Current Neuropharmacology,
Journal Year:
2022,
Volume and Issue:
21(3), P. 517 - 535
Published: July 7, 2022
Brain
disorders
are
a
prevalent
and
rapidly
growing
problem
in
the
medical
field
as
they
adversely
affect
quality
of
life
human.
With
an
increase
expectancy,
it
has
been
reported
that
diseases
like
Alzheimer's,
Parkinson's,
stroke
brain
tumors,
along
with
neuropsychological
disorders,
also
being
at
alarmingly
high
rate.
Despite
various
therapeutic
methods
for
treating
drug
delivery
to
challenging
because
very
complex
Blood
Barrier,
which
precludes
most
drugs
from
entering
effective
concentrations.
Nano-carrier-based
systems
have
widely
by
researchers
overcome
this
barrier
layer.
These
due
their
small
size,
offer
numerous
advantages;
however,
short
residence
time
body
owing
opsonization
hinders
success
vivo.
This
review
article
focuses
on
aspects
modifying
surfaces
these
nano-carriers
polymers,
surfactants,
protein,
antibodies,
cell-penetrating
peptides,
integrin
binding
peptides
glycoproteins
such
transferrin
&
lactoferrin
leading
enhanced
time,
desirable
characteristics
ability
cross
blood-brain
(BBB),
increased
bioavailability
regions
targeted
delivery.
PLoS ONE,
Journal Year:
2023,
Volume and Issue:
18(2), P. e0281004 - e0281004
Published: Feb. 28, 2023
The
present
study
aimed
to
prepare
solid
lipid-based
nanoparticles
(SLNs)
using
Precirol
®
ATO
5
as
lipid
and
Poloxamer
188
Tween
80
surfactant
co-surfactant
respectively,
SLNs-derived
gel
for
sustained
delivery,
enhanced
in-vitro
cytotoxicity,
cellular
uptake
of
5-FU
permeation
across
the
skin.
5-FU-loaded
SLNs
were
prepared
by
hot
melt
encapsulation
method
converted
into
SLN-derived
a
gelling
agent
(Carbopol
940).
had
particle
size
in
range
76.82±1.48
327±4.46
nm,
zeta
potential
between
-11.3±2.11
-28.4±2.40
mV,
entrapment
efficiency
(%)
63.46±1.13
76.08±2.42.
FTIR
analysis
depicted
that
there
was
no
chemical
interaction
formulation
components.
Differential
scanning
calorimetric
showed
thermal
stability
powdered
X-ray
diffraction
revealed
successful
incorporation
nanoparticles.
release
biphasic
behavior
with
initial
burst
followed
over
48
hr.
greater
cytotoxic
effect
on
skin
melanoma
(B16F10
cells)
squamous
cell
carcinoma
(A-431
compared
free
drug
solution
after
Flow
cytometry
fluorescence
microscopy
displayed
quantitative
qualitative
SLNs.
acceptable
safety
biocompatible
profile
an
acute
toxicity
Wistar
rats.
Moreover,
ex-vivo
studies
2.13±0.076
folds
flux
SLN
derived
plain
gel,
retention
target
2.54±0.03
gel.
Pharmaceutics,
Journal Year:
2023,
Volume and Issue:
15(2), P. 443 - 443
Published: Jan. 29, 2023
Contemporary
trends
in
combinatorial
chemistry
and
the
design
of
pharmaceuticals
targeting
brain
disorders
have
favored
development
drug
candidates
with
increased
lipophilicity
poorer
water
solubility,
expected
improvement
delivery
across
blood-brain
barrier
(BBB).
The
growing
availability
innovative
excipients/ligands
allowing
improved
controlled
release
makes
lipid
nanocarriers
a
reasonable
choice
to
overcome
factors
impeding
through
BBB.
However,
wide
variety
methods,
study
designs
experimental
conditions
utilized
literature
hinder
their
systematic
comparison,
thus
slows
advances
brain-targeting
by
lipid-based
nanoparticles.
This
review
provides
an
overview
methods
most
commonly
during
preclinical
testing
liposomes,
nanoemulsions,
solid
nanoparticles
nanostructured
carriers
intended
for
treatment
various
CNS
via
parenteral
route.
