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Fig. 16 Post-loading of HPPH and CD-COOH in PAA NPs at variable ratios and their compar-
ative in vivo PDT efficacy in BALB/c mice (10 mice/group). The imaging and therapy dose:
0.47 μ mol/kg. For PDT, the tumors were irradiated with light (665 nm, 135 J/cm 2 , 75 mW/cm 2 )at
24 h postinjection
approach best conserved the PDT efficacy of HPPH [ 80 ]. In the follow-up studies,
different HPPH to CD ratios were examined to minimize the undesirable quenching
of HPPH electronic excitation energy due to FRET (fluorescence resonance energy
transfer). The finalized nanoparticle incorporated HPPH and CD with an amine
functional group in 2:1 ratio and demonstrated excellent tumor-imaging (NIR
fluorescence) and PDT efficacy in vivo [ 79 ] . A direct correlation between FRET
and PDT efficacy was observed. The nanoconstruct that showed higher FRET
produced lower long-term tumor cure.
Incorporation of different CD derivatives (either with an amine or a chlorine
functional group) was attempted for further optimization. Furthermore, F3 peptide
and PEG were covalently conjugated to the surface of the PAA nanoparticle [ 80 ].
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