Table
1 Particle size, PDI, and zeta potential of ?-T-FU-PLGA/5-FU-PLGA NPs
(n=3; mean ± standard deviation)

Formulation type

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Nanoformulation

Particle Size (nm)

Polydispersity index (PDI)

Zeta potential (mV)

Non-Targeted
Surface Nanoparticles

5-FU-PLGA
nanoparticles

148.50±6.50

0.16±0.02

-17.50±0.50

Surface
Targeted Nanoparticles

?-Tocopherol-FU-PLGA
nanoparticles

161.50±3.50

0.3±0.05

-23.50±1.80

 

Abbreviations:
PDI, polydispersity index; ?-T-FU-PLGA-NPs, targeted ?-Tocopherol-5-Fluorouracil-poly(D,L-lactic-co-glycolic)
nanoparticles; 5-FU-PLGA-NPs, non-targeted 5-Fluorouracil-poly(D,L-lactic-co-glycolic)
nanoparticles

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Table
2 In vitro drug release of ?-T-FU-PLGA-NPs and
5-FU-PLGA-NPs in different time interval up to 160 hours

Time (hours)

 
In vitro cumulative percentage of  drug
release data at pH 7.4 & pH 4.5

5-FU-PLGA nanoparticles (%
release)

?-tocopherol-FU-PLGA (% release)

pH 7.4

pH 4.5

pH 7.4

pH 4.5

0

0

0

0

0

5

16.08±0.55

13.45±0.36

12.08±0.55

11.69±0.73

10

19.21±0.61

17.89±0.74

16.97±0.25

14.27±0.61

20

23.56±0.35

21.41±0.16

19.25±0.45

15.73±0.41

40

36.98±0.85

25.68±0.87

27.85±0.49

21.12±0.39

60

59.45±0.65

35.65±0.45

49.78±0.26

35.16±0.74

80

67.78±0.75

46.46±0.73

61.26±0.65

41.12±0.78

120

82.45±0.54

67.76±0.93

78.09±0.22

61.55±0.45

140

86.25±0.35

68.36±0.98

82.78±0.50

63.95±0.19

160

86.55±0.25

69.55±0.25

82.93±0.25

64.45±0.22

 

Abbreviation:
?-T-FU-PLGA-NPs, targeted ?-Tocopherol-5-Fluorouracil-poly(D,L-lactic-co-glycolic)
nanoparticles; 5-FU-PLGA-NPs non-targeted 5-Fluorouracil-poly(D,L-lactic-co-glycolic)
nanoparticles.

 

 

 

 

 

 

 

 

Table
3 Inhibitory
effects of ?-T-FU-PLGA-NPs and 5-FU-PLGA-NPs on the proliferation of the SCC15, 5-FU resistance cell line (n=3; mean ±
standard deviation)

 

Concentration
of Nanoparticles
(µg/ml)

5-FU-PLGA
NPs-SCC-15

?-
Tocopherol -FU-PLGA NPs-SCC-15

Value

Inhibitory
rate (%)

IC50
(µg/ml)

Value

Inhibitory
rate (%)

IC50
(µg/ml)

0

0.84±0.03

 

 
 
 
23.25

0.79±0.04

 

 
 
 
13.19

0.25

0.71±0.05

17.89

0.53±0.05

39.45

1.50

0.59±0.06

29.59

0.53±0.05

49.52

3.0

0.54±0.03

38.12

0.51±0.03

59.23

4.5

0.46±0.05

53.96

0.45±0.02

64.23

6.0

0.36±0.06

59.65

0.41±0.05

69.59

7.5

0.31±0.03

65.69

0.39±0.05

76.29

 

Abbreviations:
5-FU,
5-Fluorouracil; ?-T-FU-PLGA-NPs, targeted ?-Tocopherol-5-Fluorouracil-poly(D,L-lactic-co-glycolic
acid) nanoparticles; 5-FU-PLGA-NPs, non-targeted 5-Fluorouracil-poly(D,L-lactic-co-glycolic)
nanoparticles; SCC15, squamous cell carcinoma-15 cells.

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