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.
Highlights
Of the spanlastic formulations containing entrapped Epigallocatechin gallate (EGCG) or the equivalent concentration of EGCG dispersion were introduced in the donor chamber over the cellulose membrane; 200 μL aliquots were withdrawn at the predetermined time intervals and substituted by an equal volume of fresh buffer solution to preserve a constant volume of the receptor medium [77]
EGCG-loaded spanlastic and the niosomal formulations were evaluated with regard to their entrapment efficiency of EGCG within the SNVs (EE)%, drug content, Q12h, % drug permeated, and deformability index (DI) to investigate the influence of storage conditions on the stability of both formulations
The current study demonstrated the preparation of EGCG-loaded spanlastics as an effective and flexible nanocarrier for improving the bioavailability of EGCG
Summary
Using different formulation strategies for encapsulating EGCG is considered an efficient approach to combat these shortcomings [1,14,15] The nanovesicular systems, such as liposomes and niosomes, are comprised of polar and non-polar parts; they could entrap both hydrophilic and lipophilic drugs. Song et al [14] explored that the niosomal formulations of (+) catechin and (−) EGCG exhibited higher stability, improved absorption, and lower toxicity than the free drug. These conventional carriers have a non-flexible nature and lack deformability during passage through different biological membranes [18]. The current study aimed to enhance the oral bioavailability of EGCG by encapsulation into spanlastic nanocarriers
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