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. 2011 Oct 24;50(44):10330-4.
doi: 10.1002/anie.201104510. Epub 2011 Sep 14.

Polysilsesquioxane nanoparticles for targeted platin-based cancer chemotherapy by triggered release

Joseph Della Rocca  1 , Rachel C Huxford, Erica Comstock-Duggan, Wenbin Lin
Affiliations

Polysilsesquioxane nanoparticles for targeted platin-based cancer chemotherapy by triggered release

Joseph Della Rocca et al. Angew Chem Int Ed Engl. .
No abstract available

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Figures

Figure 1
Figure 1
a) TEM micrograph of as-synthesized particles of 1. Scale bar = 200 nm. b) DLS curves for 1 (□), PEG-1 (○), and APEG-1 (▲). c) TGA curves for 1 (——), PEG-1 (---), and APEG-1 (-•-•). d) IC50 values of oxaliplatin, 1, and RGD-1 tested against a panel of four cancer cell lines.
Figure 2
Figure 2
a) Cell viability curves of oxaliplatin ( formula image; IC50 = (0.37 ± 0.02) μm), PEG-1 (▲; IC50 = (0.52 ± 0.08) μm), and APEG-1 (□; IC50 = (0.17 ± 0.01) μm) against AsPC-1 cells. b) Tumor growth inhibition curves for oxaliplatin (◇), PEG-1 ( formula image), APEG-1 (○), and PBS (■) administered at 5 mg Pt kg−1 on days 0, 7, and 14 against an AsPC-1 subcutaneous mouse xenograft.
Figure 3
Figure 3
Laser scanning confocal microscopy images of AsPC-1 cells after incubation with no particle, rhod-1, PEG-rhod-1, and APEG-rhod-1 for 1 h and then treated with Annexin V/FITC. The platin loadings are 5 μm for all the particles. The green fluorescence arises from FITC and the red fluorescence arises from rhodamine B. Scale bars = 50 μm.
Figure 4
Figure 4
Histology images of resected tumors (with H&E staining) from mice receiving a) saline control, b) oxaliplatin, c) PEG-1, and d) APEG-1. Scale bars = 0.5 mm. The blue-purple dots result from nuclear staining of viable cancer cells whereas pinkish areas indicate the lack of nuclear stains (i.e., necrotic tumor tissue with no viable cancer cells or nuclear material).
Scheme 1
Scheme 1
a) Generalized scheme showing the formation of PSQ particles 1 from the PtIV precursor. Upon cellular internalization and reaction with endogenous biomolecules, the PtIV complexes in 1 will be reduced, thereby releasing the active PtII agent. b) Surface functionalization of 1 by 1) the siloxane linkage formed between silanol groups and silyl-derived molecules, and 2) the amide linkage formed between carboxylic acid groups and amine-containing molecules.
See this image and copyright information in PMC

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