A near-infrared fluorescent heptamethine indocyanine dye with preferential tumor accumulation for in vivo imaging

Preliminary Structure–activity Relationship Study of Heptamethine Indocyanine Dyes for Tumor-Targeted Imaging

“…As shown in Table 1, except the compound 5 synthesized by our laboratory, 9 all the heptamethine indocyanine dyes reported in this work were purchased from American Dye Source Incorporation (ADSL, Quebec, Canada), Sigma-Aldrich Corporation (SAC, Shanghai, China), or Spectrum Information Ltd (SIL, NJ, USA), respectively. These dyes were dissolved in dimethylsulfoxide (DMSO) diluted with appropriate vehicles and stored at À20 C before use.…”

“…9 Brie°y, three-to fourweek-old athymic nude mice were purchased from the laboratory animal center of the Third Military Medical University. Mice were injected subcutaneously in the right°ank with 2 Â 10 6 MCF-7 cultured cells suspended in 200 ul PBS.…”

“…To evaluate the dynamic dye accumulation and retention in tumors, the contrast index (CI) values were calculated as described in the a The bioactivity of these dyes was determined according to our published protocols. 9 The bioactivity was positive when the contrast index (CI) more than 2.5 in the MCF-7 tumor xenograft, while the dye with a CI value less than 2.5 was regarded as negative bioactivity. The°uorescent intensity was calculated using Kodak MI software 5.0.1. b \À" represents negative bioactivity (CI < 2.5).…”

Microfluidic platform for photodynamic therapy cytotoxicity analysis of nanoencapsulated indocyanine-type photosensitizers

“…¼ 805 nm) wavelengths and high molecular extinction coefficient (e ¼ 27.4 Â 10 4 M À1 cm À1 ) has been adopted so far as a non-targeting contrast agent in clinical and experimental NIR imaging and as a promising second generation photosensitizer in PDT. [36][37][38][39] However, IR-780 as many other hydrophobic cyanines can be disposed to light-induced decomposition (i.e., photobleaching) both in vitro and in vivo resulting in the loss of absorbance, fluorescence, and photoactivity, and thus possibly limiting its use in PDT. 40 In order to increase the potential of hydrophobic cyanines towards improvement of drug efficacy, its stability, and better intracellular penetration, they need to be encapsulated in nanocarriers to avoid any unexpected problems with photoactivity and to improve their dissolution performance by means of encapsulation via template-mediated processes.…”

“…40 In order to increase the potential of hydrophobic cyanines towards improvement of drug efficacy, its stability, and better intracellular penetration, they need to be encapsulated in nanocarriers to avoid any unexpected problems with photoactivity and to improve their dissolution performance by means of encapsulation via template-mediated processes. 27,37 The main objective of this work is a basic research focused on examination of the mechanism and effectiveness of the introduction of a photosensitizer to carcinoma cells in the form of nanocarriers such as PE nanocapsules and then performing cytotoxicity tests during photodynamic therapy based on the use of model conditions and designed system lab-on-a-chip. Newly encapsulated hydrophobic indocyanine-type photosensitizer (i.e., IR-780) was subjected to in vitro studies to determine its release characteristics on a molecular level.…”