Biomedical Engineering Reference
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CH
3
(CH
2
)
m
O
CH
2
CH
3
(CH
2
)
m
O
CH
O
O
O
NO
2
OP
O
−
H
OCH
2
CH
2
NH
C
(CH
2
CH
2
O)
n
O
CH
2
O
C
pNP-PEG-PE
+
Ligand
NH
2
aqueous buffer, pH 8 -9.5
CH
3
(CH
2
)
m
O
CH
2
CH
3
(CH
2
)
m
O
CH
O
O
O
(CH
2
CH
2
O)
n
NH
Ligand
OP
O
−
H
O
CH
2
CH
2
NH
C
O
C
CH
2
Fig. 2
Schematic of amino-group-containing ligand, such as peptide attachment using pNP-
PEG-PE
Liposome
Micelle
CPP moiety
Hydrophilic
spacer
Hydrophobic
anchoring group
Water insoluble
drug
Water soluble drug
Fig. 3
CPP attached to liposomes and micelles by the insertion into the hydrophobic phase of
liposome membrane or micelle inner core via a spacer arm (linker) with a hydrophobic “anchor”
TATp-liposomes remained intact in the cell cytoplasm at 1 h of translocation
since the fluorescence of the intraliposomal (FITC-dextran) and membrane
(rhodamine-PE) labels coincided (Fig.
4
). After 2 h, they had migrated into the
perinuclear zone and after several hours, the liposomes had completely disinte-
grated (Torchilin et al.
2003a
).
One of the major obstacles to the use of TATp-mediated intracellular delivery
of pharmaceutical nanocarriers is the lack of selectivity of TATp. This non-
selectivity has generated concern about drug-induced toxic effects towards
normal tissues. This suggested that intratumoral administration of TATp containing
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