Unraveling the Impact of Stabilizers on Nanocrystal Preparation and Oral Absorption: A Case Study of Poorly Soluble Andrographolide DOI

Bingwen Ding,

Zhenting Zheng,

Jianjia Su

et al.

Nano Letters, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 23, 2024

Drug nanocrystal engineering is an attractive pharmaceutical approach to enhancing the oral bioavailability of poorly soluble drugs. The mechanism drug stabilization, however, unclear. Here we developed andrographolide nanocrystals (AG-NCs) with various nonionic surfactants (Pluronic-F127, TPGS, or Brij-S20). We detected AG micelles (AG-MCs) at surfactant ratio 10:10 (w/w) and poor AG-NC size stability. thus quantified unbound Pluronic-F127 in AG-NCs found that proposed instantaneous binding rate sharply declined increasing input. determined saturation dose TPGS on was approximately recommend it as a key criterion for formulation. Although exhibited marginally faster dissolution rate, they possessed better mucus-penetrating transmembrane transport capacities significantly enhanced absorption compared AG-MCs. These findings give insights into impact stabilizer during preparation process nanocrystals.

Language: Английский

Luteolin: exploring its therapeutic potential and molecular mechanisms in pulmonary diseases DOI Creative Commons

Jialian Lv,

Xinyue Song,

Zixin Luo

et al.

Frontiers in Pharmacology, Journal Year: 2025, Volume and Issue: 16

Published: Feb. 12, 2025

Luteolin is a flavonoid widely found in plants, including vegetables, botanical drugs, and fruits. Owing to its diverse pharmacological activities, such as anticancer, oxidative stress protection, anti-inflammatory, neuron-preserving effects, luteolin has attracted attention research medicine. exhibits therapeutic effects on various pulmonary disease models through multiple molecular mechanisms; these include inhibition of activation the PI3K/Akt-mediated Nuclear Factor kappa-B (NF-κB) MAPK signaling pathways, well promotion regulatory T cell (Treg) function enhancement alveolar epithelial sodium channel (ENaC) activity (alleviating inflammation responses). chronic obstructive (COPD), acute lung injury/acute respiratory distress syndrome (ALI/ARDS), fibrosis, allergic asthma, cancer. Luteolin, naturally occurring polyphenol, poorly water-soluble. The oral route may be ineffective because gut absorbs this type flavonoid. Therefore, although significant biological activity, clinical application limited by challenges associated with poor water solubility low bioavailability, which are critical factors for efficacy application. These can addressed modifying chemical structure enhancing pharmaceutical formulations. We summarized advancements improving bioavailability luteolin, diseases their related mechanisms, aim providing new ideas researchers.

Language: Английский

Citations

1
Linarin attenuates hyperuricemic nephropathy by modulating Nrf2/Keap1 and TLR4/NF-κB signaling pathways DOI Creative Commons

Yongshuai Qian,

Tao Zhang, Yue Chen

et al.

Phytomedicine, Journal Year: 2025, Volume and Issue: 139, P. 156440 - 156440

Published: Jan. 29, 2025

Language: Английский

Citations

0
Thesium Chinense Turcz. and Its Compound Astragalin Alleviate Lipopolysaccharide-Induced Acute Lung Injury via the PI3K/AKT/p53 Signaling Pathway DOI
Haonan Xu,

Fang Zhang,

Che Yan

et al.

Journal of Ethnopharmacology, Journal Year: 2025, Volume and Issue: unknown, P. 119691 - 119691

Published: March 1, 2025

Language: Английский

Citations

0
Effective Approaches to Improve the Anti-Hyperuricemia Ability of Plant Polyphenols: A Review DOI
Jun Li, Peng Wu, Jing Wang

et al.

Food Reviews International, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 21

Published: Oct. 21, 2024

Accumulating evidence suggested that polyphenols exhibited significant anti-hyperuricemia properties. However, multiple studies indicated processing technologies caused the loss of in plant materials, thereby reducing their bioactivities. Herein, on beneficial effects effect were collected. Furthermore, mechanisms promoted explored. Structure-activity relationships analysis showed hydroxyl groups and C2=C3 double bond for activity. Conversely, glycosylation was a disadvantage to activity polyphenols. Moreover, improving ability through appropriate is promising approach. Thermal treatment chemical conversion increased effective polyphenol content. Fermentation enzymatic bioconversion Ultrasound regulated by impacting oxidase affecting dissolution rate state Encapsulation enhanced bioavailability, stability, solubility Thus, possible ways enhance as follows: (1) Increasing content; (2) Promoting biological polyphenols; (3) Enhancing

Language: Английский

Citations

0
Unraveling the Impact of Stabilizers on Nanocrystal Preparation and Oral Absorption: A Case Study of Poorly Soluble Andrographolide DOI

Bingwen Ding,

Zhenting Zheng,

Jianjia Su

et al.

Nano Letters, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 23, 2024

Drug nanocrystal engineering is an attractive pharmaceutical approach to enhancing the oral bioavailability of poorly soluble drugs. The mechanism drug stabilization, however, unclear. Here we developed andrographolide nanocrystals (AG-NCs) with various nonionic surfactants (Pluronic-F127, TPGS, or Brij-S20). We detected AG micelles (AG-MCs) at surfactant ratio 10:10 (w/w) and poor AG-NC size stability. thus quantified unbound Pluronic-F127 in AG-NCs found that proposed instantaneous binding rate sharply declined increasing input. determined saturation dose TPGS on was approximately recommend it as a key criterion for formulation. Although exhibited marginally faster dissolution rate, they possessed better mucus-penetrating transmembrane transport capacities significantly enhanced absorption compared AG-MCs. These findings give insights into impact stabilizer during preparation process nanocrystals.

Language: Английский

Citations

0