article · Pharmaceuticals
Epigallocatechin gallate, a green tea compound recognised for its anti-inflammatory, antioxidant, and anti-tumour properties, typically exhibits low oral bioavailability due to poor stability and limited membrane permeation. To resolve these challenges, the compound was formulated into nanospanlastics, which are flexible nanovesicles composed of surfactants and membrane-destabilising edge activators. Formulations prepared via an ethanol injection method were evaluated using a factorial design to examine entrapment efficiency, particle size, and drug release over twelve hours. Testing included laboratory characterisation, ex vivo intestinal permeation assays, and pharmacokinetic evaluations. The optimised nanospanlastic formulation exhibited significantly superior entrapment efficiency, stability, deformability, and intestinal permeability compared to conventional niosomes. Pharmacokinetic results further confirmed that the nanospanlastic system provided sustained drug release and markedly improved overall bioavailability compared to both niosomes and the unformulated compound.
Epigallocatechin gallate offers valuable anti-inflammatory, antioxidant, and anti-cancer properties, but poor absorption in the digestive tract has long restricted its practical therapeutic value. Demonstrating that nanospanlastics can enhance both stability and intestinal permeability offers a viable route to overcome these delivery barriers, helping to ensure that beneficial green tea polyphenols can reach target tissues at clinically meaningful levels.
This technology could enable pharmaceutical and nutraceutical manufacturers to develop higher-potency oral products containing green tea polyphenols. Based on the reported laboratory characterisation, ex vivo permeation assays, and pharmacokinetic data, the research is at an early, preclinical stage. Commercial translation would require subsequent toxicity assessments, clinical trials in humans, and scale-up of the ethanol injection manufacturing method to verify real-world efficacy.
AI-generated from the published abstract. Always read the original work before citing.
The present study aimed to investigate the potential of nanospanlastics for boosting the bioavailability of epigallocatechin gallate (EGCG). EGCG has valuable effects like anti-inflammation, anti-oxidation, and anti-tumorigenesis. Unfortunately, it has a low oral bioavailability due to its limited permeation and poor stability. To overcome these pitfalls, EGCG was fabricated as a nanospanlastic. Nanospanlastics are flexible nanovesicles that are composed of surfactants and edge activators (EAs). EAs improve the deformability of spanlastics by acting as a destabilizing factor of their vesicular membranes. EGCG-loaded spanlastics were prepared by an ethanol injection method, according to 2<sup>3</sup> factorial design, to explore the impact of different independent variables on entrapment efficiency (EE%), % drug released after 12 h (Q<sub>12h</sub>), and particle size (PS). In vitro characterization, ex vivo intestinal permeation test, and pharmacokinetic study of the optimized formula were performed. A newly developed RP-HPLC technique was adopted for the estimation of EGCG. The optimized formula (F4) demonstrated more prolonged drug release and a significant improvement in the EE%, permeability, deformability and stability than the corresponding niosomes. The pharmacokinetic study investigated that F4 had a more sustained drug release and a higher bioavailability than the conventional niosomes and free drugs. Nanospanlastics could be a promising approach for improving the bioavailability of EGCG.
This page summarises published work. The authoritative version sits with the publisher.
DOI: 10.3390/ph14010068
Is something wrong with this record? Report it or request removal.
Discussion
Have you built on this work, tried to replicate it, or seen it applied in practice? Share what you know. Verified researchers and MARATTO™ domain experts can open a discussion, and any member can reply. Contributions are reviewed before they appear.
No discussion yet. Open the first thread.
New to MARATTO™? Create a free account.
