Figures & data
Notes: Aptamer-conjugated lipid–polymer ligands were synthesized by conjugating the aptamer to PLA-PEG-Mal. Redox-sensitive docetaxel prodrug (DTXp) was synthesized by conjugating the DTX with glyceryl monostearate (GM) using redox-responsive thiodiglycolic anhydride (TA).
Abbreviations PLA, poly(L-lactide); PEG, poly(ethylene glycol); APT, aptamer; DTX, docetaxel; GM, glyceryl monostearate; TA, thiodiglycolic anhydride; NMR, nuclear magnetic resonance; DTXp, docetaxel prodrug; MAL, maleimide.
Abbreviations PLA, poly(L-lactide); PEG, poly(ethylene glycol); APT, aptamer; DTX, docetaxel; GM, glyceryl monostearate; TA, thiodiglycolic anhydride; NMR, nuclear magnetic resonance; DTXp, docetaxel prodrug; MAL, maleimide.
Notes: Besides spherical in shape and uniform in size, APT-DTXp/DDP-LPHNs showed coats on the particles’ surface which do not exist in DTXp/DDP-LPHNs.
Abbreviations: TEM, transmission electron microscopy; APT, aptamer; DTXp, docetaxel prodrug; DDP, cisplatin; LPHNs, lipid–polymer hybrid nanoparticles.
Abbreviations: TEM, transmission electron microscopy; APT, aptamer; DTXp, docetaxel prodrug; DDP, cisplatin; LPHNs, lipid–polymer hybrid nanoparticles.
Notes: The stability of LPHNs in serum was investigated by mixing the LPHNs with FBS (55% in volume). The changes in particle size, zeta potential, and LE LPHNs were analyzed by the same methods. Data presented as mean ±SD, n=3.
Abbreviations: LPHNs, lipid–polymer hybrid nanoparticles; LE, loading efficiency; APT, aptamer; DTXp, docetaxel prodrug; DTX, docetaxel; DDP, cisplatin; FBS, fetal bovine serum.
Abbreviations: LPHNs, lipid–polymer hybrid nanoparticles; LE, loading efficiency; APT, aptamer; DTXp, docetaxel prodrug; DTX, docetaxel; DDP, cisplatin; FBS, fetal bovine serum.
Notes: Sustained release behaviors were observed for DTXp, DTX and/or DDP-loaded LPHNs. DDP release profiles of APT-DTXp/DDP-LPHNs, DTXp/DDP-LPHNs and APT-DDP-LPHNs were similar in hypoxic and normal condition. However, DTX release manners of APT-DTXp/DDP-LPHNs, DTXp/DDP-LPHNs and APT-DTXp-LPHNs were different, faster and more in hypoxic compared with normal condition. Data presented as mean ±SD, n=3.
Abbreviations: DTX, docetaxel; DDP, cisplatin; APT, aptamer; DTXp, docetaxel prodrug; LPHNs, lipid–polymer hybrid nanoparticles; H, hypoxic condition; N, normal condition.
Abbreviations: DTX, docetaxel; DDP, cisplatin; APT, aptamer; DTXp, docetaxel prodrug; LPHNs, lipid–polymer hybrid nanoparticles; H, hypoxic condition; N, normal condition.
Notes: FITC was applied to the LPHNs systems and incubated with A549 cells or BEAS2B cells for 2 h. The fluorescence intensity of the cells was determined by flow cytometer. Cell uptake of APT-DTXp/DDP-LPHNs was higher than that of non-modified DTXp/DDP-LPHNs. Data presented as mean ±SD, n=6. * P < 0.05.
Abbreviations: APT, aptamer; DTXp, docetaxel prodrug; DTX, docetaxel; DDP, cisplatin; LPHNs, lipid–polymer hybrid nanoparticles; FITC, fluorescein 5-isothiocyanate.
Abbreviations: APT, aptamer; DTXp, docetaxel prodrug; DTX, docetaxel; DDP, cisplatin; LPHNs, lipid–polymer hybrid nanoparticles; FITC, fluorescein 5-isothiocyanate.
Notes: Blank APT-LPHNs was nontoxic to A549 cells, while drug-loaded LPHNs and free drugs exhibited dose-dependent cytotoxicity. Drug-loaded LPHNs showed significantly higher cytotoxicity than free drugs, especially in lower concentrations. Aptamer-decorated APT-DTXp/DDP-LPHNs exhibited better cell inhibition ability than that of APT-DTXp-LPHNs, APT-DTX-LPHNs, APT-DDP-LPHNs, and non-decorated DTXp/DDP-LPHNs. Data presented as mean ±SD, n=6. * P < 0.05.
Abbreviations: LPHNs, lipid–polymer hybrid nanoparticles; MTT, 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide; APT, aptamer; DTXp, docetaxel prodrug; DTX, docetaxel; DDP, cisplatin.
Abbreviations: LPHNs, lipid–polymer hybrid nanoparticles; MTT, 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide; APT, aptamer; DTXp, docetaxel prodrug; DTX, docetaxel; DDP, cisplatin.
Notes: APT-DTXp/DDP-LPHNs showed higher tumor distribution than non-decorated DTXp/DDP-LPHNs. Single drug contained APT-DTXp-LPHNs and APT-DDP-LPHNs exhibited weaker tumor inhibition efficiency than APT-DTXp/DDP-LPHNs. Prodrug-based APT-DTXp-LPHNs gained smaller tumor size than that of APT-DTX-LPHNs at the end of the study. Data presented as mean ±SD, n=6. * P < 0.05.
Abbreviations: LPHNs, lipid–polymer hybrid nanoparticles; DTX, docetaxel; DDP, cisplatin; APT, aptamer; DTXp, docetaxel prodrug.
Abbreviations: LPHNs, lipid–polymer hybrid nanoparticles; DTX, docetaxel; DDP, cisplatin; APT, aptamer; DTXp, docetaxel prodrug.