Synergistic Combination of Camptothecin and through Selfassembly of Amphiphilic Drug Conjugate

Minxi Hu, Ping Huang, Yao Wang, Yue Su, Linzhu Zhou, Xinyuan Zhu,* and Deyue Yan*

School of Chemistry and Chemical Engineering, Shanghai Key Lab of Electrical Insulation and Thermal Aging, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, P. R.

* Correspondence to: [email protected]; [email protected]. Fax: +862154741297

Table of Contents

Supplementary Figures

1 Figure S1: H NMR spectra of CPT and CPTCOOH in DMSOd6.

Figure S2: FTIR spectra of CPT, FUDR, and CPTFUDR conjugate.

Figure S3: (A) UV/Vis spectra of CPT, FUDR and CPTFUDR conjugate in acetonitrile. (B) Fluorescence emission spectra of CPT (λ ex = 360 nm, λ em = 430 nm) and

CPTFUDR conjugate (λ ex = 360 nm, λ em = 426 nm) in DMSO.

Figure S4: The UV absorbance of DPH in an aqueous solution of CPTFUDR nanoparticles with various concentrations. The CAC value of CPTFUDR nanoparticles is about 15 M.

Figure S5: Influence of storage on (A) diameter (the diameter measured in Day 1 was set as control, and the data are presented as ratios to the control) and (B) PDI of CPTFUDR nanoparticles with the extension of time in water.

Figure S6: (A)Total ion chromatography (TIC) of CPT and CPTFUDR . (B, C) Extracted ion chromatography (EIC) of CPTFUDR (m/z = 693.1835, (M+H +)) and CPT (m/z = 349.1165, (M+H +)). The retention time of CPTFUDR and CPT is 3.92 and 3.79 min, respectively.

Figure S7: (A) Total ion chromatography (TIC) of the extracts. (B, C) Extracted ion chromatography (EIC) of CPTFUDR (m/z = 693.1853, (M+H +)) and FUDR (m/z = 349.1205, (M+H +)). The retention time of CPTFUDR and CPT is 3.93, and 3.80 min, respectively.

Figure S8: Flow cytometry histogram profiles of HT29 cells treated with CPTFUDR nanoparticles containing coreencapsulated Nile red for 30 min, 2 h and 4 h.

1 Figure S1. H NMR spectra of CPT and CPTCOOH in DMSOd6.

Figure S2. FTIR spectra of CPT, FUDR, and CPTFUDR conjugate.

Figure S3 . (A) UV/Vis spectra of CPT, FUDR and CPTFUDR conjugate in acetonitrile. (B) Fluorescence emission spectra of CPT (λ ex = 360 nm, λ em = 430 nm) and CPTFUDR conjugate (λ ex = 360 nm, λ em = 426 nm) in DMSO.

Figure S4. The UV absorbance of DPH in an aqueous solution of CPTFUDR nanoparticles with various concentrations. The CAC value of CPTFUDR nanoparticles is about 15 M.

Figure S5. Influence of storage on (A) diameter (the diameter measured in Day 1 was set as control, and the data are presented as ratios to the control) and (B) PDI of CPTFUDR nanoparticles with the extension of time in water.

Figure S6. (A)Total ion chromatography (TIC) of CPT and CPTFUDR. (B, C) Extracted ion chromatography (EIC) of CPTFUDR (m/z = 693.1835, (M+H +)) and CPT (m/z = 349.1165, (M+H +)). The retention time of CPTFUDR and CPT is 3.92 and 3.79 min, respectively.

Figure S7. (A) Total ion chromatography (TIC) of the cell extracts. (B, C) Extracted ion chromatography (EIC) of CPTFUDR (m/z = 693.1853, (M+H +)) and FUDR (m/z = 349.1205, (M+H +)). The retention time of CPTFUDR and CPT is 3.93, and 3.80 min, respectively.

Figure S8. Flow cytometry histogram profiles of HT29 cells treated with CPTFUDR nanoparticles containing coreencapsulated Nile red for 30 min, 2 h and 4 h.