Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University , Beni Suef , Egypt.
Department of Pharmaceutics and Clinical Pharmacy, Faculty of Pharmacy, Nahda University (NUB) , Beni Suef , Egypt.
Drug Dev Ind Pharm. 2019 Oct;45(10):1624-1634. doi: 10.1080/03639045.2019.1648500. Epub 2019 Aug 9.
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 release, the release kinetics, FTIR, permeation, nasal mucosa toxicity, and 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 resveratrol released from nano-emulsion and nasal nano-emulgel was 96.17 ± 4.43% and 78.53 ± 4.7%, respectively. 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 and AUC of resveratrol obtained after nasal administration of nasal nano-emulgel was 2.23 and 8.05 times, respectively. Similarly, T 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.
纳米乳凝胶已成为最重要的控释系统之一,它兼具凝胶和纳米乳的优点。本工作旨在开发白藜芦醇鼻用纳米乳凝胶,采用卡波姆 934 和泊洛沙姆 407 作为凝胶剂。通过对所选系统的进一步表征,确定了最佳的纳米乳。制备了鼻用纳米乳凝胶,并对其进行了释放、释放动力学、FTIR、渗透、鼻黏膜毒性和药代动力学研究。最佳的纳米乳由 Tween 20、Capryol 90 和 Transcutol 以(54.26:23.81:21.93%v/v)的比例组成,透光率为 100%,白藜芦醇溶解度为 159.9±6.4mg/mL,粒径为 30.65nm。纳米乳和鼻用纳米乳凝胶中白藜芦醇的释放分别为 96.17±4.43%和 78.53±4.7%。12 小时内渗透持续,达到 63.95±4.7%。组织病理学研究表明,该配方对鼻黏膜安全且耐受。鼻用纳米乳凝胶鼻腔给药后 C 和 AUC 分别为 2.23 和 8.05 倍,T 增加至 3.67±0.82h。优化后的鼻用纳米乳凝胶建立了鼻内安全性和生物利用度的提高,因此被认为是一种针对大脑的设计良好的系统。