BACKGROUND: Fucoxanthin is a hydrophobic carotenoid with many beneficial biological activities. However, due to low aqueous solubility their clinical efficacy is limited thus leading to poor oral bioavailability. To address this issue, we encapsulated fucoxanthin in rhamnolipid fabricated bovine serum albumin (BSA) loaded nanoparticles (LNPs) for improving solubility dependent bioavailability of fucoxanthin.RESULTS: These synthesized LNPs were characterized by dynamic light scattering (DLS), ultraviolet (UV)-visible spectrophotometry, high-performance liquid chromatography (HPLC), Fourier-transform infrared (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC). Our results showed that LNPs were spherical in shape with particle size around 180 nm along with positive zeta potential. The encapsulation efficiency and loading efficiency calculated for LNPs were 69.66 ± 1.5% and 14 ± 0.2%, respectively. The antioxidant assay of LNPs indicate high radical scavenging activity compared to pure fucoxanthin. Besides this, our release studies indicates that drug release occur from the matrix of nanocarrier system through diffusion based on concentration. Thus, these findings indicate successful encapsulation of fucoxanthin, with improved solubility thereby leading to increased bioavailability. This nano formulation is derived from components which are FDA approved that could be exploited for encapsulating other vital nutraceutical molecules. CONCLUSION: Overall, our results showed successful synthesis of biodegradable nanocarrier for delivering fucoxanthin supported by molecular docking, molecular dynamics simulation and thermodynamics of free binding energy studies.
Cordycepin gets rapidly metabolized in the body into inactive form due to its structural similarity to adenosine, thus inhibiting its development as a medicinal agent. This study was aimed to improve the solubility and stability of cordycepin, a potential drug with known antiproliferative activity, by encapsulating it in bovine serum albumin: β-cyclodextrin nanoparticles. Cordycepin-loaded nanoparticles (CLNPs) were synthesized using the antisolvent method and characterized thoroughly using various techniques. Our dynamic light scattering measurement showed a particle size and zeta potential of 160 ± 2.75 nm and −20.21 ± 2.1 mV, respectively, for CLNPs. Transmission electron microscopy studies revealed that particles were spherical in morphology. These CLNPs showed sustained release of cordycepin with encapsulation and loading efficiency of 81.62 ± 1.5 and 27.02 ± 2.0%, respectively, based on high-performance liquid chromatography and UV−vis studies. Based on differential scanning calorimetry and zeta potential studies, CLNPs improve cordycepin stability and solubility. Our molecular simulations and binding energy calculation also showed favorable protein interaction between cordycepin, bovine serum albumin, and β-cyclodextrin, further supporting the notion of improved stability. In vitro cytotoxicity, apoptosis, and cellular uptake studies on breast cancer cells showed that the synthesized nanoparticles had greater cytotoxicity as compared to free cordycepin.
<p>Severe Acute Respiratory Syndrome Coronavirus 2 (SARS- CoV-2)
affects human respiratory function that causes COVID-19 disease. COVID-19 has
spread rapidly all over the world and became a pandemic within no time. Therefore,
it is the need of hour to screen potential lead candidates from natural
resources like edible mushrooms and marine fungi. These natural resources are
very less explored till now and known to be the source for many medicinal compounds
with several health benefits. These medicinal compounds can be easily exploited
for the faster development of nutraceuticals for controlling SARS-CoV-2
infections. Our in-silico research suggests that bioactive compounds originating
from mushroom and marine fungi shows strong potential to interact with ACE2
receptor or main protease of SARS-CoV-2, showing the inhibition activity
towards the enzymatic protease. We performed a series of in silico studies for
the validation of our results, which includes Molecular docking, drug likeness property
investigation by Swiss ADME tools, MD simulation, and thermodynamically stable
free binding energy calculation. Overall, these results suggest that Ganodermadiol
and Heliantriol
F bioactive compounds originating from edible mushroom has strong
potential to be developed as low-cost nutraceutical against SARS-CoV-2 viral
infection. The drug candidate isolated from marine fungi and edible mushroom
are highly unexplored for the development of potential alternative drug against
SARS-CoV-2 virus with minimum side effects. That is why we decided to screen
some active metabolites from the marine fungi and mushrooms, which offer some
encouraging results. Though our in-silico studies of these compounds are showing
a promising result against SARS-CoV-2 main protease and ACE2 receptor binding
domain, the effectiveness of these bioactive compounds should be further
validated by proper clinical trials.</p>
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