Self-nanoemulsifying drug delivery system (SNEDDS) of the poorly water-soluble grapefruit flavonoid Naringenin: design, characterization,in vitroandin vivoevaluation

Abstract

(2015) Self-nanoemulsifying drug delivery system (SNEDDS) of the poorly water-soluble grapefruit flavonoid Naringenin: design, characterization, invitro and invivo evaluation, Drug Delivery, 22:4, 552-561, DOI: 10.3109/10717544.2013 Abstract Naringenin (NRG), predominant flavanone in grapefruits, possesses anti-inflammatory, anti-carcinogenic, hepato-protective and anti-lipid peroxidation effects. Slow dissolution after oral ingestion due to its poor solubility in water, as well as low bioavailability following oral administration, restricts its therapeutic application. The study is an attempt to improve the solubility and bioavailability of NRG by employing self-nanoemulsifying drug delivery technique. Preliminary screening was carried out to select oil, surfactant and co-surfactant, based on solubilization and emulsification efficiency of the components. Pseudo ternary phase diagrams were constructed to identify the area of nanoemulsification. The developed selfnanoemulsifying drug delivery systems (SNEDDS) were evaluated in term of goluble size, globule size distribution, zeta potential, and surface morphology of nanoemulsions so obtained. The TEM analysis proves that nanoemulsion shows a droplet size less than 50 nm. Freeze thaw cycling and centrifugation studies were carried out to confirm the stability of the developed SNEDDS. In vitro drug release from SNEDDS was significantly higher (p50.005) than pure drug. Furthermore, area under the drug concentration time-curve (AUC 0-24 ) of NRG from SNEDDS formulation revealed a significant increase (p50.005) in NRG absorption compared to NRG alone. The increase in drug release and bioavailability as compared to drug suspension from SNEDDS formulation may be attributed to the nanosized droplets and enhanced solubility of NRG in the SNEDDS.

Cancer prevention and therapy through the modulation of the tumor microenvironment

“…A NRG glucuronide have same affinity for human serum albumin as naringenin. Efforts are in way to increase the bioavailability through various techniques like combining NRG with β-cyclodextrin through solid dispersion and self nano emulsifying drug (SNEDDS) technique [373]. The mixture and nanoparticles enhanced a significant increase in NRG absorption compared to NRG alone.…”

The impact of phytochemicals present in the diet on microbial signalling in the human gut

“…While grapefruit has been linked to a number of potential health benefits, it is also known to interfere significantly with the pharmacokinetics of over 85 prescription medications. This grapefruit-drug mediated interaction is believed to occur through the interference of furanocoumarins which are present in grapefruit juice with a cytochrome P450 metabolising enzyme called CYP3A4 (Bailey, Dresser, & Arnold, 2013;Khan, Kotta, Ansari, Sharma, & Ali, 2014;Pirmohamed, 2013). Furanocoumarins share some structural properties such as a "furan" moiety with halogenated furanones, which are a class of natural compounds capable of inhibiting AHL based bacterial signalling.…”

Phytobioactive compound-based nanodelivery systems for the treatment of type 2 diabetes mellitus – current status

“…The enhanced bioavailability of naringenin was most likely due to its higher solubility through self-emulsion nanodelivery systems, which can improve its therapeutic application. 186 Naringenin-loaded NPs were prepared with a mean particle size of ~66 nm, and these showed a higher bioavailability through oral delivery, thereby improving its hepatoprotective activity in rat models. 187 Similarly, naringenin-loaded solid lipid NPs were constructed with particle sizes ranging from ~60 to 80 nm, and these showed a higher cellular uptake.…”