Folic acid-modified methotrexate-conjugated PEGylated poly(ε-caprolactone) nanoparticles for targeted delivery

Enhanced toxicity and cellular uptake of methotrexate-conjugated nanoparticles in folate receptor-positive cancer cells by decorating with folic acid-conjugated d -α-tocopheryl polyethylene glycol 1000 succinate

“…FOL was functionalized with propargylamine according to the reported method [31] with slight modification. In brief, to the solution of FOL (0.50 g, 1.13 mmol) in 15 mL of anhydrous dimethyl sulfoxide (DMSO), NHS (0.26 g, 2.26 mmol) and DCC (0.28 g, 1.36 mmol) were added under nitrogen atmosphere.…”

“…In case of P(MTXCLCL)-mPEG copolymers, the amount of MTX along the copolymer was quantified after hydrolyzed with a mixture of 50 mM borate buffer pH 9.5 and methanol (1:1 v/v) as reported elsewhere [31]. The unbound MTX in hydrolyzate was analyzed by HPLC method.…”

“…The MTX-conjugated (P(MTXCLCL)-mPEG) nanoparticles was prepared by dialysis method [31] using 10 and 20 %mol of MTX-conjugated copolymers. To prepare the targeted nanoparticles (FOL-P(MTXCLCL)-mPEG nanoparticles), the MTX-conjugated nanoparticles were decorated with TPGS-FOL.…”

“…The release behavior of MTX from the P(MTXCLCL)-mPEG nanoparticles was assessed by the published dialysis method [31] using dialysis bag with MWCO of 6000-8000 Da (Cellu-Sep T2, Bioron GmbH, Germany). The nanoparticles (7.5 mg/mL, 2 mL) were filled in the dialysis bag.…”

“…The amount of MTX was analyzed by the reported HPLC method using Shimadzu HPLC machine (Shimadzu Corporation, Kyoto, Japan) [31]. A reverse phase Hypersil ODS column (5 m particle size, 250 × 4.6 mm, Thermo Fisher Scientific Inc., USA) was used as a stationary phase.…”