Journal of Pharmaceutical Innovation最新文献

Background

The purpose of this study was to evaluate the antioxidant and antidiabetic activities of an ethanol extract of Hibiscus sabdariffa L. (EEHS) and to compare its topical anti-inflammatory activity to a cream formulated from the plant’s essential oil (EO).

Methods

Dried calices powder of the plant was subjected to ethanol extraction using a Soxhlet extraction apparatus. Total phenolic content and total anthocyanin content were assessed. The antioxidant activity was evaluated through a DPPH free radical scavenging assay. EEHS was studied for antidiabetic activity in streptozotocin induced diabetic rats by oral administration of the extract (300 mg/kg body weight) for 15 days. Blood glucose level was estimated and compared with Glucophage (500 mg). In order to understand the biological activity of H. Sabdariffa in the inflammatory response, cream of the EEHS and EO were formulated. Cream was made into oil in water base (O/W) containing 1% and 0.5% (m/m) concentration of EEHS and EO, respectively. An acute dermal irritation test on rabbits of the formulated creams was carried out. The topical anti-inflammatory effect of the creams formulated was determined by the croton oil-induced mouse ear edema test.

Results

EEHS containing polyphenolic and anthocyanin compounds exhibited antioxidant properties. The IC50 value of H. sabdariffa was found to be 0.221, indicating its potent inhibitory activity in the tested assay. EEHS at a dose of 300 mg/kg significantly reduced blood glucose levels in hyperglycemic rats from 333 ± 10.226 to 183.33 ± 10.345 mg/dL (P < 0.05 vs. diabetic control) after 14 days of treatment. This reduction was greater than that observed in the positive control group, with glucose reduction percentages of 44.94% and 22.96%, respectively, on day 14. Moreover, EEHS was observed to be non-toxic at doses up to 5 g/kg body weight. In acute inflammation, EEHS demonstrated greater efficacy than EO, achieving inhibition rates of 70% and 66.66%, respectively. The histological study of tissues obtained from mouse ears provided confirmation of the results obtained during this study.

Conclusion

The findings demonstrate that EEHS, rich in polyphenols and anthocyanins, exhibits significant antioxidant, antihyperglycemic, and anti-inflammatory properties along with a favorable safety profile - supporting its potential as a natural therapeutic agent.

Purpose

This study aimed to develop mucoadhesive polymeric nanoparticles of fexofenadine hydrochloride for ocular delivery to improve precorneal retention, corneal permeation, and therapeutic efficacy in allergic conjunctivitis. The work addressed limitations of conventional eye drops, including rapid elimination and poor bioavailability.

Methods

Nanoparticles were prepared using a modified nanoprecipitation method with Eudragit RL 100 and polyvinyl alcohol (PVA). Formulations were evaluated for particle size, PDI, zeta potential, entrapment efficiency, and morphology (SEM, DLS). In vitro release studies and kinetic modelling were performed to assess release behaviour. Mucoadhesion was measured via mucin binding, while ex vivo permeation across excised goat cornea assessed transcorneal transport. Hemolysis assays evaluated biocompatibility.

Results

The optimised formulation (F4) exhibited a particle size of 165.9 nm, PDI of 0.232, and zeta potential of −14.8 mV, with 71% entrapment efficiency. SEM confirmed spherical particles (91–97 nm in dry state), with DLS showing hydrated swelling to 215.6 nm. The formulation demonstrated sustained release (~90% in 6 h) following non-Fickian kinetics. Mucoadhesion was strong, with 84.10% mucin binding. Ex vivo studies revealed a permeability coefficient of 1.09 cm/h, nearly ten times higher than that of a pure drug solution. Hemolysis remained below 5%, confirming safety.

Conclusion

The developed mucoadhesive nanoparticulate system offers a promising platform for controlled and enhanced ocular delivery of fexofenadine hydrochloride, capable of improving drug retention and permeability. However, in vivo pharmacokinetic and therapeutic evaluations are warranted to confirm the ex vivo findings and establish clinical applicability.

Purpose

Diabetes mellitus (DM) remains a major global health concern, necessitating the development of novel therapeutics that overcome the limitations of existing treatments, such as insulin resistance, weight gain, and gastrointestinal side effects. This study aimed to explore the antidiabetic potential of soy-derived isoflavones through computational approaches, focusing on their inhibitory activity against aldose reductase (AR), a key enzyme implicated in DM-associated complications.

