A series of Nα-phthaloyl bridged cyclic pentapeptide derivatives were synthesized and characterized on the basis of spectral and elemental analyses. A preliminary cytotoxicity evaluation of all novel compounds was carried out against four human cancer cell lines, human lung (A-549), colon (CaCo-2), prostate (PC-3) and breast (MCF-7) cancer cells at 100 μM concentration using MTT growth inhibition assay. Compound 3 gave the highest cytotoxic activity towards the human colon (CaCo-2) cancer cell line (Growth Inhibition = 72.4 %). Further molecular docking of the promising derivative 3 was developed to study its binding mode within the active site of EGFR enzyme. The docking results suggest good fitting through different hydrogen bond interactions with the protein residues to elicit anticancer activity

https://ejchem.journals.ekb.eg/article_58172_1a00fe97564f76dae5bebd252d05c2a5.pdf

Design, Synthesis and Molecular Docking Studies of Novel Cyclic Pentapeptides Based on Phthaloyl Chloride with Expected Anticancer Activity

Docetaxel (DTX)-based formulation development is still confronted with significant challenges, due to its refractory solubility and side effects on normal tissues. Inspired by the application of the transdermal drug delivery model to topical treatment, we developed a biocompatible and slow-release DTX-containing emulsion via self-assembly prepared by a high-speed electric stirring method and optimized the formulation. The results of accelerated the emulsion stability experiment showed that the emulsion prepared at 10,000 rpm/min had a stability of 89.15 ± 2.05%. The ADME, skin irritation, skin toxicity and molecular interaction between DTX and excipients were predicted via Discovery Studio 2016 software. In addition, DTX addition in oil or water phases of the emulsion showed different release rates in vitro and ex vivo. The DTX release ex vivo of the DTX/O-containing emulsion and the DTX/W-containing emulsion were 45.07 ± 5.41% and 96.48 ± 4.54%, respectively. In vitro antioxidant assays and anti-lipid peroxidation models revealed the antioxidant potential of DTX. However, DTX-containing emulsions could maintain and even enhance the antioxidant effect, both scavenging free radicals in vitro and inhibiting the process of lipid peroxidation.

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The Fabrication of Docetaxel-Containing Emulsion for Drug Release Kinetics and Lipid Peroxidation

The development of biocompatible nanocomposite hydrogels with effective wound healing/microbicidal properties is needed to bring out their distinguished characteristics in clinical applications. The positive interaction between graphene oxide/reduced graphene oxide (GO/rGO) and hydrogels and aloe vera gel represents a strong strategy for the advancement of therapeutic approaches for wound healing. In this study, the synthesis, characterization, and angiogenic properties of graphene-based nanocomposite gels have been corroborated and substantiated through several in vitro and in vivo assays. In this respect, graphene oxide was synthesized by incorporating a modified Hummer’s method and ascertained by Raman spectroscopy. The obtained GO and rGO were uniformly dispersed into the aloe vera gel and hydrogel, respectively, as wound healing materials. These formulations were characterized via in vitro bio-chemical techniques and were found suitable for the appropriate cell viability, attachment, and proliferation. In addition, in vivo experiments were conducted using male Wistar rats. This revealed that the GO/rGO-based gels stimulated wound contraction and re-epithelialization compared to that of the non-treatment group. From the study, it is suggested that GO/rGO-based aloe vera gel can be recommended as a promising candidate for wound healing applications.

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Efficacy of Graphene-Based Nanocomposite Gels as a Promising Wound Healing Biomaterial

Sinomenine (SIN), a natural product, has been used to treat rheumatoid arthritis (RA) in China for thousands of years. SIN has been developed for the treatment of RA by way of tablets and injections, but both dosage forms have been associated with severe adverse reactions. Making SIN into liposomes-in-hydrogel biomaterials for external use has a good slow-release effect and can play an important role in avoiding the first-pass effect, gastrointestinal reaction, and increasing the local action time of drugs. SIN-loaded liposomes were formed by the thin-film dispersion method, then SIN-loaded liposomes-in-hydrogels were prepared by combining the SIN-L with hyaluronic acid (HA) hydrogels. In this paper, the basic characteristics, In vitro and Ex vivo release, and antioxidant activity of SIN-loaded liposomes-in-hydrogels were studied. The results showed that SIN-loaded liposomes-in-hydrogels have good sustained-release and antioxidant effects, and the preparation is expected to be a good biomaterial. 

<i>In vitro</i> and <i>Ex vivo</i> Antioxidant Activity and Sustained Release Properties of Sinomenine-Loaded Liposomes-in-Hydrogel Biomaterials Simulating Cells-in-Extracellular Matrix

Modified polymeric gels, including nanogels, which play not only the role of a bioinert matrix, but also perform regulatory, catalytic, and transport functions due to the active fragments introduced into them, can significantly advance the solution to the problem of targeted drug delivery in an organism. This will significantly reduce the toxicity of used pharmaceuticals and expand the range of their therapeutic, diagnostic, and medical application. This review presents a comparative description of gels based on synthetic and natural polymers intended for pharmaceutical-targeted drug delivery in the field of therapy of inflammatory and infectious diseases, dentistry, ophthalmology, oncology, dermatology, rheumatology, neurology, and the treatment of intestinal diseases. An analysis was made of most actual sources published for 2021–2022. The review is focused on the comparative characteristics of polymer gels in terms of their toxicity to cells and the release rate of drugs from nano-sized hydrogel systems, which are crucial initial features for their further possible application in mentioned areas of biomedicine. Different proposed mechanisms of drug release from gels depending on their structure, composition, and application are summarized and presented. The review may be useful for medical professionals, and pharmacologists dealing with the development of novel drug delivery vehicles.

