Journal of Applied Pharmaceutical Research (JOAPR)
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Neuroprotective insights into Agave cantala: dual modulation of neuroinflammation and oxidative stress by phytochemicals through integrated in silico and in vitro approaches
Get PDFBackground: Neurodegenerative disorders such as Alzheimer’s and Parkinson’s are strongly associated with chronic neuroinflammation and oxidative stress. Phytochemicals from medicinal plants offer promising multitarget therapeutic potential. Objective: This study evaluated the dual therapeutic activity of phytochemicals from Agave cantala in modulating neuroinflammatory and oxidative stress pathways. Methodology: Bioactive compounds were identified using GC-MS, focusing on delphinidin, tigogenin, Agavasaponin_H, and Agavasaponin_E. Molecular docking was performed to assess their binding affinity toward inflammatory cytokines TNF-α and IL-6. In vitro anti-inflammatory activity was evaluated in LPS-stimulated RAW 264.7 macrophages by measuring TNF-α and IL-6 levels. Antioxidant activity was assessed through DPPH, ABTS, and FRAP assays. Results and Discussion: Docking studies revealed strong interactions of delphinidin and tigogenin with TNF-α and IL-6, suggesting effective inhibition. In vitro, delphinidin reduced TNF-α and IL-6 production by up to 81% and 75%, respectively, in a dose-dependent manner. Tigogenin and the saponins also showed notable cytokine suppression. The Agave cantala extract exhibited significant antioxidant activity, achieving 78.3% radical scavenging in the DPPH assay at 100 μg/mL. These results indicate that the identified phytochemicals modulate key inflammatory and oxidative pathways, supporting their multitarget action. Conclusion: The integrated in silico and in vitro data highlight Agave cantala phytochemicals, especially delphinidin and tigogenin, as promising candidates for managing neuroinflammation and oxidative stress. Further in vivo validation and pharmacokinetic profiling are recommended to support their clinical potential
Phytochemical analysis, antioxidant potential, and cytotoxic activity of extracts of Quisqualis indica L.
Get PDFBackground: The present study investigates the antioxidant and cytotoxic potential of the 50% hydroalcoholic extract of Quisqualis indica leaves. Methodology: Phytochemical screening was conducted to determine the presence of phenolics and flavonoids. TPC and TFC were analyzed using the Folin–Ciocalteu method and the aluminum chloride colorimetric assay, respectively. The antioxidant activity was evaluated through the DPPH radical scavenging assay at concentrations ranging from 10 to 100 µg/mL. Cytotoxicity was assessed in A549 human lung carcinoma cells using the MTT assay with extract concentrations from 0 to 1000 µg/mL. Results and Discussion: Phytochemical analysis confirmed the presence of phenolics and flavonoids, with total phenolic content measured as 9.25 ± 0.081 mg gallic acid equivalents (GAE)/g 50% hydroalcoholic extract and total flavonoid content as 4.33 ± 0.24 mg quercetin equivalents (QE)/g 50% hydroalcoholic extract. Antioxidant activity was assessed using the DPPH radical scavenging assay across extract concentrations ranging from 10 to 100 μg/mL. The 50% hydroalcoholic extract exhibited a dose-dependent antioxidant effect with an IC50 value of 48.56 μg/mL. Cytotoxicity was evaluated against A549 human lung carcinoma cells using the MTT assay, with treatments administered at concentrations ranging from 0 to 1000 μg/mL. The extract demonstrated significant cytotoxicity with an IC50 value of 4.76 μg/mL. Conclusion: These findings suggest that Q. indica may serve as a potential source of bioactive compounds with antioxidant and anticancer activities, warranting further investigation through in vivo and mechanistic studies
Phytochemical profiling and antioxidant evaluation of root ethanol extract of Maesa indica (Roxb.) sweet
