Release characteristics of cisplatin chitosan microspheres and effect of containing chitin.
To increase cisplatin (CDDP) content, to suppress burst effect during the initial phase of drug release, and to improve the capacity of the system for sustained release, we prepared various types of CDDP chitosan microspheres incorporating chitin and investigated the content of CDDP and its in vitro release kinetics from these microspheres. The results of this study showed that the CDDP content increased with increasing chitosan concentration and that the incorporation of chitin in the carrier matrix produced a more pronounced increase in drug content. The addition of chitin also led to inhibition of the initial burst effect. The rate of CDDP release reduced with increasing concentration of chitosan: that is, the 50% CDDP release time was about 0.5 h with the microspheres prepared with 1.0% of chitosan and about 4.5 h with those prepared with 5.0% of chitosan, indicating about nine-fold prolongation. The addition of chitin further resulted in retardation of the rate of CDDP release. Meanwhile, our chitosan microspheres were shown to undergo enzymatic degradation by lysozymes.
Nishioka
Y
Y
Department of Pharmacy, Kochi Medical School Hospital, Japan.
Kyotani
S
S
Okamura
M
M
Miyazaki
M
M
Okazaki
K
K
Ohnishi
S
S
Yamamoto
Y
Y
Ito
K
K
D002686:Chitin / Q000031:analogs & derivatives* / Q000737:chemistry*; D048271:Chitosan; D002945:Cisplatin / Q000008:administration & dosage* / Q000737:chemistry; D003692:Delayed-Action Preparations; D005079:Excipients; D007202:Indicators and Reagents; D008863:Microspheres; D009113:Muramidase / Q000737:chemistry
D003692:Delayed-Action Preparations; D005079:Excipients; D007202:Indicators and Reagents; D002686:Chitin; D048271:Chitosan; D009113:Muramidase; D002945:Cisplatin