Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

Abstract

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 23 factorial design, to explore the impact of different independent variables on entrapment efficiency (EE%), % drug released after 12 h (Q12h), 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.

Zolmitriptan Intranasal Spanlastics for Enhanced Migraine Treatment; Formulation Parameters Optimized via Quality by Design Approach

“…Moreover, the optimized formula showed a PDI of 0.685 and a ZP of −28.0 mV. The PDI value suggests the reasonable homogeneity of the formulation [33]. Zeta potential value predicts vesicular stability [35].…”

“…This is due to the unsaturation of the alkyl chain, allowing chain bending and results in a smaller size. Additionally, a high Tween 80 concentration reduces the interfacial tension, causing particle portioning [33].…”

“…Vesicles have a well-defined spherical shape with defined boundaries, which is related to the amphiphilic nature of the non-ionic surfactants. Non-ionic surfactants tend to develop spherical vesicles, which decrease the surface-free energy [33].…”

Formulation of Chitosan-Coated Brigatinib Nanospanlastics: Optimization, Characterization, Stability Assessment and In-Vitro Cytotoxicity Activity against H-1975 Cell Lines

“…Nanovesicles (liposomes and niosomes) can be used for the treatment of cancer with excellent results. It can also improve the stability of encapsulated drugs [ 15 , 16 ]. These conventional carriers, on the other hand, are rigid and lack deformability while passing through biological membranes.…”

“…Nanospanlastics (NSPs) are flexible nanovesicles that are non-immunogenic, biodegradable, and harmless. They’re also more chemically stable than conventional liposomes [ 16 ]. For these reasons, several studies are focusing on the use of NSPs formulations as a promising delivery system in preference to the conventional nanovesicles.…”