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Current nanocarriers in therapeutic improvement of Andrographolide

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Life ScienceS
|
Biomedical applications
62
SEPTEMBER 2022
Volume 64 Number 3
Introduction
In the discovery of novel drugs, natural compounds have
impressive properties and characteristics such as better therapeutic
effects as well as low toxicity compared to synthesized agents.
Andrographolide (AG) is the representative bioactive chemical
of the plant
Andrographis paniculata
that is currently being
explored in the pharmaceutical industry. This compound proposes
significant beneficial advantages such as antibacterial [1], anti-
inflammation, cancer prevention, and neuroprotective properties
(see Fig. 1) [2]. Antimicrobial activity is the most prominent
effect, which has been applied to the treatment of infectious
diseases since ancient times, for example, for gastrointestinal
inflammation-related diseases and respiratory infection [3].
Also, AG can be considered as an antiviral agent [4], especially
express inhibition of SARS-CoV-2 in Calu-3, which are human
lung epithelial cells [5]. Promising treatments of AG could be
confirmed by numerous current clinical trials on lung infection,
arthritis, rheumatoid, gastrointestinal cancer, migraine, cognitive
impairment, COVID-19 virus, and so on.
AG is a white crystalline powder with an extremely bitter
flavour. At neutral to basic pH, Andrographolide is unstable and
hydrolyses to an inert product. The high hydrophobicity (log
P=2.632±0.135), poor water solubility (3.29±0.73 mg/ml), and
fast transportation by P-glycoprotein out of the cells are all factors
that contribute to the poor bioavailability of AG. Therefore, it is
important to study methodologies to improve therapeutic treatment
with AG. Many pharmaceutical techniques such as solid dispersion
[6], inclusion complex [7], and nanotechnology [8] have been
invest
igated to improve the solubility and permeability of AG.
Fig. 1.
Therapeutic effects of Andrographolide.
Nan
otechnology is considered the most promising strategy
for drug delivery systems, especially for natural compounds
and specifically for AG [9]. The incorporation of natural
herbs in nanoplatforms is necessary for the enhancement of
biocompatibility, the prolongation of drug circulation in living
bodies, and the ease of permeability through the cell membrane
for effective treatments. In particular, AG nano formulations
show better results in bioavailability, targeting effect, and safety
[10]. Hence, modern drug delivery systems loading AG through
various uptake routes, which could improve solubility, stability,
absorption, and overcome resistance mechanisms in tumour cells
are summarized.
Current nanocarriers in therapeutic
improvement of Andrographolide
Van Hong Nguyen
*
, An Hong Nguyen Pham
Pharmaceutical Engineering Lab, School of Biomedical Engineering, International University,
Vietnam National University, Ho Chi Minh city
Received 27 April 2022 ; accepted 22 July 2022
*
Corresponding author: Email: [email protected]
Abstract:
Currently, herbs have been investigated for novel bioactivities and improvement of traditional therapeutic effectiveness.
Among them,
Andrographis paniculata
, with the active component Andrographolide, is well recognized as an anti-
inflammatory, anti-bacterial, anti-cancer, anti-hypertensive, anti-hyperglycaemic, hepatoprotective, and anti-
hyperlipidaemic compound. However, Andrographolide has poor physicochemical properties that limit its medical
application. In this review article, nano drug delivery systems including nanovesicles, inorganic nanoparticles, lipid-
based nanoparticles, polymeric nanoparticles, nanocrystals, nanoemulsions, and microemulsions, which can deliver
Andrographolide through different routes such as oral, injection, or dermal, and their influences in increasing treatment
benefits are presented.
Keywords:
A. paniculata
, Andrographolide, herbal, nanocarriers, therapeutic effect.
Classification number:
3.6
DOI : 10.31276/VJSTE.64(3).62-68
Life ScienceS
|
Biomedical applications
63
SEPTEMBER 2022
Volume 64 Number 3
Nano drug delivery systems loading Andrographolide
Nanostructures including inorganic nanoparticles (NPs),
polymeric NPs, lipid-based NPs, micelles, and nanovesicles are
employed for delivery of AG to boost the therapeutic effects on
various types of diseases.
Inorganic NPs
Inorganic NPs are non-toxic, biocompatible, as well as
hydrophilic and highly stable in comparison with organic ones
[11]. Besides, inorganic NPs have received a lot of attention
as drug or gene delivery vehicles because of their high cellular
absorption ability, low immunogenic response, and low
cytotoxicity. Inorganic NPs include calcium phosphate, silica,
iron oxide, magnesium phosphate, gold, and other metals. The
electromagnetic, optical, and catalytic properties of metal NPs
such as gold and silver NPs are known to be influenced by
their shape and size. The targetability and controlled release of
these NPs were obtained through physicochemical modification
[8] mainly by conjugating with organic components, making
them exceedingly biocompatible. The combination of inorganic
NP design with multidisciplinary approaches enables future
applications of AG in drug delivery and tissue engineering [11].
Mesoporous silica NPs (MSNs) have a highly organized
mesoporous structure that may give an exceptionally high
specific surface area and aperture volume, which are suited for
drug loading among different inorganic NPs, especially AG.
