Synthesis and Characterization of Poly(methyl acrylate)-grafted-Sodium Salt of Partially Carboxymethylated Tamarind Kernel Powder

Ceric ammonium nitrate (CAN)-initiated graft copolymerization of methyl acrylate (MA) onto sodium salt of partially carboxymethylated tamarind kernel powder (Na-PCMTKP, DS = 0.15) was studied in an aqueous medium by solution polymerization technique. The growth of the graft reaction was monitored gravimetrically. The role of various synthesis variables on the grafting yields was examined to achieve the maximum graft yields (%G = 278.27, %GE = 94.38, %Hp = 5.62) and the influence of the synthesis variables in the graft copolymerization has been discussed. The reactivity of methyl acrylate (MA) towards graft copolymerization was compared with that of acrylonitrile (AN) on the basis of the results obtained from the earlier studies and plausible explanation was furnished for the observed reactivity of both the monomers towards grafting. The evaluated optimized reaction conditions were utilized to study the effect of reaction medium on grafting and it was found that reaction medium plays an important role in graft copolymerization. In order to ascertain the grafting, characterization of the samples made by FTIR, TGA and SEM was conducted. The synthesized novel graft copolymer may find potential application to be used as metal adsorbents.

Synthesis and Characterization of Glycidyl Esters of Acrylic and Methacrylic Acids for NIPU Coatings

Glycidyl acrylate (GA) and Glycidylmethacrylate (GMA) are the reaction products of the epichlorohydrin (ECH) with acrylic acid (AA) and methacrylic acid (MAA) respectively. These monomers were synthesized via two different routes i.e. direct reaction of AA and MAA with ECH and second by reaction of AA and MAA with Sodium hydroxide to form sodium salt of the acid followed by reacting with ECH. The polymerization inhibitor used was tert-butyl hydroquinone (TBHQ) and catalysts used were triethylamine (TEA) and quaternary ammonium salt. Experimental results show that first route is suitable for synthesizing GA and second route is suitable for synthesis of GMA. The catalysts also have drastic effect on the conversion to the respective glycidyl esters. The study of the effect of catalyst and polymerization inhibitor has been carried out via both routes.

Protective effects of Derinat, a nucleotide-based drug, on experimental traumatic brain injury, and its cellular mechanisms

Traumatic brain injury is the most common cause of death and disability in young people including sport athletes and soldiers, people under 45 years of age in the industrialized countries, representing a growing health problem in developing countries, as well as in aging communities. Treatment of the latter is a serious challenge for modern medicine. This type of injury leads to many kinds of disorders and, quite often, to disability. These issue require development of new methods for brain trauma treatment. The new approach to brain trauma treatment was studied in murine experiments. In particular, sodium salt of deoxyribonucleic acid (DNA) was used. This preparation is a drug known as a mixture of peptides with immunomodulatory effect which is widely used for different kinds of therapy. Derinat, a sodium salt of DNA, isolated from the caviar of Russian sturgeon, is a proven immunomodulator for treatment of diseases associatd with reactive oxygen species (ROS), including brain ischemia-reperfusion (IR) injury. Here we show that treatment with Derinat exert neuroprotective, anti-oxidative, and anti-inflammatory effects in experimental model of traumatic brain injury (TBI) in rats. Intraperitoneal injection of Derinat several times over 3 days after TBI showed less pronounced damage of the injured brain area. Immunohistochemical study showed that the Derinat-induced morphological changes of microglia in cerebral cortex and hippocampus 7 days after TBI. TBI-induced accumulation of 8-oxoguanine (8-oxoG), the marker of oxidative damage, was significantly attenuated by Derinat administration, both on 7th and 14th day after TBI. To investigate cellular mechanism of anti-inflammatory effects, the primary cultures of murine microglia supplied with ATP (50 M and 1 mM), as a substance released at injured site, were used to mimic the in vitro inflammatory response. Derinate treatment caused an increase of glial levels of mRNAs encoding neurotrophic factor (GDNF) and nerve growth factor (NGF) in the presence of ATP, whereas tissue plasminogen activator (tPA) mRNA was inhibited by ATP with or without Derinat. Interleukin-6 (IL-6) mRNA expression was not affected by ATP but was increased by Derinat. Both mRNA and protein levels of ATP-induced TNFα production were significantly inhibited by Derinat. These results partially contribute to understanding mechanisms of immunomodulatory effects of DNA preparations in traumatic brain injury.

