Water Soluble
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2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Y. Santhosh Kumar ◽  
Langeswaran Kulanthaivel ◽  
G. S. Hikku ◽  
R. Saravanan ◽  
Thangavelu Lakshmi ◽  
...  

Kaempferol and combretastatin are polyphenolic compounds derived from plant sources which are known for their antibacterial activity. However, owing to their large size and water insolubility, their antibacterial activity is limited. In this context, the present study focused on the nanoformulation of kaempferol (NF-k) and combretastatin (NF-c) and their influence on water solubility and antibacterial properties. The NF-k and NF-c were prepared using the solvent evaporation method and were thoroughly characterized for evaluating the morphology, molecular vibrations, size, etc. Based on the results, it is observed that the pristine forms of kaempferol and combretastatin drugs get nanoformulated and completely soluble in water. Using particle size analyzer, the particle sizes of NF-k and NF-c were estimated as 334 nm and 260 nm, respectively, which are very fine compared to pristine kaempferol and combretastatin (5193 nm and 1217 nm, respectively). The molecular vibrations that exist in NF-k and NF-c were confirmed by the Fourier transform infrared spectra, where the nanoformulated drug showed lower intensities than the pristine form of kaempferol and combretastatin. The drug release kinetics of the nanoformulated drugs were carried out using the dialysis membrane method and were compared with their pristine forms. Owing to the size effect, the NF-k and NF-c release up to 50% of the drug in a sustained manner till 50 h showing twofold higher concentration than the control where it released 25%. The antibacterial activity was assessed by measuring the optical density at 600 nm using UV-vis spectrophotometer and displayed significant activity against gram-positive Staphylococcus aureus strain. The mechanisms behind the antibacterial activity of NF-k and NF-c were discussed in detail. The activation of ATP-dependent efflux pump system and the blockage of porin channels could be the cause for the bactericidal activity. Our understanding of efflux pumps and their role in antibacterial activity is still in its early stages. No studies have been performed to date using nanoformulations of kaempferol and combretastatin to investigate their roles. This complicates the determination of the exact mechanisms acting against bacterial growth when using nanoformulation drugs. Our increasing knowledge of water-soluble nanoformulation drugs and their roles in reduced bacterial activity will pave the way to developing effective treatments in the future.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1776
Author(s):  
Lingling Qi ◽  
Chao Liu ◽  
Yingying Zhang ◽  
Zheao Zhang ◽  
Hongxia Duan ◽  
...  

Micelle is mainly used for drug delivery and is prepared from amphiphilic block copolymers. It can be formed into an obvious core-shell structure that can incorporate liposoluble drugs. However, micelles are not suitable for the encapsulation of water-soluble drugs, and it is also difficult to maintain stability in the systemic circulation. To solve these problems, a type of polymer material, Fmoc-Lys-PEG and Fmoc-Lys-PEG-RGD, was designed and synthesized. These copolymers could self-assemble into micelles driven by π–π stacking and the hydrophobic interaction of 9-fluorenylmethoxycarbony (Fmoc) and, at the same time, form a framework for a hydrogen-bonding environment in the core. Mitomycin C (MMC), as a water-soluble drug, can be encapsulated into micelles by hydrogen-bonding interactions. The interaction force between MMC and the polymers was analyzed by molecular docking simulation and Fourier transform infrared (FTIR). It was concluded that the optimal binding conformation can be obtained, and that the main force between the MMC and polymers is hydrogen bonding. Different types of MMC nanoparticles (NPs) were prepared and the physicochemical properties of them were systematically evaluated. The pharmacodynamics of the MMC NPs in vitro and in vivo were also studied. The results show that MMC NPs had a high uptake efficiency, could promote cell apoptosis, and had a strong inhibitory effect on cell proliferation. More importantly, the as-prepared NPs could effectively induce tumor cell apoptosis and inhibit tumor growth and metastasis in vivo.


2021 ◽  
Vol 11 (21) ◽  
pp. 9917
Author(s):  
Regina M. B. O. Duarte ◽  
Armando C. Duarte

The current understanding of water-soluble organic aerosol (OA) composition, sources, transformations, and effects is still limited to outdoor scenarios. However, the OA is also an important component of particulate matter indoors, whose complexity impairs a full structural and molecular identification. The current limited knowledge on indoor OA, and particularly on its water-soluble organic matter (WSOM) fraction is the basis of this feature paper. Inspired by studies on outdoor OA, this paper discusses and prioritizes issues related to indoor water-soluble OA and their effects on human health, providing a basis for future research in the field. The following three main topics are addressed: (1) what is known about the origin, mass contribution, and health effects of WSOM in outdoor air particles; (2) the current state-of-the-art on the WSOM in indoor air particles, the main challenges and opportunities for its chemical characterization and cytotoxicity evaluation; and (3) why the aerosol WSOM should be considered in future indoor air quality studies. While challenging, studies on the WSOM fraction in air particles are highly necessary to fully understand its origin, fate, toxicity, and long-term risks indoors.


Gels ◽  
2021 ◽  
Vol 7 (4) ◽  
pp. 179
Author(s):  
Youjie Sheng ◽  
Canbin Yan ◽  
Yang Li ◽  
Yunchuan Peng ◽  
Li Ma ◽  
...  

The foams stabilized by nanoparticles (NPs), water-soluble polymers, and surfactants have potential application prospects in the development of new, environmentally friendly firefighting foams. In the present study, a gel foam containing a water-soluble polymer (xanthan gum, XG), hydrophilic silica NPs, hydrocarbon surfactant (SDS), and fluorocarbon surfactant (FS-50) were prepared. The surface activity, conductivity, viscosity, and foaming ability of foam dispersions were characterized. The gel foam stability under a radiation heat source and temperature distribution in the vertical foam layer were evaluated systematically. The results show that the addition of NPs and XG has a significant effect on the foaming ability, viscosity and foam thermal stability, but has a very subtle effect on the conductivity and surface activity. The foaming ability of the FS-50/SDS solution was enhanced by the addition of NPs, but decreased with increasing the XG concentration. The thermal stability of the foams stabilized by SDS/FS-50/NPs/XG increased with the addition of NPs and increasing XG concentration. Foam drainage and coarsening were significantly decelerated by the addition of NPs and XG. The slower foam drainage and coarsening are the main reason for the intensified foam thermal stability. The results obtained from this study can provide guidance for developing new firefighting foams.


2021 ◽  
Vol 784 ◽  
pp. 139091
Author(s):  
Yanyan Li ◽  
Guichen Li ◽  
Qian zhang ◽  
Yuxia Li ◽  
Qifan Jia ◽  
...  

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