Targeting moiety

Platform

Tumour model

Drug encapsulated

Study outcome

Ref.

Folate receptor

Dendrimer

Oral

Methotrexate (MTX)

Enhance localization in tumour and liver tissue. Increased MTX antitumour effects and reduced drug toxicity

[133]

Liposomes

Oral

Doxorubicin (DOX)

Internalization was 10 folds higher, significant reduction tumour growth and 30-50% increase in life span

[134,135]

Oral

Oligo-nucleotides

Showed no difference between targeted and nontargeted NP

[136]

Magnetite

Breast

No drug

Increased cellular internalization

[137]

PSMA antigen

PLGA-PEG

Prostate

Docetaxel

Effective uptake (77 fold increase) by cells, inhibited tumour growth and drug toxicity

[138,139]

Tranferrin receptor

Gold-PEG

Solid Tumour

No drug

Nps localized to the tumour tissues with decreased amounts in the liver

[140]

Liposome

Leukemia

DOX and Verapamil (Pgp inhibitor)

Cytotoxicity was 5.2 time greater that non-targeted NPs

[141]

Polymeric

Prostate/ Leukemia

Cyclodextrin

Efficient delivery of drugs to cells

[142]

PLGA

Prostate

Paclitaxel

Single dose induce complete inhibition of tumor growth and increased mouse survival rate (80%)

[143]

Epidermal receptors

HER-2-Liposome

Breast

No drug

No significant difference observed between targeted and nontargeted Nps.

[144]

 

Brain

Boron

Cellular increase by 8 fold was observed

[145]

EGF-gelatin

Lung

No drug

Enhanced uptake in cell in a time and dose dependent manner

[146]

αvβ3 integrin

Liposome

Pancreas/ Renal

Doxorubicin

NP targeted tumour vessel, induced selective apoptosis in tumour, caused a 15 fold increase in anti-metastasis activity and reduced systemic side effects

[147]

PLGA

Liver

Paclitaxel/ Doxorubicin

Hindered tumour growth and prolonged survival of mice

[148]

 

Melanoma/Colon

ATPμ-Raf mutant gene

Sustained tumour regression through cell apoptosis activation

[149]

Micelles

Connective tissue

Doxorubicin

30 fold increase of cellular uptake was observed

[150]

Vascular cell adhesion molecule (VCAM-1)

Liposomes

Lung

No drug

73.1 % localization seen within 30 min with only 30.3% seen with nontargeted NPs

[151]

Luteinizing hormone releasing hormone

Iron oxide

Breast

No drug

NPs were detected specifically in the cytosol of primary and metastatic tumours, whereas unconjugated NPs gathered in the liver

[152]

Sigma receptor

Liposomes

Lung

Survivin siRNA

Targeted NP enhanced delivery, downregulated survivn expression, induced cell cytotoxicity, apoptosis and chemosensitized cells to cisplatin. In vivo targeted NPs localized to specific tumour sites

[137]

Liposomes

Prostate

Doxorubucin

Increased accumulation, inhibited tumour growth and reduced systemic toxicity usually caused by the free drug

[153]

Table 1: Targeted nanoparticles for cancer therapy.