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. Author manuscript; available in PMC: 2022 Jan 10.
Published in final edited form as: J Control Release. 2020 Oct 1;329:624–644. doi: 10.1016/j.jconrel.2020.09.055

Table 1.

Stimuli-responsive peptide-functionalized liposomal formulations entrapping anticancer agents for targeted therapy of cancer

Surface attached peptide Anticancer agent Liposome formulation Targeted cancer type Peptide Target site/ Action Size (nm) Reference
CPP: H7K(R2)2 DOX DSPE-PEG-NHS Brain (in vitro and in vivo) Cell penetrating and pH responsive peptide targeting glioma tumor cells 92.19 [87]
CPP: GGRRRRRRRRR-amide DOX SPC-STR-EDCl-NHS-mPEG2000-hydrazone-stearate Breast cancer (in vitro and in vivo) CPP-facilitated delivery of anticancer agent in breast cancer. 121.25 [94]
Print3G Calcein DOPE:CHEMS:CHO
L:PEG750-DSPE (43:21:30:6)
Breast cancer (in vitro) Antagonist of an oncoprotein involved in breast cancer growth and invasion 162.6 163.8 [120]
CPP: [D]-H6L9 PTX DSPE-PEG2000 Breast cancer Integrin αvβ3 targeting by peptide and drug release by local hyperthermia 130–135 [95]
D[KLAKLAK]2 (KLA) PTX SPC:CHOL:PTX = 10:1:1 SPC:DKD:CHOL:PTX = 8:2:1:1 Lung cancer Initiates apoptotic cell death 132 [121]
ELAAWCRWGFLL ALLPPGIAGGGC Vaccine DMPC:DMPG:Chol: DOPE Breast cancer Activation of cytotoxic T lymphocytes (CTLs) 126–142 [122]
CGKRKD(KLAKLAK)2 DTX PBAE-PEG Breast cancer (in vitro) Angiogenic blood vessels in tumors 117 [96]
TDSILRSYDWTY TDSILRSYDGGG DOX NHS-PEG-DSPE Lung metastasis Non-small cell lung cancer (NSCLC) cells 65–75 [123]
H peptide RF peptide K peptide miR-200 Irinotecan DSPE:PEG Colorectal cancer Tumor neovasculature undergoing angiogenesis, and one mitochondria-targeting peptide 147–174 [124]
KSSPHSRN(SG)5RG DSP Calcein DOPE:CHEMS:DSPE-PEG2000 Colon cancer Cell-adhesion domain of fibronectin, specifically integrin α5β1 receptor 98.36 [125]
NGR DOX DPPC:MSPC:DSPE-PEG2000-NGR:DiO:: 85.2:9.7:5:0.1 Breast cancer and metastasis CD13/ aminopeptidase N 107.8 [126]
CPP: CRGDRGPDC [iRGD] DOX DSPE-PEG2000:MPPC:DPPC Liver cancer αvβ3 integrins and neuropilin-1 84 [127]
CPP: CKRRMKWKK siRNA DPPC:MSPC:DSPE-PEG2000:: 87:3:10 Breast cancer (in vitro and in vivo) CPP-facilitated delivery of anticancer agent 90 [128]
Cyclic RGD DOX DSPC/DPPC:DSPE-PEG (or DSPE-PEG-cRGD):cholesterol:E LP = 55:2:10:0.55 Breast cancer (in vitro and in vivo distribution) αvβ3 integrin 181 [129]
CPP: CKRRMKWKK DOX DPPC: MSPC: (DSPE-PEG2000-NGR or DSPE-PEG2000) :: 87:3:10 Fibrosarcoma (in vitro and in vivo study) CPP-facilitated delivery of anticancer agent 82–89 [130]
CREKA DOX DPPC, MSPC, DSPE-PEG, and DSPE-PEG-CREKA (86:10:2:2 molar ratio) Breast cancer Targeted clotted plasma proteins in tumor vessels and temperature triggered release of DOX 83.8 [131]
CCRGDKGPDC DOX DSPE-PEG2000-maleimide Breast tumor model αvβ3 integrin 94.2 [132]
CPP: CGRRMKWKK Campothecin DSPE-PEG2000, DSPC and DPPC (molar ratio of 10:10:90) Cervical cancer (in vitro and in vivo CPP-facilitated and ultrasound triggered delivery of anticancer agent 189–190 [103]
CPP: CKRRMKWKK NGR: CYGGRGNG DOX DSPE-PEG2000-NGR Breast cancer (in vitro and in vivo) CPP-facilitated delivery of anticancer agent 195–202 [104]
AG73: CGGRKRLQVQLSIRT DOX DSPC and DSPE-PEG2000-OMe Colon cancer cells in-vitro study Syndecan-2 targeting combined with ultrasound trigger release 130–170 [133]
Elastin like polypeptide DOX DPPC:DSPE-PEG-2000:cholesterol:SA-ELP3-NH2 = 55:2:15:0.4125 Squamous cell carcinoma (in vitro and in vivo) Facilitated stimuli-responsive release of anticancer agents 161.8 [134]
CPP: CKRRMKWKK siRNA DSPC and DPPC In vivo distribution and cellular uptake in human breast adenocarcino ma cells CPP-facilitated delivery of anticancer agent 201 [135]
CPP: CKRRMKWKK (derived from Penetratin) DOX DPPC:MSPC:DSPE-PEG2000 (87:3:10) Fe3O4 Breast cancer (in vitro and in vivo study) CPP facilitated magnetic hyperthermia-triggered release of DOX 90–100 [136]
CPP: R8 PTX Cholesterol:SPC: DSPE-PEG2K-R8(35:65:0.8) Breast cancer (in vitro and in vivo study CPP facilitated and pH sensitive release of PTX 120 [137]
PEGylated cleavable lipopeptide (PCL) H-G-Trp(Boc)-I-P-V-Ser(tBu)-L-Arg-(Pbf)-Ser(tBu)-G-Glu(tBu)-Glu(tBu)-Glu(tBu)-Glu(tBu)PEG2000 DOX POPC:Cholestrol:PCL (60:35:5) Prostate adenocarcino ma (in vitro and in vivo) MMP enzyme facilitated cleavage and ultrasound triggered release of DOX 127 [138]

Abbreviations: CPP, cell penetrating peptide; Chol, cholesterol; CHEMS, cholesteryl hemisuccinate; DSPE-PEG2000, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[poly(ethylene glycol) 2000]; DOX, doxorubicin; DTX, docetaxel; DPPG-Na, dipalmitoyl phosphatidylglycerol; DPPC, dipalmitoyl phosphatidylcholine; DOPE, Dioleoylphosphatidylethanolamine; DSPC, distearoylphosphatidylcholine; DSPE-PEG2000-OMe, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] EDCI, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride; mPEG2000-hydrazone-stearate (mPEG2000-Hz-stearate); HSPC, hydrogenated soy phosphatidylcholine; MSPC, 1-myristoyl-2-stearoyl-sn-glycero-3-phosphocholine; MPPC, 1-myristoyl-2-palmitoyl-sn-glycero-3-phosphocholine; DSPE-PEG-NHS, 3-(N-succinimidyloxyglutaryl)aminopropyl; PBAE-PEG, poly(beta-amino ester) poly(ethylene glycol); PTX, paclitaxel; STR, stearate; SPC, soy phospholipids.