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. Author manuscript; available in PMC: 2010 Nov 22.
Published in final edited form as: Ther Deliv. 2010 Jul 1;1(1):169–193. doi: 10.4155/tde.10.8

Table 1.

Cytosolic targeting of drug therapeutics (includes endosomal/lysosomal escape, in some cases).

Class of targeting agent Targeting agent composition Drug delivered (trade name if available) Ref.
Liposomes Liposome composed of lipid bilayer neutral lipids, DPPC and cholesterol Amikacin (Arikace) [347]
Liposomal includes soybean oil and phospholipids Cyclosporin [348]
Doxorubicin STEALTH® liposome containing MPEG–DSPE, HSPC and cholesterol Doxorubicin (Doxil®) [349]
pH-sensitive liposomes Liposomes composed of CHEMS and DOPE Diptheria toxin A chain [38]
DOPE, N-succinyl–DOPE and PEG–ceramide Gentamycin [350]
Thermosensitive liposomes DPPC, HSPC and cholesterol liposomes surface modified with DSPE-PEG-2000:PNIPAM-AAM17 Doxorubicin [351]
Targeted thermal magnetic liposomes DPPC, cholesterol, DSPE–PEG(2000) and DSPE–PEG(2000)–folate Doxorubicin [352,353]
Polymeric micelles PEG–poly(aspartic acid) block copolymer Doxorubicin (Adriamycin®) [354]
pH-sensitive micelles PEG-block-poly(aspartate-hydrazide) or PEG–p(Asp-Hyd) was modified using either levulinic acid or 4-acetyl benzoic acid attached via hydrazone bonds Doxorubicin (Adriamycin) [355]
pH-sensitive micelles with cell surface targeting Amphiphilic block copolymers that self-assemble into spherical micelles, folate–PEG–poly(aspartate-hydrazone-adriamycin) with γ-carboxylic acid-activated folate Doxorubicin (Adriamycin) [356]
Thermosensitive micelles/polymers Micellar cyclotriphosphazenes Human growth hormone [43]
Biodegradable triblock copolymer of PLGA–PEG–PLGA (ReGel®) Paclitaxel [357]
Cell-penetrating peptides Doxorubicin bound to HPMA-based polymer with the cell-penetrating peptide Tat Doxorubicin [358]
Cationic polymers and cationic lipids Polyethyleneimine Genes (DNA) [61,359]
Virus mimetic Hydrophobic polymer core (poly(L-histidine-co-phenylalanine)(poly(His32-co-Phe6) and two layers of hydrophilic shell (one PEG end linked to core polymer; other end to BSA) Doxorubicin [346]
NES NES (LQLPPLERLTL) encoded in a plasmid Genes (DNA) [6,7,60]
NES (ALPPLERLTL) conjugated to DNA Antisense oligonucleotide [360]

BSA: Bovine serum albumin; CHEMS: Cholesterylhemisuccinate; DOPE: Dioleoylphosphatidylethanolamine; DPPC: Dipalmitoylphosphatidylcholine; DSPE: Distearoylphosphatidylethanolamine; HPMA: N-(2-hydroxypropyl)methacrylamide; HSPC: Fully hydrogenated soy phosphatidylcholine; MPEG: Methoxypolyethylene glycol; NES: Nuclear export signal; PEG: Polyethylene glycol; PLGA: Poly(lactide-co-glycolide).