CURCUMIN-BASED MULTIFUNCTIONAL NANOSYSTEMS

The use of multifunctional nanosystems in medicine and research is of contemporary interest. Aim. The purpose of the work was to summarize publications on the prospects of creating and using nanocontainers based on curcumin (Cur). Cur fluorescence in nanoparticles (NP) makes it possible to investigate the distribution of fluorescent and non-fluorescent components, significantly accelerating the study and implementation of drugs in practice. Particular attention is paid to the use of hydrophobic substances in NP, to penetrate into a living cell. Understanding the interaction of NP with living cells is extremely important when these particles are used to transport and deliver water-insoluble drugs to cells. Cur is one of the drugs with various and very promising pharmaceutical effects, it is poorly soluble in aqueous media, and the use of nanocarriers is an effective way to significantly increase its bioavailability. Cur has its own fluorescence, which enables to use it in multifunctional fluorescent nanosystems, for example, with Pluronic® micelles. The use of the fluorescence method makes it possible to trace the stages of interaction of Cur-loaded NP with cultured cells and their localization in cell organelles. With this approach, nanoscale dynamics of drug distribution and stability is observed over time. Conclusions. The main conclusion is that for unstable in the aquatic environment drugs such as Cur, it is necessary to use the most hydrophobic nanostructures without traces of water, which include the nuclei of Pluronic® micelles. This method makes it possible to use other poorly water-soluble drugs. A promising area of nanomedicine is the creation of complex bio-compatible nanomaterials based on several active drugs that reduce the toxicity of preparations to normal cells.

Evaluation of Bacterial Biofilm as Biosensor for Detecting Phenol, Catechol, and 1,2-dihydroxynaphthalene

Monitoring of water quality from the presence of polyaromatic hydrocarbon (PAHs) compounds and its derivates are important for keeping the healthy aquatic environment. Some of those derivates are phenol and several related compounds sharing simmilar structures. This reseach aimed for the detection of those phenol and several similar compounds monitoring due to PAHs degradation. Three identified bacterial isolates of Pseudomonas aeruginosa, Staphylococcus sciuri, and Bacillus amyloliquifaciens were selected based on their phenol degradation characters. On physiological properties all three isolates were observed to degrade several hydrophobic substances such as for naphthalene and anthracene. Yet, genetic analysis indicated that the phenolic degradating oxygenase gene was detected only in the P. aeruginosa and S. sciuri. Applying those isolates for biofilm as biosensor showed a sufficient analytical performance such as their limit of detection between 0.1-0.5 μM.

A rapid screening method to select microdialysis carriers for hydrophobic compounds

Microdialysis is a minimally invasive sampling technique which is widely applied in many fields including clinical studies. This technique usually has limitation on sampling hydrophobic compounds as aqueous solutions are commonly used as the perfusates. The relative recovery of hydrophobic compounds is often low and irreproducible because of the non-specific binding to microdialysis membranes or catheter tubing. Carriers such as cyclodextrins have been used to improve the recovery and consistency, however the identification of an optimal carrier can only be achieved after time-consuming and costly microdialysis experiments. We therefore developed a rapid, convenient, and low-cost method to identify the optimal carriers for sampling hydrophobic compounds with the use of centrifugal ultrafiltration. Doxorubicin was used as the model compound and its relative recoveries obtained from centrifugal ultrafiltration and from microdialysis were compared. The results show that the relative recoveries are highly correlated (correlation coefficient ≥ 0.9) between centrifugal ultrafiltration and microdialysis when different types or different concentrations of cyclodextrins were used as the carriers. In addition to doxorubicin, this method was further confirmed on three other drugs with different hydrophobicity. This method may facilitate and broaden the use of microdialysis perfusion on sampling or delivering hydrophobic substances in various applications.

Size-Dependent Biodistribution of Fluorescent Furano-Allocolchicinoid-Chitosan Formulations in Mice

The aim of this study was to compare the biodistribution in mice of functionalized rhodamine B (Rh) labeled colchicine derivative furano-allocolchicinoid (AC, 6) either conjugated to 40 kDa chitosan (AC-Chi, 8) or encapsulated into chitosan nanoparticles (AC-NPs). AC-NPs were formed by ionotropic gelation and were 400–450 nm in diameter as estimated in mice by dynamic light scattering and confocal microscopy. AC-Chi and AC-NPs preserved the specific colchicine activity in vitro. AC preparations were once IV injected into C75BL/6 mice; muscles, spleen, kidney, liver, lungs, blood cells and serum were collected at 30 min, 2, 5, 10, and 20 h post injection. To analyze the distribution of the furano-allocolchicinoid preparations in body liquids and tissues, Rh was measured directly in sera or extracted by acidic ethanol from tissue homogenates. Preliminary Rh extraction rate was estimated in vitro in tissue homogenates and was around 25–30% from total quantity added. After in vivo injection, AC-NPs were accumulated more in liver and spleen, while less in kidney and lungs in comparison with free AC and AC-Chi. Therefore, incorporation of colchicine derivatives as well as other hydrophobic substances into nano/micro sized carriers may help redistribute the drug to different organs and, possibly, improve antitumor accumulation.

