Surface-modified gemcitabine with mucoadhesive polymer for oral delivery.
Gemcitabine microparticles were prepared using chitosan, polyethylene oxide or carbopol as the mucoadhesive polymer and eudragit L100-55 as the enteric polymer by a double emulsion method. The particle size and zeta potential changed from 1338.3 ± 254.1 nm to 2459.4 ± 103.6 nm and -5.16 ± 1.62 mV to 2.84 ± 0.65 mV, respectively, with increasing chitosan to gemcitabine weight ratio from 0.25 to 1. The gemcitabine-loaded microparticles without mucoadhesive polymer (F50) showed the particle size and zeta potential of 671.3 ± 58.3 nm and - 16.7 ± 1.82 mV, respectively. The cellular uptake of gemcitabine into Caco-2 cells from gemcitabine-loaded microparticles with chitosan increased with increasing incubation time in Caco-2 cells compared to that of gemcitabine-loaded microparticles with polyethylene oxide or carbopol, suggesting that chitosan might be the optimal mucoadhesive polymer. Gemcitabine microparticles will be tested to identify whether the oral absorption could be increased in the future.
College of Pharmacy and Institute of Drug Research & Development, Chungnam National University, 220 Gungdong, Yuseonggu, Daejeon 305-764, South Korea.
Ji-Ho
JH
Lim
Sung-Kyun
SK
You
Jong-Suep
JS
Baek
Chan-Ju
CJ
Hwang
Young-Guk
YG
Na
Sang-Chul
SC
Shin
Cheong-Weon
CW
Cho
D000180:Acrylic Resins / Q000737:chemistry; D000284:Administration, Oral; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D018938:Caco-2 Cells; D048271:Chitosan / Q000737:chemistry*; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D008863:Microspheres; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D011145:Polyvinyls / Q000737:chemistry*; D000093542:Gemcitabine
D000180:Acrylic Resins; D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; C446821:Eudragit L100-55; D011145:Polyvinyls; C006912:carboxypolymethylene; D003841:Deoxycytidine; D011092:Polyethylene Glycols; D048271:Chitosan; D000093542:Gemcitabine