Get PDFBackground: Healing herbs have long been used in traditional medicine due to their therapeutic properties and rich content of bioactive molecules. Despite its traditional applications, research on the root part of Maesa indica is scarce. This study focuses on exploring the phytochemical composition and antioxidant potential of the ethanol extract of M. indica roots. Methodology: Secondary metabolites were identified using Liquid Chromatography–Quadrupole Time-of-Flight Mass Spectrometry (LC-Q-TOF-MS). Antioxidant activities were evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and the metal chelating activity assay. Quantification of total phenolic content (TPC) and flavonoids was also conducted. Results and Discussion: Preliminary phytochemical analysis revealed the presence of flavonoids, phenols, steroids, and saponins. LC-Q-TOF-MS profiling identified seven primary secondary metabolites. The root extract exhibited high phenolic content (380.91 ± 23.52 µg/mg) and moderate flavonoid concentration (114.21 ± 6.25 µg/mg). Antioxidant activity of root extract was demonstrated by DPPH radical scavenging showed strong activity (IC₅₀: 88.78 µg/mL) and moderate ferrous ion chelating activity (IC₅₀: 172.31 µg/mL), suggesting effective free radical neutralization. Conclusion: The findings highlight the root extract of M. indica as a promising source of natural antioxidants. Compared to previous studies on aerial parts of the plant, the root extract offers comparable or enhanced antioxidant capacity, suggesting its value in future pharmaceutical and nutraceutical formulation
Formulation and evaluation of a bifonazole-loaded chitosan-honey invasomal hydrogel for enhanced topical antifungal activity
Get PDFBackground: To develop a novel bifonazole-loaded chitosan-honey invasomal hydrogel to improve the drug's topical antifungal efficacy. In this formulation, invasomal vesicles, composed of phospholipids, ethanol, and terpenes, were utilized to enhance the penetration of bifonazole through the skin. Methodology: These invasomal carriers were incorporated into a chitosan-based hydrogel matrix, which provided structural stability and bioadhesive properties, allowing for better retention on the skin. Additionally, natural honey, known for its antibacterial and wound-healing properties, was included to enhance the therapeutic benefits of the hydrogel. Results & Discussion: Invasomes were prepared using soya phosphatidylcholine, ethanol (30% v/v), and d-limonene (0.5%) and then incorporated into a chitosan-honey gel matrix. Among the six formulations (IF1–IF6), IF5 showed optimal results, with 93.32% drug release over 12 hours, a viscosity of 6545 ± 26 cps, a pH of 6.85, and antifungal inhibition zones of 17 mm (Candida albicans) and 11 mm (A. flavus). The formulation was characterized in terms of its physical properties, including viscosity, gel strength, and spreadability, and evaluated for its drug entrapment efficiency, in vitro drug release profile, and ex vivo skin permeation. This study demonstrates a synergistic system enhancing skin permeation, drug retention, and antifungal efficacy. Conclusion: This formulation represents a promising alternative for the effective and patient-friendly treatment of superficial fungal infections, offering improved drug delivery, enhanced therapeutic efficacy, and a reduced dosing frequency
Evaluation of Allium sativum polysaccharides as an adjunct to metformin in streptozotocin induced diabetic rats
Get PDFBackground: Metformin is widely prescribed for the management of diabetes; prolonged intake of metformin at higher doses is often associated with several mild to severe side effects. In recent years, plant polysaccharides have been rigorously studied for their antidiabetic properties. In this study, the complementary effect of Allium sativum polysaccharides with metformin was investigated in STZ-induced Wistar rats. Methodology: The rats were divided into five groups (n=6): normal control, diabetic control, metformin-treated (100 mg/kg b.w.), and metformin + ASP (50 mg + 200, 100 mg/kg b.w.). For 28 days, FBG and body weight were monitored. After 28 days, the rats were euthanized, and liver function markers were measured. Results and Discussion: Compared with diabetic control, combination therapy with metformin (50 mg) and ASP (200 mg) resulted in a significant reduction in glucose levels from 324.09 ± 2.90 to 125.84 ± 3.37 mg/dL. Similarly, the combination of Met 50 mg + 100 mg ASP lowered FBG levels to 178.96 ± 3.53 mg/dL. The results of a 2-way ANOVA indicated a significant interaction between the row and column factors (F(16, 125) = 192.6, p < 0.0001). Both combination therapies led to an initial decrease in body weight by day 7, followed by a subsequent recovery by day 28. In liver function test, both the combination therapies reduced AST (p < 0.05) and ALP enzyme levels (p < 0.05). Conclusion: The investigated combination therapy showed antidiabetic activities by improving glucose metabolism and liver function in rats
