Pharmaceutical technological trends containing flavonoids: a patent review

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 17(3), P. 363 - 379

Published: Jan. 21, 2025

Flavonoids such as silibinin, hesperetin, and phloretin exhibit well-documented biological activities, including anti-inflammatory, cytoprotective, anticarcinogenic, antioxidant effects. However, their clinical application remains limited due to challenges poor aqueous solubility, low bioavailability, restricted intestinal absorption, which can significantly reduce pharmacological efficacy. This review analyzed patents related innovative pharmaceutical technologies for flavonoids. The analysis used databases from the World Intellectual Property Organization European Patent Office. Following a comprehensive screening process, 38 were selected detailed examination. These highlighted numerous studies on novel formulations, characterizations, proprietary conditions. highlights technologies, nanocapsules, nanoemulsions, solid dispersions, phospholipid carriers, inclusion complexes, microemulsions, other advanced systems, enhance bioactive molecules' water solubility stability. Consequently, these improve permeability absorption through intended administration route, demonstrating potential of flavonoids promising candidates various treatments, particularly when integrated into technologies.

Language: Английский

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A review of the current status of biological effects of plant-derived therapeutics in breast cancer

Molecular Biology Reports, Journal Year: 2025, Volume and Issue: 52(1)

Published: Jan. 24, 2025

Language: Английский

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Unlocking the Neuroprotective Potential of Silymarin: A Promising Ally in Safeguarding the Brain from Alzheimer’s Disease and Other Neurological Disorders

Molecular Neurobiology, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 17, 2025

Language: Английский

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Micelle silymarin supplementation to sows’ diet from day 109 of gestation to entire lactation period enhances reproductive performance and affects serum hormones and metabolites

Journal of Animal Science, Journal Year: 2021, Volume and Issue: 99(12)

Published: Nov. 26, 2021

The aim of the present study was to explore influences varying doses micelle silymarin (0%, 0.05%, 0.1%, and 0.2%) supplementation on sows' feed intake, milk yields, serum hormones, litter growth using 40 multiparous sows (Landrace × Yorkshire, parity from 3 5) 109th prenatal day 21st postnatal day. Each treatment included 10 each sow used as an experimental unit. On weaning day, weight gain were linearly improved (P < 0.01, both), corresponding increasing dose in diet. Also, weight, gain, average daily (ADG) piglets born treated exceeded 0.05) those offspring control (0% silymarin). Feed intake week 1, 2, entire lactation period increased (linear, P 0.01) increased. Body (BW) loss during reduced = 0.003) with amounts silymarin. Average yields also 0.002) sows, exceeding 0.046) that sows. uniform increases observed 0.037) fat content produced by 14 lactation. Epinephrine concentrations aspartate aminotransferase (AST) activity 21 postpartum declined 0.010) increased, both compared control. In addition, had higher superoxide dismutase (SOD) at parturition glutathione peroxidase (GSH-Px), lower oxidized (GSSG) concentrations, GSSG/GSH (glutathione) ratio (all, Moreover, silymarin-treated tended (0.05 <0.1) have catalase (CAT) total antioxidant capacity (T-AOC) concentrations. Taken together, results showed fed levels incremental dose-dependent effect diminished BW loss, greater weaning, 0.2% could be optimal achieve better effect.

Language: Английский

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Comparative efficacy of silibinin and nano-silibinin on lead poisoning in Male Wistar rats

Toxicology, Journal Year: 2022, Volume and Issue: 475, P. 153242 - 153242

Published: June 1, 2022

Language: Английский

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Fisetin-Loaded Nanostructured Lipid Carriers: Formulation and Evaluations against Advanced and Metastatic Melanoma

Molecular Pharmaceutics, Journal Year: 2023, Volume and Issue: 20(12), P. 6035 - 6055

Published: Oct. 31, 2023

Fisetin (Fis), a natural flavonoid with anticancer effects, suffers from delivery constraints. Fisetin-nanostructured lipid carriers (NLCs) were developed for better efficacy against metastatic melanoma, employing the design of experiment (DoE) approach. The optimized NLCs depict particle diameter 135.0 ± 5.5 nm, polydispersity index (PDI) 0.176 0.035, and an entrapment efficiency 78.16 1.58%. formulation was stable over period 60 days demonstrated sustained release drug (74.79 3.75%) 96 h. Fis-NLCs depicted at least ∼3.2 times lower IC50 value ∼1.8 higher uptake 48 h in A-375 B16F10 cells compared to that Fis. It also inhibited mobility melanoma induced cell cycle arrest G1/S phase. Reverse transcriptase polymerase chain reaction (RT-PCR) Western blot results show enhanced expression Nrf2/NQO1 genes apoptotic effect by upregulation BAX mRNA expression. protein levels p53 ∼2-fold pure In-vivo studies 5.9- 10.7-fold inhibition melanoma-associated metastasis lungs liver, respectively. outcomes this study as effective tool melanoma.