Methods

An integrative in-silico strategy was applied, combining gene expression profiling, molecular docking, molecular dynamics (MD) simulations, and quantum chemical analyses. The GSE30529 gene expression dataset was analyzed to assess AR (AKR1B1) expression in diabetic renal tissues. Molecular docking, MM/PBSA, and MM/PBSA analyses were used to evaluate the binding affinity and stability of isoflavone–AR complexes. Frontier molecular orbital (FMO) analysis and Molecular Electrostatic Potential (MEP) mapping were conducted to assess electronic reactivity and interaction potential.

Results

Gene expression analysis revealed significant upregulation of the AKR1B1 gene (LogFC = 0.85, p < 0.05) in diabetic conditions, confirming AR as a viable target. Among the isoflavones, genistein exhibited the strongest AR binding affinity (docking score − 9.1 kcal/mol; ΔG_binding − 20.56 kcal/mol), with MD simulations confirming its superior structural stability compared to the apo protein and reference compound. Glycitein displayed a narrow HOMO–LUMO gap (4.42 eV), indicating high electronic reactivity, consistent with MEP mapping results.

Conclusion

Computational findings suggest that soy isoflavones, particularly genistein and glycitein, as promising AR inhibitors. Further in-vitro, in-vivo, and clinical validation is warranted to confirm their efficacy in DM management.

Staphylococcus aureus (S. aureus) is an opportunistic pathogen, which is listed among bacteria of immediate concern by World Health Organization (WHO). Alternative treatment options are needed to control the infections caused by S. aureus because the level of antibiotic resistance has reached to the alarming level with the currently available treatment methods. Therefore, the current study was designed to check the antibacterial activity of anthraquinones i.e. citreorosein, emodin, physcion, emodin-1-O-β-D-glucoside, emodin-8-O-β-D-glucoside and physcion-8-O-β-D-glucoside extracted from Reynoutria japonica (R. japonica) against the clinical isolates of S. aureus. Antibacterial activity of the isolated compounds was determined using minimum inhibitory concentration (MIC) method. Among all anthraquinones, citreorosein, emodin and physcion displayed the promising growth inhibitory activity against Methicillin Sensitive S. aureus (MSSA) and Methicillin Resistant S. aureus (MRSA). In addition, a molecular docking study revealed high binding ability of citreorosein and emodin to the active site of DNA gyrase protein of the bacteria. Furthermore, we checked the major and minor constituents in roots R. japonica and revealed that the most potent compounds were the major constituents. These findings advance our knowledge of R. japonica potential as a functional food and popular herbal remedy.

Acne vulgaris is a common inflammatory skin condition marked by comedones, pimples, and cysts across various age groups. Tretinoin is widely used in topical therapy because it regulates keratinocyte turnover and reduces inflammation, but its utility is restricted by poor penetration, instability, and irritation. This study focused on developing a tretinoin-loaded nanoemulsion to address these drawbacks and improve therapeutic performance. The formulation used tea tree oil as the oil phase, Tween 80 as the surfactant, and PEG 400 as the co-surfactant, prepared through high-energy emulsification. It was evaluated for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, drug release, and skin permeation. Biological assessments included antibacterial activity against Propionibacterium acnes and Staphylococcus epidermidis, along with anti-inflammatory testing using lipopolysaccharide-induced keratinocyte inflammation. The nanoemulsion achieved a mean droplet size of 103.25 ± 0.11 nm and a PDI of 0.234 ± 0.08, indicating uniformity. A zeta potential of − 18 mV suggested adequate stability. In vitro analyses showed sustained drug release and higher permeation than conventional tretinoin solution. The system exhibited strong antibacterial action and decreased cytokine production, confirming anti-inflammatory potential. Overall, the nanoemulsion enhanced stability, minimized irritation, and demonstrated promise as a safer and more effective topical therapy for acne vulgaris.

Graphical Abstract

Purpose

Poly(lactic‑co‑glycolic acid) (PLGA) nanoparticles are widely used for cancer drug delivery. Co‑encapsulation of agents with complementary mechanisms can improve efficacy at tolerated doses. We evaluated PEGylated PLGA nanoparticles co-loading doxorubicin and capsaicin for activity against breast cancer cells.