Fabrication of levofloxacin-loaded ph-sensitive eudragit polymeric floating microballoon biomaterial for gastroretentive drug delivery
Get PDFBackground: The design of improved biomaterials for medication administration is vital in overcoming problems associated with standard therapy for Helicobacter pylori (H. pylori)-induced stomach ulcers. This study aims to develop and characterize floating biomaterial of levofloxacin microballoon biomaterials based on a fluoroquinolone-benzoxazine system conjugated with methylated piperazine and carboxylic acid groups, strategically designed for prolonged gastric delivery. Methodology: Using the emulsion solvent diffusion method, thirteen preparations were developed by different polymer ratios (pH-sensitive Eudragit RS-100 and Ethyl Cellulose), stirring speeds, and temperatures. Results and Discussion: In the buoyancy study simulated gastric fluid (pH 1.2), the best formulation (F9) shows superior encapsulation efficiency (90.2%) and sustained drug release profile (91.2% over 8 hours) that increases its effectiveness against H. pylori. FTIR and SEM analyses conducted during characterization studies verified the drug stability and the spherical microballoon morphology, with a particle size of 81.2 µm. Levofloxacin-loaded microballoon biomaterials provide a unique gastro-retentive delivery system that improves patient compliance, reduces off-target effects, and maintains effective drug concentrations at the infection site, thereby strengthening the therapeutic efficacy of levofloxacin against H. pylori. Conclusion: This creative method offers a viable substitute for traditional therapies for stomach ulcers and is consistent with the overarching objectives of targeted delivery systems and structure-based drug development
Applications of bioactive compounds of traditional Chinese medicine in breast cancer management
Get PDFBackground: Over the past few decades, the prevalence of breast cancer has been rapidly increasing, making it one of the most prevalent malignancies diagnosed in women globally. Traditional Chinese Medicine (TCM) has gained attention as a potential approach for managing breast cancer by boosting immune response, inhibiting cancer-related gene activity, and alleviating the adverse effects of radiotherapy and chemotherapy. TCM offers a valuable framework for therapeutic systems and scientific exploration that is widely practiced in many regions worldwide, primarily in China, Korea, and Japan. The herbal components of TCM exhibit complex biological activities that influence multiple aspects of cancer progression, including cell proliferation, programmed cell death (apoptosis), immune modulation, and tumor-host interactions. Methodology: A systematic literature review was conducted using peer-reviewed articles published between 2017 and 2024. Relevant data were collected from publicly available scientific databases. Non-English, Conference papers, and duplicate studies were excluded to ensure the inclusion of high-quality and relevant research findings. Result and Discussion: Analysis revealed that specific bioactive compounds in TCM exhibit significant anti-cancer effects. For example, ginsenoside Rg3 inhibited tumor growth by 45% in vivo, while curcumin reduced MDA-MB-231 breast cancer cell viability by 60% at 20 μM. Conclusion: The promise of TCM, especially its bioactive components and medicinal herbs in the treatment of breast cancer, is the main highlight of this paper. Additionally, it highlights the key scientific databases that provide critical insights into TCM research while exploring the therapeutic mechanisms of Chinese herbs and their bioactive components in mitigating breast cancer progression.
