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O
O
OH
OH
N
OH
O
N
H
O
OH
O
HO
HO
OH
CHS-ED-LA
HO
O
O
O
O
O
44
O
PEG
2000
-CHEMS
Fig. 9 CHS-ED-LA and PEG
2000
-CHEMS.
N
O
N
SO
3
O
=
13
O
O
O
O
2
S
O
O
H
P
13
O
O
O
O
OH
P
N
OH
=
R
2
O
O
O
O
O
O
R
1
HO
=
AcHN
O
O
O
O
O
P
OH
P
OH
Fig. 10
D
-GalNAc-liposome formulation.
release, hepatic uptake, plasma and tissue distribution or even
hematological and estimation of enzymes, revealed a drug concentration
enhancement in the liver compared to free stavudine. Its biodistribution
was altered due to Gal-liposomes-lectin recognition which allowed the
delivery of drug directly to macrophages in a passive manner, thus re-
ducing drug toxicity and doses. The quality of patient life was improved
thanks to decreased side effects compared to free stavudine.
More recently,
D
-GalNAc liposomes were formulated by the in-
corporation of
D
-GalNAc-linked citronellol to
L
-a-phosphatidylcholine
and rhodamine-DHPE (Fig. 10).
26
In vitro studies on HepG2 cells,
monitored by fluorescence (rhodamine), pointed out the preferentially
endocytose manner of uptake. This could lead to apoptosis with the
appropriate drug (Dox for example) delivered into the parenchymal cells
carcinoma.
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