/pdf/polymeric-gel-systems-cytotoxicity-and-drug-release-as-key-1ytetf1c.pdf

Polymeric Gel Systems Cytotoxicity and Drug Release as Key Features for their Effective Application in Various Fields of Addressed Pharmaceuticals Delivery

The purpose of this study was to prepare and evaluate kaempferol-loaded carbopol polymer (acrylic acid) hydrogel, investigate its antioxidant activity in vitro, and compare the effects on drug release under different pH conditions. Drug release studies were conducted in three different pH media (pH 3.4, 5.4, and 7.4). The kaempferol-loaded hydrogel was prepared by using carbopol 934 as the hydrogel matrix. The morphology and viscosity of the preparation were tested to understand the fluidity of the hydrogel. The antioxidant activity of the preparation was studied by scavenging hydrogen peroxide and 2,2-diphenyl-1-picrilhidrazil (DPPH) radicals in vitro and inhibiting the production of malondialdehyde in mouse tissues. The results showed that kaempferol and its preparations had high antioxidant activity. In vitro release studies showed that the drug release at pH 3.4, 5.4, and 7.4 was 27.32 ± 3.49%, 70.89 ± 8.91%, and 87.9 ± 10.13%, respectively. Kaempferol-loaded carbopol hydrogel displayed greater swelling and drug release at higher pH values (pH 7.4).

/pdf/in-vitro-evaluation-of-kaempferol-loaded-hydrogel-as-ph-23ej6s1l.pdf

In Vitro Evaluation of Kaempferol-Loaded Hydrogel as pH-Sensitive Drug Delivery Systems

A simple approach for the synthesis of Ortho Phthaloyl Chloride(OPC) was studied .Response surface methodology (RSM) was used to optimize the synthesis conditions of OPC. A 4-factor central composite design (CCD) was used for experimental design and analysis to obtain the optimal processing parameters, such as amount of triphosgene(BTC), amount of catalyst, reaction temperature and time. The 3-D response surface and the contour plots derived from the mathematical models were applied to determine the optimal conditions. The optimum reaction conditions were as follows: amount of BTC 62 g, amount of cat. 3.3 g, reaction temperature 75°C, reaction time 5 h. Under these conditions, The yield of OPC was 96.61%. Comparison of predicted and experimental values revealed good correspondence, implying that empirical model could be used to adequately describe the relationship between the factors and response in OPC synthesis process.

Synthesis of Ortho Phthaloyl Chloride Using Triphosgene by Response Surface Methodology

g-C_3N_5 is a new 2D material synthesized only in the last few years which has better absorption ability in visible light range than traditional g-C_3N_4. However, the narrower bandgap restricts its redox ability when used as a photocatalyst. In this work, ferric iron and g-C_3N_5 heterojunctions were prepared through post-calcination (Fe/CN-a) and solvothermal (Fe/CN-b) methods. The photo-Fenton catalytic activity of Fe/CN-a under visible light is remarkably increased by 17.0 times compared to the g-C_3N_5 in degrading methyl orange (an anionic dye), while that of Fe/CN-b increases by 4.8 times in the degradation of methylene blue (a cationic dye). The iron element exists in the form of monodispersed Fe(III) in Fe/CN-a, while it forms α-Fe_2O_3 nanocubes in Fe/CN-b. The Z-scheme heterojunctions, which simultaneously maintain the narrow bandgap, efficient electron–hole separation and strong redox ability, account for the photo-Fenton catalytic activity enhancement. Graphical abstract

Enhancing the photo-Fenton catalytic activity of g-C_3N_5 under visible light through Z-scheme heterojunction with ferric iron

Rheumatoid arthritis (RA) is a chronic degenerative disease characterized by persistent systemic synovitis, with a high risk of stiffness, pain, and swelling. It may affect the other extra-articular tissues. There is no ideal treatment for this disease at present, and it can only be controlled by medication to alleviate the prognosis. Exosomes are small vesicles secreted by various cells in the organism under normal or pathological conditions, and play a role in immune response, antigen presentation, cell migration, cell differentiation, tumor invasion and so on. Due to the adverse effects of conventional drugs and treatments in the treatment of RA, exosomes, as a nanocarrier with many advantages, can have a great impact on the loading of drugs for the treatment of RA. This article reviews the role of exosomes in the pathogenesis of RA and the progress of exosome-based therapy for RA. 

Xi Tao Cheng

Papers

In Vitro Evaluation of Kaempferol-Loaded Hydrogel as pH-Sensitive Drug Delivery Systems

The Fabrication of Docetaxel-Containing Emulsion for Drug Release Kinetics and Lipid Peroxidation

Synthesis of Ortho Phthaloyl Chloride Using Triphosgene by Response Surface Methodology

Enhancing the photo-Fenton catalytic activity of g-C_3N_5 under visible light through Z-scheme heterojunction with ferric iron

The novel delivery-exosome application for diagnosis and treatment of rheumatoid arthritis.