Chromatographic profiling of leniolisib impurities using HPLC and LC-MS/MS: degradation behaviour, structural characterization, and in-silico toxicity evaluation
Get PDFBackground: This study presents a comprehensive analytical investigation of leniolisib, focusing on impurity profiling, degradation kinetics, structural characterization, and in silico toxicity prediction of degradation products (DPs). Methodology: A systematic approach was employed to optimize the analytical method for leniolisib and its impurities, along with LC–MS/MS-based identification and in-silico toxicity prediction of DPs. Result and Discussion: Method optimized as Waters Symmetry C18 column and an isocratic mobile phase (methanol: sodium acetate buffer, 55:45 v/v) at 0.90 mL/min with UV detection at 229 nm. Leniolisib was most susceptible to acid and oxidative stress, resulting in 31.24% and 39.58% degradation, respectively. Pseudo-first-order kinetics was observed with rate constants of 0.0329 h⁻¹ (acidic) and 0.0414 h⁻¹ (oxidative), with half life of 21.08 h and 16.73 h. LC–MS/MS elucidates the identities of major DPs that enable the proposed degradation pathways. The MS/MS characterization confirms DP 1 with a formula of C13H15N5O with a mass of 257 g/mol, whereas DP 2, 3, and 4 were identified to have formulas of C20H26N6O2, C13H12F3N5O, and C17H19F3N6O with masses of 382, 311, and 380 g/mol, respectively. The In-silico toxicity predictions show DP 1 (LD₅₀ = 500 mg/kg) and DP 2 (729 mg/kg) as moderate toxicity (class 4), DP 4 shows the least toxicity (class 5, LD₅₀ = 1750 mg/kg), whereas DP3 shows the highest toxicity (class 3, LD₅₀ = 250 mg/kg). Conclusion: The developed method and accompanying data provide a critical foundation for routine quality control, stability testing, and regulatory submissions for leniolisib-based formulations
Development of abemaciclib-encapsulated nanosponges for breast cancer: optimization, drug release kinetics, and in vitro efficacy
Get PDFBackground: Abemaciclib (ABC) is a new, orally administered pharmaceutical agent authorised for the purpose of combating breast cancer. The drug's low bioavailability necessitates dosing two to three times daily, which may reduce patient compliance. To lessen the severity of side effects and prolong the duration of action, sustained-release formulations are required. Developing an ABC sustained-release nanoparticle system was the primary goal of this study. Methodology: Both the sustained-release polymer (EC) and the surfactant (KP-188) were derived from ethyl cellulose, in an emulsion-solvent diffusion synthesis of nanosponges (NS). We examined the impact of varying surfactant concentrations and drug-to-polymer ratios on PS, PDI, ZP, %EE, %DL, particle size, drug loading, zeta potential, and polydispersity index. Results and Discussion: The optimized formulation (F11) achieved an entrapment efficiency of 86.52±0.25% and a cumulative drug release of 77.12% over 24 hours. The drug release followed a sustained pattern over 24 hours. It best fits the Higuchi kinetic model, which indicates that drug diffusion was the primary mechanism of release from the matrix system. The MTT experiment demonstrated that ABC might be a viable cytotoxic nanocarrier for breast cancer cells from humans, specifically MCF-7 and MDA-MB-231. On top of that, following contact with storage settings of 25, 5, and 45 °C for six months, ABC maintained its drug release property with no modification in the percentage release. Conclusion: This study shows that the created NS could effectively transport and release ABC, amplifying its impact in the battle against breast cancer
In vitro anticancer potential of Manilkara hexandra (Roxb.) leaf methanolic extracts via SRB and MTT assays against MCF-7 cell line
Get PDFBackground: Cancer causes millions of deaths worldwide, with cases expected to reach 28.4 million by 2040. Natural plant compounds offer safer alternatives for cancer treatment. Aim: This study tested the anticancer activity of Manilkara hexandra leaf extracts against MCF-7 breast cancer cells. Materials and methods: Methanolic extraction, followed by sequential fractionation via column chromatography, yielded bioactive fractions that underwent phytochemical and GC-MS characterization. Quantification of cytotoxicity was performed using sulforhodamine B (SRB) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays across a concentration gradient (10–80 μg/mL). Result and Discussion: Chemical screening found alkaloids, flavonoids, tannins, and other bioactive compounds. The petroleum ether-ethyl acetate (PE-EA) fraction contained quercetin (25.28%) and another major flavonoid (28.62%). This fraction exhibited strong dose-dependent cell killing, reducing cell survival to 31.8% (SRB) and 33.0% (MTT) at 80 μg/mL (p < 0.001). The IC₅₀ was 55 μg/mL in both assays. Conclusion: The anticancer activity correlates with high flavonoid content, suggesting these compounds cause cell death through apoptosis or cell cycle arrest. M. hexandra PE-EA fraction shows promise as a natural anticancer agent for breast cancer treatmen