Journal
CARBOHYDRATE POLYMERS
Volume 240, Issue -, Pages -Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2020.116239
Keywords
Tumor-associated macrophage; Tumor-targeting therapy; Photodynamic therapy; Alginate; Phthalocyanine; Conjugate
Categories
Funding
- Marine High-Tech Programs of Fujian Province, China [2016-14]
- Natural Science Foundation of Fujian Province, China [2016J01055, 2018J05016]
- National Natural Science Foundation of China [U1705282, 21907015]
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Tumor-associated macrophages (TAMs)-targeted photodynamic therapy (PDT) has dual-selectivity and hence is promising in cancer treatment. Since the scavenger receptor-A (SR-A) on TAMs can recognize polyanions, two molecular-weight sodium alginates (SA1, 41.2 kDa; SA2, 1231.5 kDa) were herein respectively conjugated with 1-[4-(2-aminoethyl) phenoxy] zinc (II) phthalocyanine (1) and two novel conjugates were obtained, characterized and evaluated for their TAMs-targeted PDT efficacy. The SA introduction makes 1 water-soluble, less aggregated and capable of emitting considerable fluorescence in water. Compared with 1, both conjugates, especially 1-SA1, can give higher selectivity and photocytotoxicity to SR-A-positive macrophages J774A.1 than SR-A-negative HepG2 cells. The in vivo biodistribution evaluation shows both conjugates can selectively accumulate at the tumor site and 1-SA1 owns higher tumor accumulation. 1-SA1 can achieve an 87 % tumor inhibition rate without observable systemic toxicity. These results reveal the great potential of SA as a carrier for conjugating anti-tumor drugs and 1-SA1 for TAMs-targeted PDT.
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