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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5264_Библиотеки_им_академика_М_И_Перельмана.pdf
54
Plant-based Foods and their Implications in Brain Health
Formulations
Spices
Raw/
Extract
Method of
extraction
Extracted
compositions Yield
AD
pathways
evaluated
Native
extract
Macro/ micro-
encapsulate Nano- vehicle
- - - - Curcumin
micelles
- - - - Poly (d,l- lactide-
co- glycolide)-
b- poly (ethylene
glycol)- b-
poly(d,l-
lactide- co-
glycolide)
(PLGA- PEG-
PLGA)
micelles
TABLE 4.2 (Continued)
Spice compounds, their extracts and formulations: Mode of action in targeted pathways
of AD pathogenesis
55
Impact of Indian Herbs and Spices on Alzheimer’s Disease
(continued)
Nasal
formulations
Characteristics of
the extract or the
formulations and
their pharmaceutical/
pharmacokinetic profiles
Preclinical/
Clinical study Remarks References
- - - - EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
For the short- time
bioavailability
study:
Doses:
1.75 µL curcumin
micelles solution/
g body weight
(equivalent to 120
µg curcumin/ g body
weight)
Duration:
45 min
Route of
administration:
Oral
For the long- term
feeding study:
Doses:
3.5 µL curcumin micelles
solution/ g body weight
(equivalent to 120
µg curcumin/ g body
weight)
Duration:
21 days
Route of
administration:
Oral
For the short- time
bioavailability study:
Female NMRI mice
(aged between 8- 24
months)
For the long- term
feeding study: Female
young and aged NMRI
mice (3 Months;
18 months)
Target(s):
In vivo bioavailability
study in brain and
blood plasma
Major nding(s)
reported:
Curcuminoid levels in
plasma and brain
increased around 10- to 45-
fold, respectively, vis- à-
vis the native curcumin
32
- - - - EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
In silico
Doses:
N.R
Duration:
N.R
Route of
administration:
Intravenous
Subject:
Mice model
Target(s):
pharmacokinetics and
tissue distribution
Major nding(s)
reported:
Plasma levels of curcumin
micelles were
increased by
1.31- fold compared with
curcumin solution;
brain distribution of
curcumin micelles
increased by 6.28- fold;
more effective for AD
treatment
33
56
Plant-based Foods and their Implications in Brain Health
Formulations
Spices
Raw/
Extract
Method of
extraction
Extracted
compositions Yield
AD
pathways
evaluated
Native
extract
Macro/ micro-
encapsulate Nano- vehicle
C; D - - - - Nanoliposome:
C - - - - Nanocurcumin
C - - - - - - Thermosensitive
TABLE 4.2 (Continued)
Spice compounds, their extracts and formulations: Mode of action in targeted pathways
of AD pathogenesis
57
Impact of Indian Herbs and Spices on Alzheimer’s Disease
Nasal
formulations
Characteristics of
the extract or the
formulations and
their pharmaceutical/
pharmacokinetic profiles
Preclinical/
Clinical study Remarks References
nanostructured
lipid carrier
coated with
lactoferrin
- - EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
Doses:
2 mg/ kg/ day
Duration:
3 weeks
Route of
administration:
Intravenous
Subject:
Sprague Dawley rats
(180- 220 g) and ICR
mice (18- 22 g)
Target(s):
Inhibitory effect on
oxidative stress
reduction; brain
uptake
Major nding(s)
reported:
oligomerization; acted
as showed antioxidant
potency; may provide a
platform for brain
targeting
34
(A novel
polymeric
nanoparticle
formulation
of curcumin,
polymerized by
N- isopropyla-
crylamide,
vinylpyrrolidone,
and acrylic acid)
- - EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
In vivo doses:
23 mg/ kg body weight
Duration:
3 months
Route of
administration:
Oral
Subject:
In - vitro BBB Model and
Tg2576 Mice
Target(s):
Inhibitory effect on
; in
vitro and in vivo
bioavailability
study in brain and
blood plasma; BBB
permeability
Major nding(s)
reported:
memory function in
vivo
35
curcumin
nasal gel;
FMeC1 nasal
solution
EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
