Lignin‐Containing Self‐Nanoemulsifying Drug Delivery System for Enhance Stability and Oral Absorption of trans‐Resveratrol

Abstract

Self‐nanoemulsifying drug delivery system (SNEDDS) is recently studied for enhancing the bioavailability of hydrophobic drugs, such as resveratrol (RSV). However, the functional design of SNEDDS for the drug structural protection is not studied yet. Here, this paper presents an efficient approach by adding lignin (a kind of abundant biomass resource) to enhance the stability of trans‐RSV and meantime improve its oral bioavailability. Higher stability of trans‐RSV (just decreased 2% to cis‐RSV after 1 h under direct sunlight) is observed after loaded by lignin‐containing SNEDDS (RSV/SLS SNEDDS). Low toxicity, high transfer efficiency (apparent permeability coefficient >1 × 10−7 cm s−1), and bioavailability (1.371%) of RSV/SLS SNEDDS is successfully demonstrated in Caco‐2 cells and rat model, respectively. This study serves to illustrate a simple, versatile, environmental, and economic sustainability approach to the development of nanodelivery systems for light instability drugs.

Recent Strategies in Resveratrol Delivery Systems

“…Various pharmacokinetic parameters revealed directly the enhanced adsorption rate of RSV SNEDDS. The AUC of the proposed formulation resulted in a 72‐fold increase in bioavailability and C max value rose considerably to 24 fold as compared to RSV suspended in water . Similarly, in vivo studies revealed a 5‐fold increase of the bioavailability of RSV encapsulated in solid lipidic nanoparticles compared to RSV suspension.…”

“…For example, the isomer degradation in the SNEDDS was evaluated inside and outside the dialysis bag. Interestingly, the results showed that SNEDDS greatly reduced the photochemical degradation of trans ‐RSV, whereas the amount released and degraded of RSV from free solution was 50–50 (Figure ), which may be due to the directly contact with light and oxygen …”

“…In contrast, Dai and co‐workers also designed a SNEDDS for RSV. The formulation was composed of sodium lignin sulfonate/Tween 80/PEG‐400 as mixed surfactants and olive oil . So‐formed spherical particles were 119±5 nm in diameter with a high ζ‐potential value of −22±1 mV.…”

“…2 times higher than from pure RSV solution) (Figure ). Thus, the proposed formulation contributed to improve the dispersion and dissolution of RSV in the gastroenteric environment …”

“…It is worth mentioning that a higher cumulative amount of RSV‐SNEDDS (composed of sodium lignin sulfonate/Tween 80/PEG‐400 as mixed surfactants and olive oil) was transported, from the apical‐to‐basolateral direction through Caco‐2 cells monolayers, than from pure RSV solution …”