When Albumin Meets Liposomes: A Feasible Drug Carrier for Biomedical Applications

Albumin, the most abundant protein in plasma, possesses some inherent beneficial structural and physiological characteristics that make it suitable for use as a drug delivery agent, such as an extraordinary drug-binding capacity and long blood retention, with a high biocompatibility. The use of these characteristics as a nanoparticle drug delivery system (DDS) offers several advantages, including a longer circulation time, lower toxicity, and more significant drug loading. To date, many innovative liposome preparations have been developed in which albumin is involved as a DDS. These novel albumin-containing liposome preparations show superior deliverability for genes, hydrophilic/hydrophobic substances and proteins/peptides to the targeting area compared to original liposomes by virtue of their high biocompatibility, stability, effective loading content, and the capacity for targeting. This review summarizes the current status of albumin applications in liposome-based DDS, focusing on albumin-coated liposomes and albumin-encapsulated liposomes as a DDS carrier for potential medical applications.

Weldability of Underwater Wet-Welded HSLA Steel: Effects of Electrode Hydrophobic Coatings

The paper presents the effects of waterproof coatings use to cover electrodes on the weldability of high-strength, low-alloy (HSLA) steel in water. With the aim of improving the weldability of S460N HSLA steel in water, modifications of welding filler material were chosen. The surfaces of electrodes were covered by different hydrophobic substances. The aim of the controlled thermal severity (CTS) test was to check the influence of these substances on the HSLA steel weldability in the wet welding conditions. The visual test, metallographic tests, and hardness Vickers HV10 measurements were performed during investigations. The results proved that hydrophobic coatings can reduce the hardness of welded joints in the heat-affected zone by 40–50 HV10. Additionally, the number of cold cracks can be significantly reduced by application of waterproof coatings on the filler material. The obtained results showed that electrode hydrophobic coatings can be used to improve the weldability of HSLA steel in underwater conditions.

The effect of hydrophobic gases on the nervous system of Daphnia magna

Hundreds of hydrophobic substances: alkanes, alcohols, benzodiacepines, barbiturates, ethers and even gases, can induce General Anaesthesia (GA) in mammal animals. Moreover, it has been suggested that the primary site of action of such agents is on the spinal cord. Here, we investigate a scenario that is in double measure important to understand the mechanisms behind GA: its induction under water in invertebrate animals. We evaluate the capacity of xenon, nitrous oxide and krypton to suppress harmful sensations, provoked by intense light, in the crustacean D. magna. Due to the hydrophobic characteristics of those gases, we designed a special chamber to force them to dissolve in water at pressures up to to 50 atmospheres, whereas at the same time measure in real time the motility of the animals. Surprisingly, the aquatic animals are immobilized with xenon and nitrous oxide. Under this condition, they don’t respond to a noxious stimulus. Our results are crucial to understand the action of inert gases in GA and the role of the spinal cord.

Fabrication and Characterization of Human Serum Albumin Particles Loaded with Non-Sericin Extract Obtained from Silk Cocoon as a Carrier System for Hydrophobic Substances

Non-sericin (NS) extract was produced from the ethanolic extract of Bombyx mori silk cocoons. This extract is composed of both carotenoids and flavonoids. Many of these compounds are composed of substances of poor aqueous solubility. Thus, this study focused on the development of a carrier system created from biocompatible and biodegradable materials to improve the biological activity of NS extracts. Accordingly, NS was incorporated into human serum albumin template particles with MnCO3 (NS-HSA MPs) by loading NS into the preformed HAS-MnCO3 microparticles using the coprecipitation crosslinking dissolution technique (CCD-technique). After crosslinking and template dissolution steps, the NS loaded HSA particles are negatively charged, have a size ranging from 0.8 to 0.9 µm, and are peanut shaped. The degree of encapsulation efficiency ranged from 7% to 57% depending on the initial NS concentration and the steps of adsorption. In addition, NS-HSA MPs were taken up by human lung adenocarcinoma (A549 cell) for 24 h. The promotion of cellular uptake was evaluated by flow cytometry and the results produced 99% fluorescent stained cells. Moreover, the results from CLSM and 3D fluorescence imaging confirmed particle localization in the cells. Interestingly, NS-HSA MPs could not induce inflammation through nitric oxide production from macrophage RAW264.7 cells. This is the first study involving the loading of non-sericin extracts into HSA MPs by CCD technique to enhance the bioavailability and biological effects of NS. Therefore, HSA MPs could be utilized as a carrier system for hydrophobic substances targeting cells with albumin receptors.