insulin via the gastrointestinal (GI) tract of normal male Sprague-Dawley (SD) strain rats to a greater extent than that of the phosphate buffer solution (PBS) of insulin.
Qian
Feng
F
State Key Laboratory of Genetic Engineering, Department of Pharmaceutical Sciences, and Department of Biochemistry, School of Life Sciences, Fudan University, Shanghai 200433, China.
Cui
Fuying
F
Ding
Jieying
J
Tang
Cui
C
Yin
Chunhua
C
D000818:Animals; D001709:Biotechnology / Q000379:methods*; D048271:Chitosan / Q000737:chemistry*; D002794:Choline / Q000031:analogs & derivatives / Q000737:chemistry; D016503:Drug Delivery Systems; D007328:Insulin / Q000737:chemistry; D008297:Male; D008689:Methacrylates / Q000737:chemistry; D020366:Methylmethacrylate / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D036103:Nanotechnology / Q000379:methods; D011108:Polymers / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D019737:Transplants
D007328:Insulin; D008689:Methacrylates; D011108:Polymers; C491922:choline methacrylate; D020366:Methylmethacrylate; D048271:Chitosan; C519537:diethylaminoethyl methacrylate; D002794:Choline