TABLE 1.
Representation of Integrin targeted Liposomal preparation modified with RGD peptide.
| Composition of liposomal preparation | Particle diameter and zeta potential of targeted preparation | Anti-cancer molecule/gene therapy | Type of animal model | Type of cancer | Outcome of the study | References |
|---|---|---|---|---|---|---|
| Phosphatidylethanolamine, Cholesterol, Cholesteryl hemisuccinate (CHEMS) | 129.61 ± 3.2 nm and −26.38 mV | Docetaxel (DTX) | Female Balb/c nude mice | Breast cancer | Under same concentration, RGD based Ph sensitive liposome showed enhanced cytotoxicity than plain DTX and non-targeted liposome due to the tumor homing effect | Chang et al. (2015) |
| Phosphatidylethanolamine, cholesterol, PEG 2000, Linoleic acid | 146.4 ± 4.4 nm and −31.82 mV | DTX | Female Balb/c nude mice | Breast cancer | Dual targeting and PEG modified liposome enhanced the uptake while prolonging the circulation time | Zuo et al. (2016) |
| Cholesterol, phospholipid, Fructose, RGD | 113.6 ± 2.1 nm and 4.20 ± 0.17 | Paclitaxel (PTX) | Kunming and Balb/c mice | Triple negative breast cancer (TNBC) | The targeted preparation showed 2.62 times higher accumulation than non-targeted liposome | Pu et al. (2019) |
| Mal-PEG-DSPE, RGD | 60.85 nm and −42.3 mV | Diacedic norcantharidin (NCTD) | Nude mice | TNBC | The tumor growth and metastasis reduced after treatment with RGD modified preparation | Li et al. (2019) |
| 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), 1,2-distearoylphosphatidylethanolamine-methoxy-polyethylene glycol (DSPE-PEG2000), cholesterol, cRGD | 120.21 ± 5 nm and 11 ± 1.1 mV | miR-34a | — | TNBC | The targeted liposomes possibly improved the therapeutic efficiency of mRNAs in breast tumor cells and CSCs | Vakhshiteh et al. (2020) |
| DSPE-PEG2000-R8-RGD, SPC, Cholesterol, DSPE-PEG2000 | 105.9 ± 0.7 nm and −4.95 ± 0.59 | PTX | Balb/c | Glioma | The tandem R8-RGD peptide improved transportation of drugs across BBB, enhanced penetrability and tumor targeting | Liu et al. (2014) |
| Dipalmitoyl phosphatidylcholine (DPPC), cholesterol, TPGS, RGD | 182.3 ± 7.5 nm and 1.10 ± 0.25 | Docetaxel | Charles Foster Rats | Glioma | RGD-TPGS decorated theranostic liposomes were 6 fold more effective than plain DTX | Singh et al. (2016) |
| Mal-PEG3400-DSPE, HSPC (hydrogenated soy phosphatidylcholine) and mPEG2000-DSPE, cholesterol | 115.17 ± 1.01 nm, — | Doxorubicin | BALB/c | Glioma | The multifunctional targeted drug delivery system improved the uptake and anti-glioma activity | (Z et al., 2017) |
| Methoxypolyetheleneglycol (Mw 2000)-distearylphosphatidylethanolamine (DSPE-PEG), SPC, Cholestrol, RGDm | 211 nm, — | Doxorubicin | C57BL mice | Melanoma | RGDm modified preparation at dose 5 mg/kg of DOX prolonged the survival time manyfold | Xiong et al. (2005a) |
| Methoxypolyetheleneglycol (Mw 2000)-distearylphosphatidylethanolamine (DSPE-PEG), SPC, Cholestrol, RGD | — | Doxorubicin | C57BL/6 mice | Melanoma | The circulation time and tumor accumulation was demonstrated after treatment with targeted preparation | Xiong et al. (2005b) |
| Methoxypolyethelene glycol (Mw = 2000)–distearyl phosphatidylethanolamine (DSPE PEG), Cholestero, egg phosphatidylcholine (EPC), RGD | 90.54 ± 0.34, 1.01 ± 0.65 | Combretastatin A-4 and DOX | C57BL/6 | Melanoma | Co-encapsulation of vascular disrupting and anti-cancer agents revealed excellent results for tumor therapy | Zhang et al. (2010) |
| DSPE PEG 2000, egg phosphatidylcholine, cholesterol, monomeric cRGD peptide (mo-RGD), dimeric cRGD peptide (di-RGD) and flexible dimeric RGD peptide (di-P-RGD) | 100 nm, — | — | C57BL/6 | Melanoma | Delivery system designed based on concern over receptor clustering improved the binding potential of RGD | Guo et al. (2014) |
| DSPE, Cholesterol. TH peptide with a terminal cysteine [AGYLLGHINLHHLAHL (Aib) HHIL-Cys], TR peptide with a terminal cysteine [c (RGDfK)-AGYLLGHINLHHLAHL (Aib)HHIL-Cys] | 126.4 ± 0.566 nm and −4.56 ± 0.48 mV | PTX | C57BL/6 | Melanoma | The TR- liposome enhanced the cellular internalization and improved the survival rate | Shi et al. (2015) |
| Hydrogenated soya phosphatidylcholine (HSPC), Cholesterol, DSPE-mPEG (2000), RGD | 87.9 ± 3.9 nm, in between −19 and −21 mV | Bufalin | — | Lung cancer | The targeted therapy improved the anti-proliferation activity by prolonging circulation time and improving cellular internalization | ZhangY. et al. (2019) |
| Cholesterol, Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE), DSPE-128 mPEG 2000), cRGD | 125.06 ± 4.90 and 11.78 ± 0.21 mV | siRNA | Swiss albino wistar rats | Lung cancer | The liposomal preparation with siRNA inhibited the viability of A549 cells | Khatri et al. (2014) |
| HSPC, mPEG2000-DSPE, cholesterol and α-tocopherol | 115.9 ± 2.4, — | DOX | BALB/c | Colon cancer | RGD peptide with intermediate hydrophilicity made headway to control tumor growth and improve the survival time | Amin et al. (2013) |
| Egg phosphatidylcholine, DSPE-PEG2000, (DOTAP) chloride, CaCO3 | Between 115 and 120 nm, zeta potential ranged between 20 and 25 mV | PTX + Protein (BSA) | Male ddY mice and BALB/c mice | Colon cancer | pH sensitive release of drug and targeting of nanoparticle synchronized the bio-distribution leading to significant anti-tumor activity | Peng et al. (2019) |
| DSPE-PEG2000, Cholesterol, RGD, TAT-Cysteine peptide | 89.41 ± 0.80 and 1.18 ± 0.92 | — | HepG2 xenograft nude mice (specie not explained) | Liver cancer | The synergic effect shown by RGD and TAT modified liposomes enhanced the lysosomal escape, clustering the nanocarrier in the cytoplasm | Mei et al. (2014) |
| DSPE-PEG, Chlorodimethyloctadecylsilane, distearoyl phosphatidylcholine (DSPC), RGD | 152 nm, 20 mV | Arsenic trioxide | H22 tumor xenograft mice | Liver cancer | The nanocarrier with controlled release and targeted therapy modified the anti-cancer potency of arsenic trioxide | Fei et al. (2017) |