In vivo anti-tumor TPGS-TG assays were performed in MCF-7 tumor-bearing nude mice. When the tumor volume reached approximately 100–120 mm3, mice were randomly assigned to six groups (n = 6): (a) normal saline group (Control); (b) 375 mg/kg TPGS-TG (High TPGS TG); (c) 15 mg/kg Abraxane® (Abraxane); (d) blank TG combined with 15 mg/kg Abraxane® (Blank TG-Abraxane); (e) 375 mg/kg TPGS-TG combined with 15 mg/kg Abraxane® (High TPGS TG-Abraxane); and (f) 187.5 mg/kg TPGS-TG combined with 15 mg/kg Abraxane® (Low TPGS TG-Abraxane). Blank TG and TPGS-TG were administrated twice via intratumoral injection. Concurrently, Abraxane® was administrated by tail vein injection on days 1, 4, 7, 10, and 13. Body weights and tumor sizes were measured every 2 days. On day 14, mice were humanely sacrificed, and tumor tissue and main organs (liver, spleen, lung, and kidney) immediately sectioned and stained with H&E to assess tissue toxicity.