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. 2020 Oct 14;10(10):2022. doi: 10.3390/nano10102022

Table 3.

Main types of antibacterial Ds developed in the years 2000–2010.

Dendrimer Class Mechanism of Action Proposed Structure Characteristics Advantages Target Bacterial Species Toxins Range of Activity 2,3,4
Glyco Ds Interference with adhesion of toxins to eukaryotic cells (ECs) 1/2 G 1 PPI Ds
1 G 1 PAMAM Ds		 ↑ Interactions with carbohydrate-targets due to dendrimer multivalence Vibrio cholerae
toxin B
E. coli
enterotoxin		 ↑ 1000-times 2,3
↓ adherence 2,4
3 G 3,5-di-2-PAE(BA) 5 Vibrio cholerae
toxin B		 ↑ 380 × 103-times 2,3
Interference with adhesion of bacteria to ECs 8-valent galabiose
1 G 1 PAMAM Ds
3,5-di-2-PAE(BA) 5 		Streptococcus suis MIC *
0.3 nM
Interference with adhesion of bacteria to human erythrocytes 12-valent mannose
3G 1 PAMAM Ds		 Type I fimbriated
E. coli 		MIC *
19 μM
↑ 400-times 2,4
Interference with adhesion of bacteria to ECs 4-valent
α-C-fucosyl-Ds		 ↑ Interactions with carbohydrate−targets due to dendrimer multivalence
No cytotoxicity
↑ Stability		 P. aeruginosa IC50 § 0.14 μM
Biofilm
(P. aeruginosa) 		IC50 § 10 μM
Cationic Ds Electrostatic interactions
Bacterial membranes
disruption		 Quaternized PPI Ds ↑ Positive charge density due to dendrimer multivalence Recombinant
E. coli (TV 1048)		 EC50 # 0.14 μM
↑ 100-times 2,3
1/2 G 1 ammonium-carbosilane Ds Staphylococcus aureus MIC *
8 mg/L (2G)
1 mg/mL (1G)
E. coli MIC *
64 mg/L (2G)
4 mg/L (1G)
1-3 G 1 ammonium N,N-dimethyl-N′-allyl
N′-ethylethylene
diamine hydride-terminated carbosilane Ds		 ↑ Positive charge density due to dendrimer multivalence
Water-soluble		 E. coli MBC $
1.65 mg/L (3G)
1.70 mg/L (2G)
3.65 mg/L (1G)
S. aureus MBC $
0.82 mg/L (3G)
0.85 mg/L (2G)
1.82 mg/L (1G)
4G 1 nadifloxacin-loaded PAMAM Ds ↑ Positive charge density due to dendrimer multivalence
Antibiotics solubilization by encapsulation		 E. coli As nadifloxacin
4G 1 prulifloxacin-loaded PAMAM Ds ↑ 2-times prulifloxacin
PEG/not PEG
5G 1 PAMAM Ds
coatings		 ↑ Positive charge density due to dendrimer multivalence
↓ Cytotoxicity
Prevention of implant-associated infections		 P. aeruginosa
(ATCC 19660)		 EC50 # 1.5 μg/mL
P. aeruginosa
(clinical)		 EC50 # 0.9 μg/mL
6% PEG
3G 1 PAMAM Ds
coatings		 ↑ Positive charge density due to dendrimer multivalence
↓↓↓ Cytotoxicity		 P. aeruginosa MIC *
25 μg/mL
Hydroxyl-terminated
4G 1 PAMAM Ds		 ↑ Positive charge density due to dendrimer multivalence E. coli Inhibition of bacteria growth and ascending in uterus 6
Amoxicillin-loaded
cross-linked
4G 1 PEG-PAMAM Ds		 ↑ Positive charge density due to dendrimer multivalence
Injectable hydrogels
↑ 72 h residence time
No cytotoxicity
240 h sustained drug
release 7
Triclosan-loaded 4G 1 PPO 8/PAMAM/PAA 9
layer-by-layer device		 ↑ Positive charge density due to dendrimer multivalence
↑ Drug loading than surfactants
20 days sustained drug release 7 		S. aureus Inhibition of bacteria growth
PPO 8 triamine core
PAMAM Ds		 Positive charge density due to dendrimer multivalence
E. coli
S. aureus
K. pneumoniae
B. cereus
M. lutens
P. vulgaris
M. Smegmatis
L. monocytogenes
P. aeruginosa 		MIC * (μg/mL)
3.1–12.5
1.6–6.3
6.1–12.5
6.3–25.0
1.6–12.5
1.6–6.3
12.5
6.3–12.5
6.3–25.0
Anionic Ds Imitating detergent activity Amphiphilic Ds ↑ Negative charge density due to dendrimer multivalence
Significant selectivity		 Bacillus subtilis EC50 # 41 μM
PPO 8
Triamine/anionic
PAMAM Ds		 ↑ Negative charge density due to dendrimer multivalence
Significant selectivity
E. coli
S. aureus
K. pneumoniae
B. cereus
M. luteus
P. vulgaris
M. Smegmatis
L. monocytogenes
P. aeruginosa 		MIC * (μg/mL)
12.5–25.0
12.5
12.5–25.0
12.5–25.0
6.3–12.5
6.3–12.5
12.5–25.0
6.3–12.5
12.5–25.0
Peptide-based Ds Mimicking membrane-active antimicrobial peptides [2] 2, 4, 8-valent
polylysine-Ds with
Arg-Leu-Tyr-Arg or
Arg-Leu-Tyr-Arg-Lys-Val-Tyr-Gly sequences
on surface
[D2,4,8(R4), D2,4,8(R8)]		 ↑ Positive charge density due to dendrimer multivalence
Significant selectivity
↓ Hemolytic activity