Therefore, AG powder was loaded onto MSNs, obtained size
around 100 nm, with a significantly high loading capacity (LC)
of 22.38±0.71%. Furthermore,
in vitro
evaluation proved that AG
MSNs could decrease post-inflammatory factors by about 40%.
Moreover, AG-loaded-MSNs were designed as a pH-responsive
system, which enable these NPs to break down in an acidic
osteoarthritis environment. With a phospholipid coating layer,
MSNs as nanocarriers demonstrated good lubricating capability
in the treatment of osteoarthritis [8] (Table 1).
Polymeric NPs
Polymeric NPs are one of the most popular types of
nanocarriers, which contain natural polymers like chitosan,
alginate, gelatine, and synthesis polymers such as polylactide
(PLA) [21] and copolymers like polylactide-co-glycolide (PLGA)
[22]. Synthetic polymers with high batch-to-batch repeatability
and purity make it easier to change the pattern of drug release
from polymeric NPs [23].
In one study, a cationic-modified PLGA was used to
fabricate biopolymeric NPs loading
A. paniculata
extraction in
95% ethanol. Briefly, the preparation of the NPs is conducted
with PLGA, Pluronic F-127, and chloroform, then collected by
ultracentrifugation. AG NPs had an encapsulation efficiency (EE)
value of 43.39±0.33% in a 200-nm size range. The AG polymeric
NPs had an important impact on the induction of CCl
4
activity
by the increase of antioxidant enzymes in the liver at more than
50% effectiveness compared to the blank AG ones [15]. Besides,
chitosan-modified AG NPs on hepatic antioxidant enzymes were
also fabricated to enhance the bioactivities of AG [24]. Poorly
soluble chemicals may have significant adverse effects when
systemically given over long periods of time. Incorporation of
medicinal compounds in the hydrophobic cavity of NPs produces
the desired outcomes
in vitro
and
in vivo
. Furthermore, the
procedures for synthesizing polymers, which can have a variety
of side effects and toxicity when using chemical methods, should
be considered [25].
Micelles
Polymeric micelles, which are generated by the self-assembly
of amphiphilic blocks or grafted copolymers, have the following
advantages such as suitability for delivery of both hydrophilic
and hydrophobic bioactive chemicals, biodegradability,
biocompatibility, and an extended lifecycle
in vivo
through a
“stealth effect”, which allows them to be more precise in active
drug targeting [26].
In recent years, numerous types of copolymers have been
developed. Because of their biocompatibility and biodegradability,
as well as their ability to control drug release, amphiphilic
copolymers of PEG and PLGA are mainly used for polymeric
micelle formation. In
in vitro
cytotoxicity experiments on MAD-
MB-231 cells, even at high concentrations, blank PLGA-PEG-
PLGA micelles exhibited no cytotoxicity. Besides, AG polymeric
micelles by modified PLGA-PEG-PLGA copolymers had
sufficient size, less than 200 nm with no aggregation or adhesion,
as well as EE and loading capacity (LC) values of 92.1±0.98%,
8.4±0.04%, respectively. There was no significant change in
Nano-type
s
Excipients
Size (nm)
PDI
Zeta potential (mV)
EE (%)
LC (%)
Reference
Vesicles
Liposomes:
Soybean lecithin
Cholesterol
Mannitol
77.91±22.91
0.22±0.04
-56.13±3.33
94.77±1.77
6.70±0.69
[12]
Niosomes:
Span 60
Cholesterol
Caprylocaproyl macrogol-8 glycerides
125-226
<0.1
-34.02±1.40
97.75±1.28
N/A
[13, 14]
Inorganic NPs
Cetyltrimethyl ammonium bromide (CTAB)
2-ethoxyethanol
Aqueous ammonia
Tetraethyl orthosilicate (TEOS)
100
<0.1
−20.93±3.40
43.39±0.33
22.38±0.71
[8]
Polymeric NPs
PLGA
Chitosan
Pluronic F-127
229.7±17.17
0.234±0.02
34.4±1.87
43.39±0.33
N/A
[15]
SLNs
Egg lecithin
Tween-80
Anhydrous alcohol
Glyceryl-monostearate
Compritol ATO888
Mannitol
286.1±8.03
0.3±0.03
–20.5±0.3
91.00±0.09
3.49±0.03
[16]
Nano-emulsion
Coconut oil
Sesame oil
Jojoba oil
Polysorbate 80
Sorbitan oleate 80
Propylene glycol
225.2±3.2
0.59±0.02
-8.52±2.14
93.76±0.03
0.27±0.00
[17, 18]
Micro-emulsion
Tween 80
Isopropyl myristate
Glycerol
Sorbitol
Arachis oil
Soybean oil
15.9-18.6
0.173
22.90±31.01
N/A
N/A
[19]
Micelles
NH
2
-PEG-NH
2
polymer
PLGA-COOH
Dicyclohexyl-carbodimide
N-hydroxysuccinimide
80
<0.18
-3.5
92.1±0.98
8.4±0.04
[20]
Table 1.
andrographolide nanoparticle excipients.

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