. 2022 Apr 6;14(4):797. doi: 10.3390/pharmaceutics14040797

Table 2.

Current research on active tumor-targeted drug NCs delivery systems conducted both in vitro and in vivo.

Targeting Moieties	Receptor	Model Drug	Stabilizer	Preparation Technique	Particle Size (nm)	Morphology	Evaluation of Efficacy and Safety		References
Targeting Moieties	Receptor	Model Drug	Stabilizer	Preparation Technique	Particle Size (nm)	Morphology	In Vitro	In Vivo	References
Evaluation in subcutaneous animal models
FA	FR	PIK-75	F68 and SBL-PC	High pressure homogenization	161 ± 40	Sphere	SK-OV-3 cells	Subcutaneous SK-OV-3 tumor-bearing mice	[89]
FA	FR	HCPT	/	Supercritical antisolvent precipitation followed by ultrasonic dialysis	189.7 ± 9.5	Needle; core-shell after encapsulation into nanocomplex	KB, HeLa and A549 cells	Subcutaneous KB tumor-bearing mice	[94]
FA	FR	053	F127	Wet ball milling followed by ultrasonication	≈183.3	Rod; core-shell after encapsulation into liposomes	K562 and KU812 cells	Subcutaneous K562 tumor-bearing mice	[95]
Tf	TfR	PTX	/	Solvent-antisolvent precipitation	304 ± 13	Rod	SK-OV-3 and KB cells	Subcutaneous KB tumor-bearing mice	[99]
Albumin	SPARC	PTX	F127	Solvent evaporation	196.7 ± 34.6	Rod	B16F10 cells	Subcutaneous B16F10 tumor-bearing mice	[104]
CS	CD44	DTX	PEG and PVP	High pressure homogenization	194 ± 9	Rod	MDA-MB-231, MCF-7 and 4T1 cells	Subcutaneous 4T1 tumor-bearing mice	[110]
MA	MR	Poly I:C and PTX	CLG	Solvent-antisolvent precipitation	≈218	Rod	B16F10 cells	Subcutaneous B16F10 tumor-bearing mice	[113]
HCT	HER2	PTX	PCL-PEG	Solvent evaporation	144 ± 16	Worm-like	SK-BR-3 and MDA-MB-231 cells	Subcutaneous SK-BR-3 tumor-bearing mice	[116]
RGD peptide	Integrin α_Vβ₃	PTX	TPGS and citrate acid	Solvent evaporation	419.9 ± 80.9	Near-sphere	A549 cells	Subcutaneous A549 tumor-bearing mice	[92]
Evaluation in orthotopic animal models
Albumin	SPARC	CFZ	F127	Solvent evaporation	270.8 ± 21.5	Rod	MDA-MB-231, MCF-7, HCC1143, HCC1937 and 4T1 cells	Orthotopic 4T1 tumor-bearing mice	[105]
RGD peptide	Integrin α_Vβ₃	DTX	F127	Solvent evaporation	≈70	Irregular; core-shell after RBC membrane coating	U87 cells	Subcutaneous and orthotopic U87 tumor-bearing mice	[26]
^DWSW peptide	QSR	PTX	PVP and SDC	Solvent-antisolvent precipitation	≈169	Sphere; core-shell after C6 cancer cell membrane coating	4T1, B16F10, HepG2 and C6 cells	Orthotopic C6 tumor-bearing mice	[128]

Notes: A549 cells, human non-small cell lung cancer cell line; B16F10 cells, murine melanoma cell line; CFZ, carfilzomib; CLG, cationic β-LG; CS, chondroitin sulfate; C6 cells, rat glioma cell line; DTX, docetaxel; FA, folic acid; FR, folate receptor; F127, Pluronic F127; F68, Pluronic F68; HCC1143 cells, human breast cancer cell line; HCC1937 cells, human breast cancer cell line; HCPT, 10-hydroxycamptothecin; HCT, Herceptin^®; HeLa cells, human cervical carcinoma cell line; HepG2 cells, human hepatocellular carcinoma cell line; HER2, human epidermal growth factor receptor 2; KB cells, human epithelial carcinoma cell line; KU812 cells, human chronic myeloid leukemia cell line; K562 cells, human chronic myeloid leukemia cell line; MA, D-mannuronic acid; MCF-7 cells, human breast cancer cell line; MDA-MB-231 cells, human breast cancer cell line; MR, mannose receptor; NCs, nanocrystals; PCL-PEG, poly(ε-caprolactone)-co-poly(ethylene oxide); PEG, polyethylene glycol; PTX, paclitaxel; PVP, polyvinyl pyrrolidone; QSR, quorum-sensing receptor; RBC, red blood cell; SBL-PC, soybean lecithin with 70% phosphatidylcholine; SDC, sodium deoxycholate; SK-BR-3 cells, human breast cancer cell line; SK-OV-3 cells, human ovarian cancer cell line; SPARC, secreted protein acidic and rich in cysteine; Tf, transferrin; TfR, transferrin receptor; TPGS, D-α-tocopherol polyethylene glycol 1000 succinate; U87 cells, human glioma cell line; 4T1 cells, murine breast cancer cell line.