Biomedical Engineering Reference
In-Depth Information
2.5 mgmL
21
.
55
Conjugating one or two molecules to short oligomer chains
of ethylene glycol (OEG) via b-thioester bonds produces an amphiphilic
phospholipid-mimicking prodrug OEG-CPT or OEG-DiCPT (Figure 11.4).
These prodrugs can self-assemble in aqueous solution into stable liposome-like
nanocapsules of around 100 nm in diameter (Figure 11.4A). As shown in
Figure 11.4, the hydrophobic wall of the vesicle contains no aliphatic chains
like normal liposomes but is solely made of hydrophobic CPT drug molecules.
Thus, the drug content is as high as 40 or 58 wt%. Another important
characteristic is that since the nanocapsules or vesicles are made of the prodrug
with well-defined structures, their drug content is fixed independently of the
d
n
4
y
3
n
g
|
5
Figure 11.4
(A) Scheme of phospholipid-mimicking prodrugs OEG-DiCPT self-
assembling into stable liposome-like nanocapsules to load other drugs.
(B) CPT release kinetics from the OEG-DiCPT nanocapsules. (C) In
vivo antitumor activity of OEG-DiCPT to xenografted intraperitoneal
SKOV-3 ovarian tumors in BALB/c strain nu/nu mice. (Adapted from
Shen et al.
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with permission from the American Chemical Society.)