Study of the diffusion process in films sodium salt of carboxymethyl cellulose – drug

The transport properties of medicinal films based on sodium salt of carboxymethylcellulose and the antibiotic amikacin sulfate have been studied in this work. It has been shown that the process of sorption of water vapor by such films and the release of a drug from them proceeds in an abnormal diffusion mode, which is explained by the slowdown of relaxation processes in glassy polymers, which include the sodium salt of carboxymethylcellulose. An increase of the amount of the introduced drug is accompanied by a regular decrease in the diffusion coefficients of both the process of sorption of water vapor and the release of amikacin from the films. It is noted that the formed films of sodium salt of carboxymethylcellulose-amikacin sulfate dissolve in water during the day and do not provide a prolonged release of the drug. To reduce the solubility of the films in water, the surface modification of the polymer film with calcium chloride has been carried out. It has been found that the modification does not lead to a change in the diffusion mode, but is accompanied by a regular change in the diffusion coefficients – the longer the formed films were kept in a calcium chloride solution, the lower the diffusion coefficients of the sorption of water vapor by medicinal films and the diffusion coefficients of the release of the drug amikacin from the film. It is argued that the surface modification of polymer films based on the sodium salt of carboxymethylcellulose is an effective way of imparting to them the effect of prolonging the release of a drug.

Prospects and Challenges of the Drug Delivery Systems in Endometriosis Pain Management: Experimental and Theoretical Aspects

Endometriosis is considered a serious public health issue because of the large number of females affected by this illness. Chronic pain management in patients with endometriosis demands new strategies to increase the life quality of these patients. The development of drug delivery systems represents a new approach in pain treatment among endometriosis patients. Diclofenac sodium, one of the most utilized nonsteroidal anti-inflammatory drugs (NSAID), has its own limitations when being used in formulas such as oral, parental, or local applications. In this paper, a series of four drug release formulations based on chitosan, 2-hydroxy-5-nitrobenzaldehyde, and diclofenac sodium salt were prepared in view of the investigation of the drug release ability. The formulations were analyzed from a morphological and supramolecular point of view by scanning electron microscopy and polarized light microscopy. The in vitro drug release ability was investigated by mimicking a physiologic environment. A mathematical model, using the fractal paradigm of motion, is utilized to explain the behaviors of the drug delivery system presented in this paper. These results suggest a great potential of the proposed drug delivery system, based on chitosan and 2-hydroxy-5-nitrobenzaldehyde to improve the diclofenac sodium salt bioavailability, and it may represent a future treatment formula for endometriosis pain.

Exopolysaccharide Produced by Lactiplantibacillus plantarum-12 Alleviates Intestinal Inflammation and Colon Cancer Symptoms by Modulating the Gut Microbiome and Metabolites of C57BL/6 Mice Treated by Azoxymethane/Dextran Sulfate Sodium Salt

Exopolysaccharide produced by Lactiplantibacillus plantarum-12 (LPEPS) exhibited the anti-proliferating effect on human colon cancer cell line HT-29 in vitro. The purpose of the study was to determine the alleviating effects of LPEPS on colon cancer development of the C57BL/6 mice treated by azoxymethane/dextran sulfate sodium salt (AOM/DSS). The C57BL/6 mice treated by AOM/DSS were orally administered LPEPS daily for 85 days. The results showed that LPEPS oral administration enhanced colon tight-junction protein expression and ameliorated colon shortening and tumor burden of the AOM/DSS treated mice. Furthermore, LPEPS oral administration significantly reduced pro-inflammatory factors TNF-α, IL-8, and IL-1β levels and increased anti-inflammatory factor IL-10 level in the serum of the AOM/DSS-treated mice. LPEPS oral administration reversed the alterations of gut flora in AOM/DSS-treated mice, as evidenced by the increasing of the abundance of Bacteroidetes, Bacteroidetes/Firmicutes ratio, Muribaculaceae, Burkholderiaceae, and norank_o__Rhodospirillales and the decreasing of the abundance of Firmicutes, Desulfovibrionaceae, Erysipelotrichaceae, and Helicobacteraceae. The fecal metabolites of the AOM/DSS-treated mice were altered by LPEPS oral administration, involving lipid metabolism and amino acid metabolism. Together, these results suggested that LPEPS oral administration alleviated AOM/DSS-induced colon cancer symptoms of the C57BL/6 mice by modulating gut microbiota and metabolites, enhancing intestine barrier, inhibiting NF-κB pathway, and activating caspase cascade.