Doses:
Equivalent to a 5 mg/ kg
injection
Duration:
One hour respiratory
exposure
Route of
administration:
Intranasal
Subject:
C57BL/ 6 and 5XFAD
mice (8– 12 months
old)
Target(s):
Inhibitory effect on
in
vivo bioavailability
study in brain and
blood plasma; BBB
permeability
Major nding(s)
reported:
A promising alternative
intravenous
administration
method of existing
AD drugs
36
(continued)
58
Plant-based Foods and their Implications in Brain Health
Formulations
Spices
Raw/
Extract
Method of
extraction
Extracted
compositions Yield
AD
pathways
evaluated
Native
extract
Macro/ micro-
encapsulate
Black
pepper
Soxhlet and
extractions
(DBSA)
Piperine 4 ±0.01% w/ w - - - -
Soxhlet- apparatus 10.4 % w/ w A,
C, D, E
Vacuum- dried,
powdered
ethanolic
extract,
suspend in
propylene
glycol
- -
UAE 5.8 mg/ g - - - - - -
MAE 92.5 ±0.05%
w/ w
- - - - - -
SFE (SC- CO
2
) 91.31% w/ w - - - - - -
Naviglio Extractor 317.7 mg/ g - - - - - -
A; D; F - - PIP- loaded
micro
emulsion
A; C; D;
E; F
- - - -
TABLE 4.2 (Continued)
Spice compounds, their extracts and formulations: Mode of action in targeted pathways
of AD pathogenesis
59
Impact of Indian Herbs and Spices on Alzheimer’s Disease
Nasal
formulations
Characteristics of
the extract or the
formulations and
their pharmaceutical/
pharmacokinetic profiles
Preclinical/
Clinical study Remarks References
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
Doses:
20mg/ kg/ day,
200mg/ kg / day
Duration:
2 months
Route of
administration:
Oral
Subject:
AlCl
3
- induced AD rat
model
Target(s):
Inhibitory effect on
oligomerization;
oxidative stress; tau
protein phosphorylation
Major nding(s)
reported:
Black pepper extract
showed success in
major AD preventive
pathways; decreased
escape latency time and
increased memory in
AD- induced rat models
38
- - - - EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
R
Doses:
2.5 mg equivalent/
kg (0.2 ml/ 0.15ml)/ day
Duration:
3 days
Route of
administration:
Oral
Subject:
Adult Wistar rats
Target(s):
Inhibitory effect on AChE
activity; oxidative
stress; SOD value;
brain target
Major nding(s)
reported:
Micro emulsion increased
piperine for AD and
enhanced its delivery
to the target region of
the brain
46
80- coated
piperine
solid- lipid
nanoparticles
(P- 80- PIP- SLN)
- - EPR spectrum for
validation of antioxidant
potency: N.R.
SE value: N.R.
LD
50
: N.R.
Release kinetics
In silico study
Doses:
20mg/ kg/ day
Duration:
7 days
Route of
administration:
Intraperitoneal
Subject:
Albino Wister rat
Target(s):
Inhibitory effect on
oligomerization;
oxidative stress; tau
protein phosphorylation;
SOD value; brain target
Major nding(s)
reported:
Reduced cholinergic
degradation; reduced
oxidative stress; reduced
tangles; reduced SOD
values; the formulated
SLNs shown to be
superior than donepezil
47
(continued)
60
Plant-based Foods and their Implications in Brain Health
Formulations
Spices
Raw/
Extract
Method of
extraction
Extracted
compositions Yield
AD
pathways
evaluated
Native
extract
Macro/ micro-
encapsulate Nano- vehicle
A; D; F - - - - Piperine-
A; D; F - - - - Piperine-
- - - - - - Piperine-
- - - - - - - - Piperine-
TABLE 4.2 (Continued)
Spice compounds, their extracts and formulations: Mode of action in targeted pathways
of AD pathogenesis
61
Impact of Indian Herbs and Spices on Alzheimer’s Disease
Nasal
formulations
Characteristics of
the extract or the
formulations and
their pharmaceutical/
pharmacokinetic profiles
Preclinical/
Clinical study Remarks References
loaded
chitosan
nanoparticles
(CS- NPs)
Intranasal
formulation
using
Piperine- loaded
chitosan
nanoparticles
EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
Doses:
0.1 mL equivalent to
0.045 mg/ kg/ day;
0.1 mL equivalent to
0.250 mg/ kg/ day, pH
5.5 (drop- wise)
Duration:
21 days
Route of
administration:
intranasal
Subject:
Adult male Wistar rat
model
Target(s):
