4.4 Article

Nanosized nasal emulgel of resveratrol: preparation, optimization, in vitro evaluation and in vivo pharmacokinetic study

Journal

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Volume 45, Issue 10, Pages 1624-1634

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/03639045.2019.1648500

Keywords

Nano-emulgel; emulsion; brain targeting; resveratrol; pharmacokinetics

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Nano-emulgel has become one of the most significant controlled release systems, which has the advantages of both gels and nano-emulsions. This work aims at the formulation of nasal nano-emulgel for resveratrol, employing carbopol 934 and poloxamer 407 as the gelling agents. The optimum nano-emulsion was determined through further characterization of the selected system. The nasal nano-emulgel was prepared and tested for the in vitro release, the release kinetics, FTIR, ex vivo permeation, nasal mucosa toxicity, and in vivo pharmacokinetic study. The optimum nano-emulsion consisted of Tween 20, Capryol 90, and Transcutol at a ratio of (54.26: 23.81: 21.93%v/v), and it exhibited transmittance of 100%, resveratrol solubility of 159.9 +/- 6.4 mg/mL, globule size of 30.65 nm. The in vitro resveratrol released from nano-emulsion and nasal nano-emulgel was 96.17 +/- 4.43% and 78.53 +/- 4.7%, respectively. Ex vivo permeation was sustained during 12 h up to 63.95 +/- 4.7%. The histopathological study demonstrated that the formula is safe and tolerable to the nasal mucosa. C-max and AUC ((0-infinity)) of resveratrol obtained after nasal administration of nasal nano-emulgel was 2.23 and 8.05 times, respectively. Similarly, T-max was increased up to 3.67 +/- 0.82 h. The optimized nasal nano-emulgel established intranasal safety and bioavailability enhancement so it is considered as a well-designed system to target the brain.

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