In
order
fully
elucidate
structure,
stability,
safety
profiles,
biodistribution,
metabolism,
pharmacokinetics
immunological
effects
such
nanoparticles,
transdisciplinary
approach
characterization
is
mandatory,
covering
comprehensive
set
physical,
chemical,
vitro
vivo
biological
testing.
Biomacromolecules,
Journal Year:
2024,
Volume and Issue:
25(4), P. 2607 - 2620
Published: March 26, 2024
Riluzole
is
commonly
used
as
a
neuroprotective
agent
for
treating
traumatic
spinal
cord
injury
(SCI),
which
works
by
blocking
the
influx
of
sodium
and
calcium
ions
reducing
glutamate
activity.
However,
its
clinical
application
limited
because
poor
solubility,
short
half-life,
potential
organ
toxicity,
insufficient
bioabilities
toward
upregulated
inflammation
oxidative
stress
levels.
To
address
this
issue,
epigallocatechin
gallate
(EGCG),
natural
polyphenol,
was
employed
to
fabricate
nanoparticles
(NPs)
with
riluzole
enhance
effects.
The
resulting
NPs
demonstrated
good
biocompatibility,
excellent
antioxidative
properties,
promising
regulation
effects
from
M1
M2
macrophages.
Furthermore,
an
in
vivo
SCI
model
successfully
established,
could
be
obviously
aggregated
at
site.
More
interestingly,
properties
through
regulating
levels
stress,
inflammation,
ion
channels
fully
RNA
sequencing
sophisticated
biochemistry
evaluations.
Together,
work
provided
new
opportunities
design
fabrication
robust
multifunctional
inflammation-related
diseases
via
biological
integration
polyphenols
small-molecule
drugs.
Expert Opinion on Drug Delivery,
Journal Year:
2022,
Volume and Issue:
19(12), P. 1618 - 1635
Published: Oct. 26, 2022
Brain
diseases
including
brain
tumor,
Alzheimer's
disease,
Parkinson's
etc.
are
difficult
to
treat.
The
blood-brain
barrier
(BBB)
is
a
major
obstacle
for
drug
delivery
into
the
brain.
Although
nano-package
and
receptor-mediated
of
nanomedicine
markedly
increases
BBB
penetration,
it
yet
did
not
extensively
improve
clinical
cure
rate.
Recently,
extracellular
space
(ECS)
interstitial
fluid
(ISF)
drainage
in
ECS
have
been
found
determine
whether
dissolved
ISF
can
reach
its
target
cells.
Notably,
an
increase
tortuosity
associated
with
slower
induced
by
accumulated
harmful
substances,
such
as:
amyloid-beta
(Aβ),
α-synuclein,
metabolic
wastes,
causes
failure.The
methods
penetration
efficacy
nanomedicines
across
assessed.Invasive
delivering
via
noninvasive
near-infrared
photo-sensitive
may
provide
promising
benefit
patients
disease.
Pharmaceutics,
Journal Year:
2023,
Volume and Issue:
15(8), P. 2078 - 2078
Published: Aug. 3, 2023
Chronic
skin
exposure
to
external
hostile
agents
(e.g.,
UV
radiation,
microorganisms,
and
oxidizing
chemicals)
may
increase
oxidative
stress,
causing
damage
aging.
Because
of
their
well-known
skincare
protective
benefits,
quercetin
(Q)
omega-3
fatty
acids
(ω3)
have
attracted
the
attention
dermocosmetic
pharmaceutical
sectors.
However,
both
bioactives
inherent
properties
that
limit
efficient
delivery.
Therefore,
nanostructured
lipid
carriers
(NLCs)
enriched
PFC®
hydrogels
(HGs)
been
developed
as
a
dual-approach
vehicle
for
Q
and/or
ω3
topical
administration
improve
bioactives’
stability
permeation.
Two
NLC
formulations
were
prepared
with
same
composition
but
differing
in
surfactant
(NLC1—soy
lecithin
poloxamer
407;
NLC2—Tween®
80
dioctyl
sodium
sulfosuccinate
(DOSS)),
which
an
impact
on
physicochemical
therapeutic
performance.
Despite
NLCs
presenting
high
loading
capacity,
NLC2′s
make
them
more
suitable
ensure
longer
colloidal
stability.
Additionally,
NLC2
demonstrated
sustained
release,
indicating
higher
bioactive
storage
while
improving
permeability.