Inhibitory effect on AChE
activity; oxidative
stress; SOD value
Major nding(s)
reported: CS- NPs
considered as effective,
safe, and non- invasive
piperine delivery agent;
drug donepezil with
additional advantages
of dual mechanism
(AChE inhibition and
antioxidant effect)
48
loaded
tween
integrated
monoolein
cubosomes
- - EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
:
Release kinetics
In silico
Doses:
2.5 mg equivalent/ kg
Duration:
21 days
Route of
administration:
Oral
Subject:
Adult male Wistar rat
model
Target(s):
Inhibitory effect on AChE
activity; oxidative
stress; SOD value
Major nding(s)
reported:
Formulation considered
as safe and possesses
promising in vitro and
in vivo characteristics
for effective chronic
treatment of AD
49
encapsulated
PEG- ylated
Liposomes (PL)
- - EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
Doses:
5 mg/ kg body weight/
day
Duration:
14 days
Route of
administration:
Oral
Subject:
Male Wistar rat model
Target(s):
Effective delivery to brain;
cognition
Major nding(s)
reported:
Improved cognition and
showed antidepressant
effects; piperine intake
was slower in brain
50
encapsulated
PL nasal
formulation
EPR spectrum for
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
Doses:
7.2 µg/ day
Duration:
14 days
Route of
administration:
Intranasal
Subject:
Male Wistar rat
Target(s):
Effective delivery to brain;
cognition
Major nding(s)
reported: Improved
cognition and showed
antidepressant effects;
faster delivery to
brain in greater extent
compared to oral
administration of PL
50
(continued)
62
Plant-based Foods and their Implications in Brain Health
Formulations
Spices
Raw/
Extract
Method of
extraction
Extracted
compositions Yield
AD
pathways
evaluated
Native
extract
Macro/ micro-
encapsulate Nano- vehicle
Small
cardamom
Extract Hydro distillation
by Clevenger-
type apparatus
1, 8-
Cineole;
limonene;
acetate;
73.27% w/ w;
4.23% w/ w;
4.2% w/ w;
3.33% w/ w;
2.9% w/ w
- - - - - - - - - - - - - - - - 51
UAE followed by
hydro distillation
1,8- cineole;
acetate
26.59% to
39.34% w/
w;
22.94% to
40.56%
w/ w
- - - - - - - - - - - - - - - - 52
SFE (SC- CO
2
) 1,8- cineole 31.96 ± 0.16
mg/ g
- - - - - - - - - - - - - - - - 53
A; C; D; E - - - - - - PEG- ylated
Oil - - 1,8 cineole,
acetate,
limonene,
linalyl
acetate,
linalool
- - A; C; D Cardamom oil - - - - - - EPR spectrum for
Saffron Extract Solvent extraction
(water and
methanol 1:1 v/ v)
Crocin - - C Extracted powder
suspended in
water
- - - - - - EPR spectrum for
TABLE 4.2 (Continued)
Spice compounds, their extracts and formulations: Mode of action in targeted pathways
of AD pathogenesis
63
Impact of Indian Herbs and Spices on Alzheimer’s Disease
Nasal
formulations
Characteristics of
the extract or the
formulations and
their pharmaceutical/
pharmacokinetic profiles
Preclinical/
Clinical study Remarks References
Nanoliposomal
formulation
EPR spectrum for
validation of antioxidant
potency: Done
SE value: Done
LD
50
: Done
Release kinetics
In silico study
- - Target(s):
Inhibitory effect on
oligomerization;
oxidative stress; tau
protein phosphorylation
Major nding(s)
reported:
Inhibited AChE
oligomerization and tau
protein phosphorylation;
reduced oxidative stress
(in vitro)
4, 54, 55, 56
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
Release kinetics
In silico
Doses:
100 and
200 mg/ kg / day
Duration:
42 days
Route of
administration:
Oral
Subject:
Male albino Wistar rat
Target(s):
Inhibitory effect on
oligomerization;
oxidative stress
Major nding(s)
reported:
Inhibited AChE activity
and reduced oxidative
stress; may act as a
neuroprotector to treat
AD
57
validation of antioxidant
potency: N.R
SE value: N.R
LD
50
: N.R
In silico
Concentration:
15 µg/ ml, 15.4 µM
(in vitro assays)
Target(s):
In vitro assays (amyloid
40 (1
mg/ mL)
Major nding(s)
reported:
Crocin inhibited amyloid
in vitro
58
(continued)