Language: Английский

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Preparation of silymarin-loaded zein polysaccharide core–shell nanostructures and evaluation of their biological potentials

Green Processing and Synthesis, Journal Year: 2024, Volume and Issue: 13(1)

Published: Jan. 1, 2024

Abstract Silymarin-loaded zein polysaccharide core–shell nanoparticles (SZPCS-NPs) were synthesized where sodium alginate and pectin offer stability controlled release qualities to zein, a maize protein, having excellent biocompatibility. The present study is an attempt develop zein–silymarin nanostructures enhance water solubility, thereby improving bioavailability producing enhanced biological responses in living systems. SZPCS-NPs prepared using pH-induced antisolvent precipitation method. Five different types of combinations pectin, namely P100–A00 (non-uniform size ranging from 20 100 nm), P70–A30 (spherical uniform measuring approximately 80 nm diameter), P50–A50, P30–A70, P00–A100 exhibited irregular shapes with the presence some triangular oval structures non-uniform nm. possessed best results terms shape, size, other characterization studies. Furthermore, percent drug loading 72.5% entrapment efficiency 51.7%, respectively. resulting relative percentage 97.4% comparison commercial silymarin, 58.1%, crude 46.97% percentage, correspondingly. In addition, almost two folds’ increase antioxidant activity commercially available silymarin. Similarly, also showed better stabilization hepatic biomarker enzymes hepatoprotective for period 6 weeks, contrast silymarin formulations.

Language: Английский

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Biological Activities, Pharmacokinetics and Toxicity of Nootkatone: A Review

Mini-Reviews in Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 22(17), P. 2244 - 2259

Published: Feb. 14, 2022

Abstract: Plant-based drugs have a significant impact on modern therapeutics due to their vast array of pharmacological activities. The integration herbal plants in the current healthcare system has emerged as new field research. It can be used for identification novel lead compound candidates future drug development. Nootkatone is sesquiterpene derivative and an isolate grapefruit. Shreds evidence illustrate that nootkatone targets few molecular mechanisms exhibit its activity yet needs more exploration established. review related nootkatone, drafted through literature search using research articles books from different sources, including Science Direct, Google Scholar, Elsevier, PubMed, Scopus. been reported possess wide range activities such anti-inflammatory, anticancer, antibacterial, hepatoprotective, neuroprotective, cardioprotective. Although preclinical studies experimental animal models suggest therapeutic potential, it further warranted evaluate toxicity pharmacokinetic parameters before being applied humans. Hence present review, we summarized scientific knowledge with particular emphasis properties encourage researchers clinical settings.

Language: Английский

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OVERVIEW OF MITOXANTRONE-A POTENTIAL CANDIDATE FOR TREATMENT OF BREAST CANCER

International Journal of Applied Pharmaceutics, Journal Year: 2022, Volume and Issue: unknown, P. 10 - 22

Published: March 7, 2022

Anthraquinones are one of the popular classes aromatic compounds which possess potential anticancer properties by suppressing nucleic acid formation and proteins essential to survival cancerous cells. Mitoxantrone (MT) is an antibiotic antineoplastic agent belonging anthracycline class exhibit minimal incident drug resistance. It a synthetic drug, bound enzyme topoisomerase IIα inhibitor, intercalates DNA IIα, preventing re-ligations in strands fragmentation disruption repair. The expression this was used tumor cells marker because its key function cell proliferation. cleavable complex hypothesized damage may enhance apoptosis susceptibility mitoxantrone associated with II α protein lowered resistance breast cancer line lines inhibitors. MT ABC-transporter cancer, also designated be “Breast protein” (BCRP) it cycle non-specific anti-cancer P-glycoprotein substrate. Multiple major drawbacks can avoided reducing efflux from formulating using lipophilic carriers. This manuscript discusses about MT's source, chemistry, physicochemical properties, effects possible pathways, targeting inhibitor for therapy mechanism, Various Nano formulation development strategy, toxicity profile, few patents related information.

Language: Английский

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The Protective Effects of Silymarin on the Reproductive Toxicity: A Comprehensive Review

Current Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 30(39), P. 4421 - 4449

Published: Jan. 31, 2023

Abstract: The reproductive system is extremely vulnerable to chemotherapy drugs, ionizing radiation, toxic heavy metals, chemicals, and so on. These harmful stimuli are able induce oxidative damage, apoptosis, inflammation, other mechanisms in the organs, leading different adverse effects. It was shown that using medicinal plants (medicinal herbs) can be an effective medication for prevention treatment of multiple health conditions. Silymarin a herb extract, obtained from seeds Silybum marianum. This herbal agent nontoxic even at relatively high physiological dose values, which suggests it safe use diseases. hepato-, neuro-, cardio- nephro-protective effects silymarin have been assessed previously. protective activities point anti-oxidant, anti-apoptotic, anti-inflammatory, anti-fibrotic, immunomodulatory, membrane-stabilizing properties. In this review, we aim summarize current studies on potentials against toxicity. molecular protection cellular toxicity also studied. Moreover, findings improved formulations delivery systems addressed.

Language: Английский

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