Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry - Volume 24, Issue 4, 2025

Trans-resveratrol is a bioactive polyphenol that has been widely studied for its antioxidant, anti-inflammatory, and chemoprotective properties. It holds promise in pharmaceutical and nutraceutical formulations but is limited by poor bioavailability and stability.

This review synthesizes validated analytical methods for quantifying trans-resveratrol across various matrices. A comprehensive literature search (2000–2024) was conducted using PubMed, Scopus, and Google Scholar, focusing on RP-HPLC, HPTLC, GC, and UV spectroscopy. Method validation follows ICH guidelines.

Thirty-seven validated analytical methods were reviewed. RP-HPLC using C18 columns with acetonitrile-water mobile phases dominated the literature. The most sensitive technique identified was LC-MS/MS (LOD = 0.001 μg/mL), particularly effective in biological samples. Matrix types included wine, serum, and nanoparticle formulations.

RP-HPLC and LC-MS/MS have emerged as robust techniques for resveratrol quantification due to their sensitivity and specificity. Emerging tools like biosensors and UPLC offer rapid analysis with lower solvent consumption. Challenges such as isomerization, photodegradation, and matrix interferences necessitate stringent sample-handling protocols.

Advanced chromatographic methods, especially RP-HPLC and LC-MS/MS, are essential for the reliable quantification of trans-resveratrol. Future research should focus on analytical standardization and the development of novel delivery systems to enhance resveratrol's pharmacokinetic profile.

The study investigated the anti-inflammatory properties of Kappaphycus alvarezii by employing zebrafish larvae as a model system.

The seaweed extract was subjected to phytochemical screening, uncovering the presence of alkaloids, terpenoids, proteins, and cardiac glycosides. UV-visible, FTIR, and GC-MS were employed to identify the presence of bioactive compounds. The western blotting method was used to confirm the target proteins.

Analysis through GC-MS revealed the presence of specific organic bioactive compounds, including 4-chlorobuten-3-yne, Methane-D, trichloro, and 1-propanol,2-(1-methylethoxy), each with distinct retention times. In the group induced with a high-cholesterol diet (HCD), the activities of antioxidant enzymes (SOD, CAT, GPx, and GST) were elevated, and K. alvarezii treatment successfully reversed this effect. Additionally, the HCD group exhibited upregulation in the protein expression of MMP-9, MMP-13, MPO, IL-6, TNFα, and NFκB due to inflammation, whereas K. alvarezii therapy reversed the inflammatory process in the treated group. These findings indicate the potential of K. alvarezii to counteract inflammatory responses induced by a high-cholesterol diet through modulation of antioxidant enzyme activities and downregulation of pro-inflammatory markers.

Kappaphycus alvarezii shows promise for developing natural sources for antiradicals, food supplements, nutraceuticals, and various functional foods with therapeutic applications.

Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used to manage pain and inflammation but are associated with gastrointestinal and cardiovascular risks, especially with COX-2 inhibitors. Topical delivery systems offer a safer alternative by minimizing systemic exposure; however, poor solubility and limited skin penetration remain challenges. Enhancing solubility through solid dispersion and incorporating it into a gel formulation may improve permeability and therapeutic effectiveness, addressing the need for safer and more efficient topical NSAID delivery.

This investigation aimed to enhance the solubility and dissolution rate of poorly water-soluble etoricoxib through the development of solid dispersions using the kneading method.

A suitable carrier was selected from a pool of candidates based on polarised microscopy analysis. The influence of a solubilizer on amorphization was evaluated. Solid dispersions of Etoricoxib and its corresponding physical mixtures, incorporating or excluding the solubilizer, were prepared at varying drug-to-carrier ratios. Yield, drug content, saturation solubility, and in vitro dissolution profiles of these formulations were determined. Solid-state characterization using Fourier Transform-Infrared (FTIR), X-ray diffraction (XRD), Scanning electron microscopy (SEM), and differential scanning calorimetry (DSC) techniques was conducted.

FTIR spectra indicated the formation of intermolecular hydrogen bonds within the dispersions. XRD, SEM, and DSC analysis confirmed the amorphous transition of crystalline etoricoxib in all the prepared solid dispersions. In comparison to pure etoricoxib and its physical mixes, the produced solid dispersions showed significantly improved dissolution and solubility.

Solid dispersion technology effectively enhanced the solubility and dissolution of poorly water-soluble etoricoxib. Polarised microscopy also proved valuable for rapid excipient screening. However, the study was limited by the narrow range of solubilizers tested. While Poloxamer 407 was selected for its availability and untapped potential, broader screening of advanced solubilizers could offer improved outcomes.

The solubility increased from 99.08 to 296.8 μg/ml and the dissolution rose from 69.32% to 98.07%. These findings suggest that the kneading method and Poloxamer successfully produced amorphous solid dispersions of etoricoxib with significantly enhanced solubility and dissolution properties, potentially improving its bioavailability.

