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. 2021 Sep 14;26(18):5577. doi: 10.3390/molecules26185577

Table 3.

Selected CL drug delivery experiments investigating anti-infective agents [16,155].

Drug. Method Used Loading Conditions Results Ref.
ANTIBACTERIALS
Carbenicillin Soaking
Unmodified
Sauflon 85 lenses
500 or 100 mg/ml In tear film after 2 h
(122.5 μg/mL and 28.0 ± 9.4 μg/mL for 500 and 100 mg/mL loading, respectively)
Jain 1983
[156]
Gentamicin 40 mg/mL
gentamicin
In tear film after 6 h
(1.75 μg/mL)
Chloramphenicol 100 mg/mL
chloramphenicol
In tear film after 4 h
(4.66 ± 1.25 μg/mL)
Gentamicin Soaking
Unmodified
commercial
HEMA lenses
5 mg/mL solution overnight In tear film for up to three days of contact lens wear (1.6 μg/mL) Busin 1988
[157]
Gentamicin,
Kanamycin,
Ciprofloxacin,
Ofloxacin
Soaking
Unmodified
Etafilcon A lenses
3 mg/mL solution
for one hour
Compared to the standard prophylactic regimen (nine drops over two hours before surgery), statistically significantly higher concentrations in aqueous humour when using loaded lenses. Hehl 1999
[158]
Lomefloxacin Soaking
Unmodified
Etafilcon A lenses
3 mg/mL solution
for one-hour vibration
Concentration observed compared to hourly eye-drop instillation:
Cornea:
(213.96 ± 60.87 μg/mL
vs. 31.48 ± 13.12 μg/mL)
Aqueous humour:
(26.6 ± 4.81 μg/mL
vs. 4.69 ± 2.18 μg/mL).
Machetta 2014
[159]
Ciprofloxacin
Moxifloxacin
Soaking
Unmodified
commercial
hydrogel and
silicone hydrogel
lenses
3 mg /mL ciprofloxacin (pH 4.0) or 1 mg/mL moxifloxacin solution
for 24 h
For hydrogel lenses, release max.:
Ciprofloxacin (109 ± 5 μg/lens) Moxifloxacin (226 ± 2 μg/lens)
For silicone hydrogels:
Ciprofloxacin (63 ± 6 μg/lens)
Moxifloxacin (36 ± 1 μg/lens).
Karlgard 2003
[160]
Hui 2008
[161]
Bajgrowicz 2015
[162]
Moxifloxacin
Gatifloxacin
Soaking
Modified anionic
pHEMA-based
lenses
5 mg/mL moxifloxacin
or 3 mg/mL gatifloxacin commercial solutions
with autoclaving
In vitro:
peak drug release at 1 h:
Gatifloxacin (1187.4 μg/lens)
Moxifloxacin (1310.7 μg/lens)
In vivo:
drug concentration in the cornea, aqueous humour and crystalline lens were consistently higher than three instillations of antibiotic eye drops over 45 min.
Kakisu 2013
[74]
Ciprofloxacin Soaking
Molecularly imprinted acrylic acid pHEMA TRIS–based lenses
In vitro/in vivo: 3 mg/mL
pH 4.0 ciprofloxacin-HCl solution for 24 h
after autoclaving
In vitro:
release of ciprofloxacin for up to 14 days.
In vivo:
significant reduction in the number of bacteria with modified lenses compared to unmodified lenses or no treatment.
Hui 2012
[163]
Hui 2014
[96]
Polymyxin B Soaking
Molecularly
imprinted acrylic
acid pHEMA–based
materials
4 mg/mL polymyxin B solution for three days In vitro:
sustained release of polymyxin B for more than two weeks.
Malakooti 2015
[95]
Levofloxacin Up to 10 layers of
levofloxacin-laden
liposomes
(Prepared in
100 mg/mL solutions)
Liposome surface
ethacrylat on
hioxifilcon B face
In vitro: drug release into
3 mL of 150 mmol/L NaCl
solution monitored
byfluorescence
In vitro:
layers of liposomes:
two (8 ± 3 μg/mL)
five (24 ± 1 μg/mL)
ten (40 ± 10 μg/mL)
Release up to 120 h.
Danion 2007
[163]
Ciprofloxacin Drug-loaded PLGA film
between two
layers of pHEMA
1:1 ratio of ciprofloxacin
to PLGA, solvent casted,
between two layers
of pHEMA
In vitro:
more than four weeks of zero-order release kinetics (134 μg/day).
Ciolino 2009
[112]
ANTIVIRALS
Modified
heparan sulfate
binding peptide
G2-C
Soaking
Unmodified
commercial
Ocufilcon D
lenses
10 mg/mL
G2-C solution
for five
days at 37 °C
In vitro:
release observed over eight days.
In vivo:
treatment of mouse corneas, after three days significant reduction of viruses.
Jaishankar 2016
[164]
ANTIFUNGALS
Natamycin Soaking
Unmodified
commercial
hydrogel and
silicone hydrogel lenses
2.6 mg/mL solution
prepared using DMSO
for 24 h
199.4 ± 29.9 μg/lens Phan 2013
[165]
Natamycin
Fluconazole
Unmodified
commercial
hydrogel and
silicone hydrogel lenses
1 mg/mL solutions of
each drug
Limited yeast growth over 48 h. Phan 2016
[166]
Econazole PLGA film between two
layers of pHEMA
200 mg of econazole incorporated into 100 mg of PLGA and ethyl acetate, formed into three different surface area sizes Effective econazole fungicidal concentrations for upward of 21 days. Ciolino
2011
[113]
Fluconazole Soaking
Vitamin E (various amounts) deposited on commercial silicone hydrogel lenses
0.7 mg/mL fluconazole solution prepared using PBS Addition of 17% Vitamin E
Fluconazole release (60 mg in 10 h)
Addition of 66% of Vitamin E
Fluconazole release (60 mg in 227 h)
Peng 2010
[153]

DMSO: dimethyl sulfoxide, PBS: phosphate-buffered saline, pHEMA: poly-2-hydroxyl ethyl methacrylate, PLGA: poly(lactic-co-glycolic acid), TRIS: tris(trimethyl siloxy) silyl-propyl methacrylate.