Application of poly(ethylene glycol)–distearoylphosphatidylethanolamine (PEG-DSPE) block copolymers and their derivatives as nanomaterials in drug delivery

Figures & data

Figure 1 Synthesis of amino-PEG-DSPE.¹⁵

Abbreviations: PEG, polyethylene glycol; Boc, tert-butyloxycarbonyl; DSPE, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine; TEA, triethylamine.

Figure 2 Synthesis procedure of maleimide-PEG-DSPE.²⁴

Abbreviations: Mal, β-(N-maleimido) propionyl; Mal-PEG-SC, ω-Mal-α-succinimidyl carboxylate; MPS, N-(maleimido-propionyloxy)-succinimide ester; TEA, triethylamine.

Table 1 Nonantibody targeting moieties grafted to PEG-DSPE for cancer therapeutics

Nonantibody targeting moieties	Target	Target cells or tissues	References
Folate	Folate receptor	Cancer cells that overexpress the folate receptor	^Citation30,Citation32
Transferrin	Transferrin receptor	Cancer cells that overexpress the transferrin receptor	^Citation33,Citation34
Asn-Gly-Arg (NGR)	Aminopeptidase N (CD13)	Vasculature endothelial cells	^Citation26,Citation35
Leu-Ala-Arg-Leu-Leu-Thr (D4) or GE11	Epidermal growth factor receptor (EGFR)	Cancer cells that overexpress EGFR	^Citation6,Citation36
Galactose residues	Hepatic asialoglycoprotein receptor (ASGP-R)	Activated platelets, hepatocyte	^Citation37,Citation38
Arg–Gly–Asp (RGD)	Integrins	Vasculature endothelial cells	^Citation39,Citation40
Anisamide ligand	Sigma receptor	Human lung cancer cells	^Citation41
Vasoactive intestinal peptide (VIP)	VIP receptors	Breast cancer	^Citation42

Abbreviations: NGR, asparagine- glycine- arginine; CD13, Aminopeptidase N; D4, leucine-alanine-arginine-leucine-leucine-threonine; GE11, an amino acid sequence YHWYGYTPQNVI; EGFR, epidermal growth factor receptor; ASGP-R, hepatic asialoglycoprotein receptor; RGD, arginine-glycine-aspartic acid; VIP, Vasoactive intestinal peptide.

Table 2 Antibody targeted moieties grafted to PEG-DSPE for targeted delivery

Antibody targeting moieties	Target	Target cells or tissues	References
Anti-CD19	CD19 epitope	B lymphoma cells	^Citation48,Citation54
Anti-CD20	CD20, a B-cell surface antigen	B-cell malignancies	^Citation46,Citation55
Anti-CD22	CD22, a B-cell surface antigen	Non–Hodgkin’s lymphoma and other B-cell lymphoproliferative diseases	^Citation47,Citation56
Anti-CD33	CD33, a T-cell epitope	Myeloid leukemia cells	^Citation50
Anti-ErbB2	ErbB2 receptor	Cancer cells overexpressed the ErbB2 receptor	^Citation57,Citation58
Anti-CEA	CEA	Cancer cells that overexpress the CEA such as pancreatic cancer cells, small-cell lung cancer cells	^Citation59,Citation60
Antagonist G	–	Small-cell lung cancer	^Citation61,Citation62
Anti-HER2	HER2	Breast cancer cells	^Citation24
EGF	EGF receptor	Human glioma cells	^Citation63
Anti-GD2	Disialoganglioside (GD2)	Neuroblastoma	^Citation64
CC52	CC531	Colon cancer cells	^Citation65

Abbreviations: CD19, the cluster of differentiation 19 is a protein that in humans is encoded by the CD19 gene; CD20, cluster of differentiation 20; CD22, cluster of differentiation 22; CD33, cluster of differentiation 33; ErbB2/HER2, human epidermal growth factor receptor 2; CEA, carcinoembryonic antigen; EGF, epidermal growth factor; GD2, disialoganglioside; CC52, a murine IgG1 monoclonal antibody; CC531, a cell line was induced by treatment of WAG rats with 1,2 dimethylhydrazine.

Figure 3 (A–C) Strategies of adsorbing ligands onto the vector surface. (A) Ligand-PEG-DSPE were added as the components during the preparation of carriers; (B) Mal-PEG-liposomes were preformed, then the ligands were directly coupled to the preface; (C) the postinsertion method.

Abbreviations: Mal, β-(N-maleimido) propionyl; PEG-DSPE, poly(ethylene glycol)–distearoylphosphatidylethanolamine.

Figure 4 Schematic illustration shows the formulation of lipid polymer hybrid nanoparticles.¹⁰⁰

Abbreviation: PLGA, poly-d,l-lactide-co-glycolide.

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