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. 2020 Apr 30;15:2999–3022. doi: 10.2147/IJN.S231479

Table 3.

Functionalized Nanocarriers Aiming to Glioma Therapy Employed in Preclinical Studies

Nanocarriers Drug Functionalization Experimental in vivo Model Achievements in vivo References
Polymeric nanoparticles TMZ Angiopep-2 Biodistribution of liposomes and efficacy in C6/ICR mouse glioma models Enhanced brain distribution of DOX and promising efficacy in glioma models [177]
Dendrimers TRAIL DNA Angiopep-2 Biodistribution of dendrimers and survival analysis in C6 mouse xenografts Increased survival of xenografts [106]
PCL nanoparticles DOX Angiopep-2 Pharmacokinetics, biodistribution and survival analysis in C6/Wistar rat glioma models Enhanced brain uptake of DOX, prolonged survival of glioma models [178]
PLGA nanoparticles IP10 Angiopep-2; EGFRvIII scFv Efficacy in U87-EGFRvIII cells xenografts Reduced tumour growth, prolonged survival of glioma models [179]
Liposomes Daunomycin Anti Tf Receptor antibody Pharmacokinetic & biodistribution in rats Increased daunomycin accumulation in brain [180]
Calcium phosphate nanoparticles ATF5 siRNA Apo E Glioma distribution, ATF5 expression and survival analysis in C6 mouse xenografts Efficient tumour targeting and increased survival of xenografts [181]
Polymersomes Saporin Apo E Biodistribution and efficacy in U87 mouse xenografts Specific brain accumulation of polymersomes, encouraging efficacy towards brain tumours [182]
SLN MTX prodrug Apo E chimera peptide Biodistribution and survival analysis in F98/Fischer rat glioma model Increased brain accumulation of MTX; encouraging efficacy [50]
Lipid nanoparticles Porphyrin Apo E3 Pharmacokinetics and biodistribution in mice, efficacy in U87 mouse xenografts Selective drug accumulation in brain tumour compared to healthy parenchyma [183]
Liposomes – Cetuximab Biodistribution in U87 mouse xenografts Increased brain accumulation of liposomes [113]
Liposomes DOX Chlorotoxin Biodistribution of liposomes and efficacy in U87 mouse xenografts Brain accumulation of liposomes, reduced tumour growth [117]
Polyionic micelles Cilengitide Cilengitide Survival analysis in C6/Wistar rat glioma models Prolonged survival of glioma models [184]
Polymeric micelles DACHPt Cilengitide Efficacy in U87 mouse xenografts Reduced tumour growth [185]
Liposomes DOX Cilengitide and Peptide 22 (LDL receptor) Biodistribution and survival analysis in intracranial glioma-bearing mice Prolonged survival time of glioma models [114]
PEG−PLA micelles PTX EGFR/EGFRvIII targeting peptide Pharmacokinetics in healthy rats, biodistribution and efficacy in U87 mouse xenografts Specific micelles distribution to the brain, reduced tumour growth in glioma models [186]
PEG-PLA nanoparticles PTX F3 peptide (targeting nucleolin) and tLyp-1 peptide (targeting neuropilin) Pharmacokinetics in rats; biodistribution and survival analysis in C6 mouse xenografts Enhanced PTX accumulation and deep penetration at the tumour location; prolonged survival in xenografts [115]
PEGilated liposomes DOX GSH Pharmacokinetics, biodistribution and efficacy in U87 mouse xenografts Enhanced brain retention of DOX; strong inhibition of brain tumour growth [110]
Liposomes DOX IL-13 Efficacy in U251 mouse xenografts Reduced tumour growth in glioma models [187]
BSA nanoparticles DOX Lf Pharmacokinetics in rats, biodistribution in C6/Wistar rat glioma model Increased brain uptake of DOX [188]
Cationic liposomes DOX Lf Biodistribution and survival analysis in C6/Wistar rat glioma models Increased accumulation of DOX in brain and prolonged survival time of glioma models [109]
Liposomes 99mTc-BMEDA Lf Pharmacokinetic & biodistribution in mice Increased brain accumulation [189]
Olive oil nanoparticles TMZ Lf Pharmacokinetic & biodistribution in healthy mice; biodistribution and efficacy in GL261/C57BL/6 mouse models Enhanced brain distribution of TMZ and promising efficacy towards glioma [190]
Olive oil nanoparticles Aurora Kinase B siRNA Lf Gene silencing and survival analysis in GL261/C57BL/6 mouse models Survival improvement of glioma models treated with nanoparticles and TMZ simultaneously [191]
PEG-PCL polymersomes DOX and tetrandrine Lf Pharmacokinetics, biodistribution and efficacy in C6/Wistar rat glioma model Improved DOX distribution in brain, reduced tumour growth and increased survival in glioma models [192]
PEG-PLA nanoparticles PTX Lf and tLyp-1 peptide (targeting neuropilin) Pharmacokinetics in healthy rats, biodistribution and efficacy in C6 mouse xenografts Enhanced tumour accumulation of PTX and increased survival of glioma models [53]
NLC TMZ and vincristine Lf, RGD Biodistribution and efficacy in U87 xenografts Specific brain distribution of the drugs, promising efficacy in glioma models [193]
Liposomes DOX and vincristine T7 and DA7R Biodistribution of liposomes and efficacy in C6/ICR mouse glioma models Enhanced brain distribution of liposomes and promising efficacy in glioma models [194]
Liposomes 5-fluorouracil Tf Biodistribution of radiolabelled liposomes in healthy rats Increased brain uptake of liposomes [195]
Liposomes TMZ and bromodomain inhibitor Tf Biodistribution in mice and efficacy in U87 mouse xenografts and C57BL/6 mouse models Improved liposomes distribution to the brain; promising efficacy in glioma models [196]
SLN MTX prodrug Tf, Insulin Biodistribution in healthy rats Increased brain accumulation of MTX [51]
Liposomes DOX Tf, Octaarginin Biodistribution of liposomes and efficacy in U87 mouse xenografts Prolonged survival of glioma models [197]
SLN Docetaxel HBA Pharmacokinetics and biodistribution in healthy rats Enhanced drug brain uptake [111]
SLN Docetaxel ketoconazole Folic acid Pharmacokinetics and biodistribution in healthy rats Enhanced drug brain uptake; P-gp overcoming [61]
PEG-co-PCL nanoparticles PTX Activatable LMWP coupled to a MMP-2/9-cleavable peptide sequence Pharmacokinetics in rats; biodistribution and efficacy in C6 mouse xenografts Specific PTX accumulation in glioma; enhanced efficacy in xenografts [116]

