(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.
There is lot of confusion in the literatures regarding the method of production of nanoemulsion. According to some authors, only the methods using high energy like high-pressure microfluidizer or high-frequency ultra-sonic devices can produce actual nanoemulsions. In contrast to this concept, one research group reported for the first time the preparation of nanoemulsion by a low-energy method. Later on many authors reported about the low-energy emulsification method. The purpose of this work is to formulate, evaluate and compare nanoemulsions prepared using high-energy as well as low-energy method. Nanoemulsions formulated were based on the phase inversion composition technique (low energy method) and were selected from the ternary phase diagram based on the criterion of their being a minimum concentration of S(mix) used in the formulation. For high-pressure homogenization method (high energy method) Design-Expert software was used, and the desirability function was probed to acquire an optimized formulation. No significant difference (p > 0.05) was observed in the globule size of formulations made by each method, but the value of poly-dispersibility index between the two methods was found to be extremely significant (p < 0.001). A very significant difference (p < 0.001) was observed in the drug release from formulations made by each method. More than 60% of the drug was released from all the formulations in the initial 2 h of the dissolution study.
Low-energy emulsification techniques can also produce stable nanoemulsions. It is guaranteed that oral nanoemulsions can act as a potential tool for the delivery of poorly water-soluble therapeutic moieties in a very efficient manner.
The ability of SNEDDS to present the drug in single unit dosage form either as soft or hard gelatin capsule with enhanced solubility maintaining the uniformity of dose is unique. With the ease of large-scale production, high drug-loading capacity, improvement in release behavior of poorly water-soluble drugs and improvement of oral bioavailability, SNEDDS have emerged as preferable system for the formulation of drug compounds with bioavailability problems due to poor aqueous solubility.
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