Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System

Abstract

Luteolin (LUT) is a natural pharmaceutical compound that is weakly water soluble and has low bioavailability when taken orally. As a result, the goal of this research was to create self-nanoemulsifying drug delivery systems (SNEDDS) for LUT in an attempt to improve its in vitro dissolution and hepatoprotective effects, resulting in increased oral bioavailability. Using the aqueous phase titration approach and the creation of pseudo-ternary phase diagrams with Capryol-PGMC (oil phase), Tween-80 (surfactant), and Transcutol-HP (co-emulsifier), various SNEDDS of LUT were generated. SNEDDS were assessed for droplet size, polydispersity index (PDI), zeta potential (ZP), refractive index (RI), and percent of transmittance (percent T) after undergoing several thermodynamic stability and self-nanoemulsification experiments. When compared to LUT suspension, the developed SNEDDS revealed considerable LUT release from all SNEDDS. Droplet size was 40 nm, PDI was <0.3, ZP was −30.58 mV, RI was 1.40, percent T was >98 percent, and drug release profile was >96 percent in optimized SNEDDS of LUT. For in vivo hepatoprotective testing in rats, optimized SNEDDS was chosen. When compared to LUT suspension, hepatoprotective tests showed that optimized LUT SNEDDS had a substantial hepatoprotective impact. The findings of this investigation suggested that SNEDDS could improve bioflavonoid LUT dissolution rate and therapeutic efficacy.

Product Development Studies of Cranberry Seed Oil Nanoemulsion

“…The nanotechnology provides a prodigious opportunity to folklore medicines in order to improve their efficacy and delivery potentials [9,10]. Oil-in-water (O/W) NEs are safe and offer several advantages including encapsulation of delicate hydrophobic molecules, their controlled release, good skin penetration, prevent drug degradation, improved stability and bioavailability, and low-cost manufacturing [9][10][11][12][13]. CSO can be investigated as a possible candidate for skin diseases based on its profile of high-value chemicals and nutrients.…”

Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Apremilast: In Vitro Evaluation and Pharmacokinetics Studies

“…The ZP values were negative for all formulations, F3 = −11.2, F4 = −17.4, F7 = −20.55, F8 = −17.65 and F9 = −13.35 mV, which was due to the composition of (o/w) APR-SNEEDS that presented the negatively charged molecules at the surface, due to the presence of the fatty acid esters in Lauraglycol-FCC (oil phase). The negative charges created repulsive forces between the nanoemulsion droplets, which reflected on the physical stability of the formulations in terms of the absence of droplets combination or phase separation that resulted in the clear and transparent appearances of the formulations [ 18 ]. The mean RI of the formulations was 1.340, which in the case of SNEDDS formulation meant that the formulation is of isotropic nature.…”

“…The lipid formulation approach appears as a promising approach that can be utilized for improving the solubility, dissolution properties and oral bioavailability of poorly soluble drugs [ 25 , 26 , 27 ]. SNEDDS were reported in many studies as the best formulation to solve the problems associated with class II, III and IV drugs, which have poor solubility or/and poor permeability, which affects their overall oral bioavailability [ 12 , 13 , 14 , 15 , 16 , 17 , 18 ]. This anhydrous formulation can rapidly form fine oil-in-water nanoemulsions upon dispersion in the gastrointestinal fluids under mild agitation imparted by the gastric motility [ 18 ].…”

“…SNEDDS were reported in many studies as the best formulation to solve the problems associated with class II, III and IV drugs, which have poor solubility or/and poor permeability, which affects their overall oral bioavailability [ 12 , 13 , 14 , 15 , 16 , 17 , 18 ]. This anhydrous formulation can rapidly form fine oil-in-water nanoemulsions upon dispersion in the gastrointestinal fluids under mild agitation imparted by the gastric motility [ 18 ]. Formation of submicron droplets upon dilution produce a large interfacial surface area for transfer of the drug, which may result in increased rate and extent of absorption and hence, improved bioavailability [ 12 ].…”

“…The marketed film coated immediate release tablets of APR Otezla ® have 20–33% bioavailability compared to APR absolute bioavailability of 73% [ 5 ]. On the other hand, many studies represented SNEDDS as promising delivery systems for pharmaceutical drugs due to their tremendous advantages in enhancing solubility, spontaneously occurring emulsification, and thermodynamic and kinetic stabilities [ 12 , 13 , 14 , 15 , 16 , 17 , 18 ]. The aim of the present study was to create and optimize SNEDDS of APR to increase its solubility and dissolution rate, which sequentially will upgrade the extent of the oral bioavailability and therapeutic efficacy of the drug.…”