Methods

Nanoparticles were prepared by double emulsion, characterized by size and zeta potential, and assessed for drug loading and release. Cytotoxicity was measured in MCF‑7 cells. In silico work combined molecular docking to the BRCA1 BRCT domain with 100 ns molecular dynamics simulations (MDS) and MM‑GBSA free‑energy analysis to examine complex stability and binding energetics.

Results

The co‑loaded nanoparticles measured 207 ± 1 nm with an anionic surface (−20.7 mV). Encapsulation efficiencies were 69.65% for doxorubicin and 27.42% for capsaicin in the co‑loaded formulation. Release showed an initial burst followed by sustained diffusion. The co‑loaded nanoparticles reduced MCF‑7 viability more than free drug, with IC₅₀ 3.4 µg/mL versus 5.7 µg/mL for free doxorubicin, and combination index values indicated synergy. Docking predicted favorable binding to BRCA1. MDS showed stable complexes with backbone RMSD ~1.2–1.5 Å, persistent hydrogen bonding, and compact protein geometry. MM‑GBSA gave a favorable overall binding free energy (ΔG_bind = −74.25 ± 5.41 kcal/mol).

Conclusion

Co‑encapsulation of doxorubicin and capsaicin in PEGylated PLGA nanoparticles yields stable nanostructures with controlled release, synergistic cytotoxicity in MCF‑7 cells, and in silico evidence of stable interaction with the BRCA1 BRCT domain. These data support further preclinical evaluation.

Purpose

Mangiferin, a naturally occurring polyphenol, possesses remarkable antioxidant and anticancer properties. However, its therapeutic potential is hindered by its low and variable bioavailability. The present research work deals with the formulation and evaluation of mangiferin-loaded niosomes for breast cancer treatment, optimization using 3² factorial design, with particle size and entrapment efficiency as key responses.

Methods

All the batches of niosomes were prepared using thin film hydration methods and particle size, entrapment efficiency and cumulative drug release were determined. The optimized batch (F9) was characterized for SEM, XRD, FTIR, DSC, ex vivo permeability, in vivo pharmacokinetics and cytotoxicity.

Results

The F9 batch showed niosomal size of 221 nm, zeta potential of -40.0 mV, entrapment efficiency of 89.5%, PDI of 0.227. Percent cumulative drug release in pH 6.8 medium revealed that 80.65% of the drug was released within 24 h. Ex vivo intestinal permeability study indicated better permeation of mangiferin- loaded niosomes than pure drug. In vivo pharmacokinetic studies via the oral route indicated a 6.66-fold increase in Cmax and a 9.67-fold increase in AUC for mangiferin-loaded niosomes compared to pure drugs. Mangiferin-loaded niosomes were found to be 10.53 times more cytotoxic than pure drug on MCF-7 cell lines.

Conclusion

The findings suggest that mangiferin-loaded niosomes significantly enhance the anticancer activity of mangiferin highlighting their potential as an effective approach for breast cancer treatment.

Background

Liver diseases include a variety of pathological conditions affecting hepatic tissues, structures, and cellular components. Livopick, is claimed to possess hepatoprotective activity and is used in treating various liver conditions; however, scientific evidence supporting its efficacy is currently lacking. So, the study was designed to evaluate the hepatoprotective potential of the Livopick polyherbal formulation in treating acute experimental liver damage in albino Wistar rats caused by carbon tetrachloride.

Methods

Wistar rats were divided into various groups: standard control silymarin (100 mg/kg), Livopick high dose 150 mg/kg, and low dose 100 mg/kg, at a dose of 1 ml/kg CCl₄ administered orally by diluting with a 1:1 mixture of liquid paraffin on the day 9th of treatment to induce hepatotoxicity. Hepatic markers serum levels (ALT, ALP, AST, Total and direct bilirubin) also tissue antioxidant enzymes (GSH, CAT, SOD) were evaluated. Liver tissue histopathological analysis was conducted.

Results

CCl₄showed significant rise in serum ALT, ALP, AST, and bilirubin levels, with a marked reduction in the antioxidant enzyme activity. Pre-treatment with Livopick at both doses significantly restored the biochemical parameters. The higher dose of Livopick has shown to be comparable to silymarin. Histopathological analysis demonstrated the preservation of hepatic structure in the Livopick-treated group.

Conclusion

Livopick showed significant hepatoprotective activity against CCl₄-induced liver injury, because of antioxidant mechanisms which supports its potential as a therapeutic polyherbal formulation.

Graphical Abstract