Angiotensin-(1-7) is a crucial endocrine modulatory peptide that can enhance conditions like diabetes, obesity, and other features of metabolic syndrome. However, there is a lack of data on its long-term effects.

This study aimed to assess the impact of chronic oral administration of Angiotensin-(1-7) on adipose tissue modulation and metabolic processes in mice.

The Angiotensin-(1-7) peptide oral formulation was encapsulated within the hydroxypropyl-β-cyclodextrin oligosaccharide (HPβCD) matrix. Male Swiss mice were divided into 4 groups: standard diet (ST)+HPßCD; ST+Ang-(1-7); high-fat diet HFD+HPßCD, and HFD+Ang-(1-7). The treatment lasted for 12 months, during which body weight, food intake, glycemic and lipid profiles, visceral adiposity, oxidative stress indicators, histological parameters, quantitative real-time PCR assessments, and comprehensive in silico bioinformatics analyses were conducted.

Prolonged treatment with Ang-(1-7) led to improvements in glucose levels, visceral body adiposity, decreased cholesterol and triglyceride levels, and reduced oxidative stress. Bioinformatics analysis revealed that AKT1, an insulin signaling effector (INS), and key inflammatory markers like IL-6 and VEGF may be potential molecular mediators of Angiotensin-(1-7) effects. Non-obese animals treated with Angiotensin-(1-7) showed increased expression levels of AKT1, supporting the findings from the bioinformatics analysis.

This study demonstrates that chronic oral use of Ang-(1-7) enhances adipose and metabolic parameters, suggesting its potential as a long-term therapeutic agent for regulating metabolic disorders.

Periodontitis is a chronic inflammatory disease requiring effective anti-inflammatory treatments. Nano-silver and essential oils have shown potential due to their antimicrobial and anti-inflammatory properties. Combining these agents offers a promising therapeutic approach. This study investigated the cytotoxic and anti-inflammatory properties of a novel essential oil compound containing nanosilver using HaCaT and THP-1 human leukemia monocytic cell lines.

Neutral red uptake (NRU) assay was used to assess cytotoxicity and ELISA to evaluate the inflammatory cytokines. The test compound was compared to 0.12% chlorhexidine gluconate (CHX). Cytotoxicity was determined in HaCaT and THP-1 cell lines using NRU assay. TNF-α expression was measured using ELISA, and COX-2 inhibition assay was performed.

Cytotoxicity of the test compound was nearly absent. TNF-α levels decreased in positive control (2.81 pg/ml) and test samples (1.30 pg/ml) compared to control (22.04 pg/ml). COX-2 inhibition assay revealed test compound (0-20%) and positive control (0-100%), with 25 μM celecoxib as a standard. IC50 for HaCaT cells was 0.6334% (positive control) and 0.6051% (test group). IC50 using THP-1 cells was not converged for the test and 424.6% for positive control. IC-50 for COX-2 inhibition was 1.469% in the test and 8.801% in the positive control.

This study showed the possibility of novel essential oils and nano-silver-containing compounds as a medication material in preventing gingivitis. The cytotoxicity was negligible, while the level of TNF- α was much decreased, and COX-2 activity assays indicated its efficiency in anti-inflammatory properties. The results encourage the therapeutic potential of the compound for periodontitis, and further studies are required to demonstrate therapeutic efficiency and safety.

Results demonstrate the inhibitory effect of the test compound on COX-2 activity. The potential of a novel test compound containing essential oils and nano-silver as a promising anti-inflammatory agent warrants further investigation for its therapeutic applications in periodontitis.

The low solubility and permeability of tetrahydrocurcumin act as a barrier in its therapeutic effectiveness, particularly in the topical treatment of skin diseases like psoriasis.

Niosomes were prepared using thin-film hydration method using span 60, cholesterol as independent variables in Box Behnken design. Particle size, entrapment efficiency and drug loading were taken as dependent variables. In Box Behnken design the levels are -1, 0, and +1. The values for span 60 are 50, 75, and 100mg and for cholesterol 10, 20, and 30mg.

The optimized formulation has a particle size of 116.9 nm, entrapment efficiency of 94.7% and, drug loading of 85.23%. The niosomes showed first-order release kinetics property and maintained stability at 4°C and 25°C for three months. The desirability score obtained was 0.896.

The optimized niosomal formulation enhanced THC’s solubility, permeability, and stability, supporting its potential for effective topical psoriasis treatment. Future studies will focus on in situ gel incorporation and in vivo validation.

The developed formulation significantly improves the solubility and permeability of tetrahydrocurcumin which leads to improved therapeutic effectiveness in the formulation for the treatment of psoriasis. Further studies will incorporate these niosomes in in situ gels for the application.