102-1 食生系碩士在職專班專題討論
5101043001
何一正
Curcumin nanoformulations:a future nutraceutical for bioavaliability
Abstract
Curcumin, a natural diphenolic compound derived from turmeric Curcuma longa. In recent years,
scientists has been focused on curcumin due to its varieties bio-function without side effects such as
cancer, diabetes, cardiovascular diseases, arthritis, Alzheimer's disease, etc. only a few novel
multifunctional and composite nanosystem strategies offer simultaneous therapy as well as imaging
characteristics. The challenges to developing curcumin delivery platforms and up-to-date solutions
for improving curcumin bioavailability as bioactive nanoparticle drug potential for therapy.
Nanoparticle encapsulation improves oral bioavailability of curcumin
Curcumin, a derived product from common spice turmeric that is safe and beneficial in several
aliments was formulated into biodegradable nanoparticles with a view to improve its oral
bioavailability [1]. The curcumin encapsulated nanoparticles prepared by emulsion technique were
spherical in shape with particle size of 264 nm (polydispersity index 0.31) and 76.9% entrapment at
15% loading. Curcumin loaded PLGA nanoparticles were prepared by emulsion–diffusion–
evaporation method. Of the various stabilizers screened for preparation of nanoparticles, CTABgave
particles of smallest size compromising the entrapment, while those with PVA gave particles with
highest entrapment but larger size. Pluronic F-68 and Vit. ETGPS produced particles of
intermediate size and entrapment efficiency. Comparative in vivo plasma concentration vs. time
profiles of different curcumin formulations. The in vivo pharmacokinetics revealed that curcumin
entrapped nanoparticles demonstrate at least 9-fold increase in oral bioavailability when compared
to curcumin administered with piperine as absorption enhancer.[2]. Recently developed curcumin
organogel was used as the oil phase in the curcumin nanoemulsion formulation. Tween 20 was
selected as the emulsifier on the basis of maximum in vitro bioaccessibility of curcumin in the
nanoemulsion. In vitro lipolysis profile revealed that the digestion of nanoemulsion was
significantly faster and more complete than the organogel. Permeation experiments on Caco-2 cell
monolayers suggested that digestion-diffusion was the major absorption mechanism for curcumin in
the nanoemulsion [3]. The curcumin encapsulated in casein nanoparticles had higher biological
activity, as assessed by antioxidant and cell proliferation assays, than pristine curcumin, likely due
to the improved dispersibility. To simplify sample preparation, sodium caseinate (NaCas), a
commercially available ingredient produced by acid precipitation of caseins from bovine milk
followed by neutralization using sodium hydroxide for spray-drying. This simple approach may be
applied to encapsulate various lipophilic bioactive compounds [4]. The conjugated curcumin with
silica nanoparticles to improve its aqueous solubility and hence to make it more bioavailable.
Conjugation and loading of curcumin with silica nanoparticles was further examined with
transmission electron microscope (TEM) and thermogravimetric analyzer. conjugation of curcumin
with silica nanoparticles by using a simple wet chemical method. This protocol envisages good
bioavailability of the curcumin molecule, keeping its therapeutic activity intact. Further, this
conjugate was studied against cancerous and primary cell lines. Cytotoxicity analysis of synthesized
silica:curcumin conjugate was studied against HeLa cell lines as well as normal fibroblast cell lines.
This study shows that silica:curcumin conjugate has great potential for anticancer application [5].
Examination of the Permeation Mechanism of Curcumin in the Nanoemulsion
102-1 食生系碩士在職專班專題討論
5101043001
何一正
The permeation mechanism for curcumin in the organogel-based nanoemulsion was investigated
using Caco-2 cell monolayers to mimic the small intestine epithelium. There are two possible
mechanisms for curcumin nanoemulsion permeation: (1) Nanoemulsions would be digested by
lipase and simultaneously curcumin is solubilized by bile salts-fatty acids mixed micelles.
Subsequently, solubilized curcumin passively diffuses across the epithelium layer. This represents
the classic digestion−diffusion route applicable for all the regular lipid-based formulations; (2)
intact nanoemulsions, because of their small size, would be able to directly diffuse across the small
intestine layer without digestion [2-4].
Bioactive of curcumin nanoparticles
nanoparticulate curcumin was comparatively more effective than native curcumin against different
cancer cell lines under in vitro condition with time due to enhanced cellular uptake resulting in
reduction of cell viability by inducing apoptosis. Molecular basis of apoptosis studied by western
blotting revealed blockade of nuclear factor kappa B (NFkB) and its regulated gene expression
through inhibition of IkB kinase and Akt activation. In mice, nanoparticulate curcumin was more
bioavailable and had a longer half-life than native curcumin as revealed from pharmacokinetics
study. Thus, the results demonstrated nanoparticulate curcumin may be useful as a potential
anticancer drug for treatment of various malignant tumors [6]. ALG-CS-PF127 composite NPs have
the potential to meet some of the challenges of nanoformulation of hydrophobic drugs for delivery
to cancer cells. These composite NPs have a suitable size distribution, drug encapsulation efficiency,
and drug release kinetics. All the three components of the composite NPs—namely ALG, CS, and
PF127—have reported biocompatibility [7].
Conclusions
These varieties types of NPs have been establish to be appropriate for the encapsulation or loading
of curcumin to get better its effects in bioavailability and biofunction. The characteristics of these
curcumin nanoformulations can be modified according to the specific obligation for inducing
cellular death by various mechanisms. Overall, our understanding from the available literature is
that the use of curcumin nanoparticles in chemotherapy for cancer treatment and other disease is a
facile modality that improves existing curcumin therapies by targeting tumors or proteins and by
reducing the drug dose required. The safety of the various curcumin nanoformulations and their
efficacy in the cell-line models draw attention to their potential for estimate in in vivo models. In
the feature, the human trials need to be conducted to establish their effectiveness in clinical
applications as an improved therapeutic modality for disease treatment.
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