E. coli
P. aeruginosa
P. vulgaris
K. oxytoca
S. aureus
M. luteus
E. faecalis 		MIC * (μM)
D8(R8)/D8(R4)
0.3/0.5–0.7
0.5/0.3–0.9
0.5/0.8–1.3
0.5/0.4–0.8
0.4/0.5–0.6
0.4/0.5–0.7
0.4/0.8–1.3
4-valent
Polylysine-D core with Gln-Lys-Lys-Ile-Arg-Val-Arg-Leu-Ser-Ala sequences
on surface		 ↑ Positive charge density due to dendrimer multivalence
Significant selectivity
↓ Hemolytic activity
↓ Cytotoxicity
Good stability in plasma
E. coli
K. pneumoniae
K. oxytoca
E. aerogenes
E. doacae
P. mirabilis
A. baumannii
Citrobacter
freundii
B. cepacia
S. aureus
P. aeruginosa 		MIC * (μg/mL) 10
8
4–16
64
8
4
64→128
16–32
16

64
128
4–8
4-valent
Lysine-D core with Trp-Arg
on the surface		 ↑ Positive charge density due to dendrimer multivalence
Significant selectivity
↓ Hemolytic activity
↓ Cytotoxicity
↓ Resistance development
Capable of synergistic action		 E. coli res. MIC50 * (μg/mL)
4.5
↓ 33.5% planktonic
↓ 93.5% biofilm
S. aureus res. MIC50 * (μg/mL)
16.0

D(s) = dendrimer(s); 1 G = generation; 2 compared to non-dendrimer materials or carbohydrate residues; 3 experiments in wells; 4 experiments on cell lines; 5 PAE(BA) = poly-aminoethoxy(benzoic acid); 6 in vivo experiments; 7 in vitro experiments; 8 polypropylene oxide; 9 polyacrylic acid; 10 MIC values have not been reported when >128 μg/mL; * MIC/MIC50 = minimum inhibitory concentration/minimum inhibitory concentration of 50% of bacteria tested; § IC50 = half maximal inhibitory concentration; # EC50 = Half maximal effective concentration; $ MBC = minimum bactericidal concentration; ↑ = increased, improved, higher; ↓ = reduced, decreased, smaller; ↓↓↓ = strongly reduced.