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. 2020 Jan 13;13(2):366. doi: 10.3390/ma13020366

Table 2.

Overview of the proposed uptake mechanisms of different polymeric micelles.

Material 1,2 Uptake Mechanism(s) 1 Cell type 3 Drug 1 Comments Ref.
Mixed micelles:
TPGS2K, HS15, F127
Energy dependent
CME
CvME
Caco-2 Curcumin
DOX
Only analyzed uptake of drug [93]
OCC CME
CvME
Caco-2 Silybin
Rhodamine-123
Only analyzed uptake of drug [94,95]
OGC
SH-OGC
CME
CvME
Caco-2 Paclitaxel
Rhodamine-123
Only analyzed uptake of drug [96,97]
P(PEGMEMA)75u-b-PMMA80u Clathrin and caveolae independent
CME
CvME
WiDr DOX
NileRed
80% of the uptake was via a different, undefined uptake mechanism [106]
PEG2000-b-PLGA5000 Energy dependent
CME
Calu-3
NCI-H441
NileRed
Curcumin acetate
Only analyzed uptake of drug [98,99]
PEG3000/2000/5000-PLA40000
PEG2000/5000-PLGA40000
Energy dependent
Lipid raft mediated
Caco-2 Curcumin
Coumarin 6
Only analyzed uptake of drug [100]
PEG5000-b-PLA5000 Direct drug transfer to cell membrane
Energy dependent
Caveolae/lipid raft-mediated endocytosis
A2780 Paclitaxel
NileRed
FRET, DAF/NileRed
[5,107]
PEG-b-PLGA CvME MCF-7 DTX, 3-MA, CQ
Coumarin 6
Only analyzed uptake of drug [6]
PEO2000/5000/13000-b-PCL5000
PEO5000-b-PCL13000/24000
CME MCF-7 DiIC PEO5000-b-PCL13000 showed fastest uptake, only analyzed drug uptake [101]
PEO2000-b-PCL2600/2800
PEO5000-b-PCL4000
Direct drug transfer to cell membrane HCT-116 Pheo
Conjugated Fluorescein
[108]
PEO45u-b-PCL23u Energy dependent
CME
P19 Conjugated Rhodamine [3,109]
PEO44u-b-PCL20u Temperature, pH and energy dependent PC12 DiIC Only analyzed uptake of drug [110]
PEO5000-b-PCL2000
PEO5000-b-PDLLA5000
Direct drug transfer to cell membrane KB DiIC/DiOC
Conjugated Fluorescein
[49]
PEO5000-b-PCL4000 Direct drug transfer to cell membrane MCF-7 Pheo
DiIC/DiOC
Micelle uptake is slow (>4 hr), while release of drug is fast [111]
PEOz6000-b-PLA1100/2200/3900/8500/10000/13700 PEOz2600/3300/4500/5600/6700/8900-b-PLA4000 Energy dependent
Cholesterol dependent
Caveolae/lipid raft-mediated endocytosis
MCF-7 Paclitaxel
Conjugated DEC
PEOz/PLA ratio of 1.7-2.0 for optimal uptake [17]
Val-TPGS
Phe-TPGS
Energy dependent
CvME
CME
Macropinocytosis
Caco-2 Curcumin
Coumarin 6
Enhanced transport across intestinal epithelial barrier, Only analyzed uptake of drug [47]

1 Abbreviations: N-octyl-O, N-carboxymethyl chitosan (OCC), N-mercapto acetyl-N′-octyl-O, N″-glycol chitosan (OGC), poly(poly(ethylene glycol) methyl ether methacrylate)(P(PEGMEMA)), poly(methyl methacrylate) (PMMA), Poly(ethylene glycol)/poly(ethylene oxide) (PEG/PEO), poly(lactide-co-glycolide) (PLGA), poly(lactide) (PLA), poly(ε-caprolactone) (PCL), poly((D,L-lactide) (PDLLA), poly(2-ethyl-2-oxazoline) (PEOz), D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), Clathrin-mediated endocytosis (CME), Caveolae-mediated endocytosis (CvME), Doxorubicin (DOX), 5-dodecanoylaminofluorescein (DAF), Docetaxel (DTX), 3-methyladenine (3-MA), Chloroquine (CQ), 1,1′-Dioctadecyl-3,3,3′,3′-Tetramethylindocarbocyanine Perchlorate (DiIC), Pheophorbide-a (Pheo), 3,3′-Dihexyloxacarbocyanine Iodide (DiOC), 7-N,N-diethylamino-coumarin-3 (DEC). 2 When available, the average molecular weight of the polymer block is listed (Dalton). If the number of monomeric units was provided, it is denoted by a number followed by ‘u.’ If different sizes of the same polymer were used, they are listed separated by ‘/.’ 3 Information on the various cell lines: human colon cancer cell lines (Caco-2 and WiDr, HCT-116), human lung cancer cell lines (Calu-3 and NCI-H441), human ovarian cancer cell line (A2780), human breast cancer cell line (MCF-7), mouse pluripotent embryonic carcinoma cell line (P19), pheochromocytoma rat cell line (PC12), HeLa contaminant human tumor cell line (KB).