The
occlusive
effect
NLCs-enriched
HGs
also
has
positive
Q-loaded
NLC2,
or
without
ω3,
-enriched
efficacy
antioxidant
photoprotective
well
effective
reduction
S.
aureus
growth,
they
constitute
promising
approach
prevent
aging
other
damaging
cutaneous
processes.
Journal of Molecular Liquids,
Journal Year:
2023,
Volume and Issue:
388, P. 122749 - 122749
Published: Aug. 4, 2023
Amyotrophic
lateral
sclerosis
(ALS)
is
a
fatal
neurodegenerative
disease,
with
median
survival
of
only
2
to
4
years.
Riluzole,
drug
commonly
used
in
the
management
ALS,
has
low
aqueous
solubility
and
limited
bioavailability.
ALS
treatment
also
hindered
by
presence
blood-brain
barrier
(BBB)
that
preserves
delicate
homeostasis
cerebral
milieu,
isolating
it
making
brain
delivery
exceptionally
hard.
To
overcome
these
issues,
use
lipid
nanocarriers,
such
as
solid
nanoparticles
(SLN)
nanostructured
carriers
(NLC),
promising
strategy.
In
this
study,
SLN
NLC
were
prepared
optimized
facilitate
riluzole
uptake
into
for
therapy.
The
characterized
through
different
techniques,
respect
their
physicochemical
properties
(size,
zeta
potential
(ZP),
polydispersity
index
(PDI)),
well
encapsulation
efficiency,
morphology,
stability,
vitro
release,
crystallinity,
biocompatibility.
Riluzole-loaded
nanocarriers
exhibited
characteristics
suitable
delivery,
including
mean
diameters
between
147.2
203.1
nm,
PDI
(<
0.3),
negative
ZP
−22.5
−27.5
mV.
Additionally,
they
physically
stable
over
3
months
under
storage
conditions
(5)
℃
25
℃),
promoting
slow
sustained
release
drug,
which
was
shown
be
inside
core
matrix.
Cytotoxicity
assays
demonstrated
both
did
not
significantly
affect
viability
an
hCMEC/D3
cell
monolayer
at
concentration
up
10
μM.
results
suggest
developed
could
viable
platform
target
central
nervous
system
(CNS).
Nevertheless,
further
vivo
studies
are
needed
validate
therapeutic
efficacy
safety.
Pharmaceutics,
Journal Year:
2025,
Volume and Issue:
17(3), P. 331 - 331
Published: March 4, 2025
Background/Objectives:
Natural
substances
have
been
a
widely
studied
source
of
both
pharmaceutical
excipients
and
drugs.
Berberine
(BRB)
is
benzylisoquinoline
alkaloid
isolated
from
different
plant
sources.
It
possesses
various
pharmacological
properties
including
antibacterial,
antitumor,
antidiabetic,
neuroprotective,
hepatoprotective,
anti-inflammatory,
antioxidant,
etc.
However,
the
limited
aqueous
solubility
hinders
its
application.
Nanosized
drug
delivery
systems
are
an
innovative
approach
for
addressing
challenges
regarding
via
routes
administration.
Their
utilization
could
improve
active
constituents.
Methods:
A
melt-emulsification
ultrasonication
technique
was
applied
preparation
nanostructured
lipid
carriers
(NLCs).
They
were
thoroughly
physicochemically
characterized
by
means
Dynamic
Light
Scattering,
TEM,
FTIR,
DSC,
TGA,
In
Vitro
release.
The
efficacy
safety
evaluated
on
cholangiocarcinoma,
colorectal
adenocarcinoma,
hepatocellular
carcinoma,
lymphoma,
fibroblast,
cardioblast
cells,
as
well
rat
liver
microsomes
cytotoxicity
assays
comet
assay.
Results:
obtained
nanoparticles
had
spherical
shape
size
around
158.2
±
1.8
nm
with
negative
zeta
potential.
revealed
successful
loading
improved
dissolution
berberine
in
physiological
conditions.
studies
showed
that
BRB
NLCs
resulted
or
retained
to
tumor
cell
lines
reduced
normal
microsomes.
NLC
itself
increased
microsomal
malondialdehyde
(MDA)
formation.
Conclusions:
presented.
nanocarriers
show
favorable
physicochemical
biopharmaceutical
properties.
cellular
experiments
anticancer
safety.
These
findings
highlight
potential
applicability
gastrointestinal
neoplasms
build
foundation
future
practical
translation.