Abbreviations: 99mTc-labeled N,N-bis(2-mercaptoethyl)-N’,N’-diethylethylenediamine (99mTc-BMEDA); Apo, apolipoprotein; ATF5, activating transcription factor-5; C6, C6 cells; DA7R, DADTDWDLDPDPDR sequence, which has a high affinity for VEGFR 2; DACHPt, (1,2-diaminocyclohexane)platinum(II); DOX, doxorubicin; EGFR, epidermal growth factor receptor; EGFRvIII, mutant EGFR; F98, F98 cells; GL261, GL261 cells; GSH, glutathione; HBA, β-hydroxybutyric acid; IP10, Interferon-γ-inducible protein; LDL, low density lipoprotein; Lf, lactoferrin; LMWP, low-molecular-weight protein; MMP, matrix metalloproteinase; MTX, methotrexate; NLC, nanostructured lipid carriers; PCL, poly(ε-caprolactone); PEG, polyethylenglycol; P-gp, P-glycoprotein; PLA, poly-lactide; PLGA, poly-lactide-glycolide; PTX, paclitaxel; RGD, arginine-glycine-aspartic acid; scFv, single-chain Fv fragments; siRNA, small interfering RNA; SLN, solid lipid nanoparticles; T7, HAIYPRH sequence, which can bind to Tf receptors; Tf, transferrin; TMZ, temozolomide; TRAIL, tumor necrosis factor (TNF) related apoptosis-inducing ligand; U251, U251 cells; U87, U87 cells.