Tk. Saha et al., PREPARATION AND EVALUATION OF GLUTARALDEHYDE CROSS-LINKED CHITOSAN MICROSPHERES AS A GADOLINIUM RESERVOIR FOR NEUTRON-CAPTURE THERAPY, Chemical and Pharmaceutical Bulletin, 46(3), 1998, pp. 537-539
Chitosan microspheres (CMSs) containing water-soluble gadolinium dieth
ylenctriaminepentaacetic acid (Gd-DTPA) were prepared by an emulsion m
ethod using Span 80 as a surfactant and glutaraldehyde (GA) as a cross
-linker for the gadolinium neutron-capture therapy of cancer, When Gd-
DTPA was applied at more than a 1 : 1 number ratio of its carboxylic g
roups to the amino groups of chitosan, the content of Gd in CMS was sa
turated at about 13% and the mass median diameter of CMS was increased
beyond that of placebo CMS, The increase in the amount of Span 80 and
GA applied led to a decrease in the CMS size and the Gd content, The
electrostatic interaction between chitosan and Gd-DTPA and the prefere
ntial surface-hardening by GA contributed to the formation of fine, sp
herical, Gd-enriched and prolonged-releasing CMSs with a mass median d
iameter of 1.9 mu m, a Gd content of 6.1% and a 50% dissolution time o
f 2.3 h.