Suppr超能文献

负载ω-3 洛索洛芬的纳米乳剂的研制,以限制非甾体抗炎药治疗牙痛时的副作用。

Development of omega-3 loxoprofen-loaded nanoemulsion to limit the side effect associated with NSAIDs in treatment of tooth pain.

作者信息

Hosny Khaled M, Sindi Amal M, Alkhalidi Hala M, Kurakula Mallesh, Hassan Amira H, Bakhaidar Rana B, Abualsunun Walaa A, Almehmady Alshaimaa M, Khames Ahmed, Rizg Waleed Y, Khallaf Rasha A, Alruwaili Nabil K, Alhakamy Nabil A

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.

Center of Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah, Saudi Arabia.

出版信息

Drug Deliv. 2021 Dec;28(1):741-751. doi: 10.1080/10717544.2021.1909179.

Abstract

The majority of newly developed drugs need to be incorporated with delivery systems to maximize their effect and minimize side effects. Nanoemulsions (NEs) are one type of delivery system that helps to improve the solubility and dissolution of drugs, attempting to enhance their bioavailability and onset of action. The objective of this investigation was to develop an omega-3 oil-based NE loaded with loxoprofen (LXP) to enhance its dissolution, release, and mucosal penetration and decrease its mucosal ulcerative effects when applied in an oral treatment. LXP-loaded NEs were formulated with varying levels of omega-3 oil (10-30%), surfactant polyoxyethylene-C21-ethers (laureth-21) (40-60%), and co-surfactant polyethylene glycol-40 hydrogenated castor oil (HCO-40) (30-50%) using an extreme vertices mixture design. The developed NEs were characterized for globule size and drug loading capacity. The optimal formulation was tested for drug release, permeation, and ulcer index value. The developed NE acquired a globule size ranging 71-195 nm and drug loading capacity of 43-87%. Considering the results of the release study, the optimized NE formulation achieved 2.45-fold and 2-fold increases in drug permeation across tested mucosa compared to a marketed tablet and drug aqueous dispersion, respectively. Moreover, the optimum NE exhibited the best ulcer index in comparison to drug aqueous suspension and different formulations when tested in rats. Overall, this research highlights the capacity of NEs to deliver LXP with enhanced solubility, drug release, and permeation while effectively protecting the application site from side effects of the model drug.

摘要

大多数新开发的药物需要与给药系统相结合,以最大限度地发挥其疗效并最小化副作用。纳米乳剂(NEs)是一种给药系统,有助于提高药物的溶解度和溶出度,试图提高其生物利用度和起效速度。本研究的目的是开发一种负载洛索洛芬(LXP)的ω-3油基纳米乳剂,以增强其溶出度、释放度和黏膜渗透性,并在口服治疗时降低其黏膜溃疡性作用。采用极端顶点混合设计,用不同水平的ω-3油(10%-30%)、表面活性剂聚氧乙烯-C21-醚(月桂醇聚醚-21)(40%-60%)和助表面活性剂聚乙二醇-40氢化蓖麻油(HCO-40)(30%-50%)制备了负载LXP的纳米乳剂。对所制备的纳米乳剂进行了粒径和载药量表征。对最佳配方进行了药物释放、渗透和溃疡指数值测试。所制备的纳米乳剂粒径范围为71-195nm,载药量为43%-87%。考虑到释放研究的结果,优化后的纳米乳剂配方在经测试的黏膜上的药物渗透率分别比市售片剂和药物水分散体提高了2.45倍和2倍。此外,在大鼠体内测试时,与药物水混悬液和不同配方相比,最佳纳米乳剂表现出最佳的溃疡指数。总体而言,本研究突出了纳米乳剂在递送LXP时具有增强的溶解度、药物释放和渗透性的能力,同时能有效保护应用部位免受模型药物副作用的影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6337/8057080/68053e986c39/IDRD_A_1909179_F0001_C.jpg

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验