Sm. Ahmed et al., DISRUPTION OF MICELLAR AGGREGATES OF GANGLIOSIDE GM-1 BY COMPLEXATIONWITH ALPHA-CYCLODEXTRIN, International journal of pharmaceutics, 109(2), 1994, pp. 99-106
As previously observed for model glycolipids, micellar aggregates of t
he ganglioside GM-1 can be disrupted by the formation of inclusion com
plexes with cu-cyclodextrin ((alpha-CD). Evidence for such disaggregat
ion was obtained from narrowing and shifting of H-1- and C-13-NMR sign
als, and decreasing of C-13-NMR relaxation times (T-1) upon addition o
f alpha-CD to aqueous (D2O) solutions of the ganglioside. As a result
of the alpha-CD-induced disaggregation, GM-1 becomes permeable through
100 000 Da cut-off ultrafiltration membranes (which are virtually imp
ermeable to normal GM-1 aggregates), and can be freed from phospholipi
d contaminants. beta-Cyclodextrin (beta-CD), which gives weaker comple
xes with GM-1, does not produce any significant disaggregation effects
. Also, fully methylated beta-cyclodextrin (Me beta-CD) and hydroxyeth
yl-beta-cyclodextrin (HE beta-CD) were ineffective. A solid complex (w
hich precipitates from solutions at alpha-CD/GM-1 molar ratios >5) was
obtained, and characterized by CP/MAS C-13-NMR spectroscopy and by DS
C.