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基于纳米乳液模板研究油相和表面活性剂对海藻酸盐基利多卡因O/W纳米载体形成的影响

Studies on the Effect of Oil and Surfactant on the Formation of Alginate-Based O/W Lidocaine Nanocarriers Using Nanoemulsion Template.

作者信息

Sarheed Omar, Dibi Manar, Ramesh Kanteti V R N S

机构信息

RAK College of Pharmaceutical Sciences, RAK Medical and Health Sciences University, Ras AlKhaimah 11172, UAE.

出版信息

Pharmaceutics. 2020 Dec 17;12(12):1223. doi: 10.3390/pharmaceutics12121223.

Abstract

The application of various nanocarrier systems was widely explored in the field of pharmaceuticals to achieve better drug encapsulation and delivery. The aim of this study was to encapsulate lidocaine in alginate-based o/w nanocarriers based on the type of oil (i.e., solid or liquid), using a nanoemulsion template prepared by ultrasound-assisted phase inversion temperature (PIT) approach. The nanoemulsion template was initially prepared by dissolving lidocaine in the oil phase and surfactant and alginate in the aqueous phase, and keeping the PIT at around 85 °C, accompanied by gradual water dilution at 25 °C, to initiate the formation of nanoparticles (o/w) with the aid of low frequency ultrasound. The composition and concentration of the oil phase had a major impact on the particle size and led to an increase in the size of the droplet. The lipids that showed a higher drug solubility also showed higher particle size. On the other hand, increasing the concentration of surfactant decreases the size of the droplet before the concentration of the surfactant exceeds the limit, after which the size of the particle increases due to the aggregates that could be produced from the excess surfactant. The method used produced nanoemulsions that maintained nano-sized droplets < 50 nm, over long-term storage. Our findings are important for the design of nanocarrier systems for the encapsulation of lipophilic molecules.

摘要

在制药领域,人们广泛探索了各种纳米载体系统的应用,以实现更好的药物包封和递送。本研究的目的是基于油的类型(即固体或液体),使用超声辅助相转变温度(PIT)法制备的纳米乳液模板,将利多卡因包裹在藻酸盐基水包油纳米载体中。纳米乳液模板最初是通过将利多卡因溶解在油相中,将表面活性剂和藻酸盐溶解在水相中制备的,并将PIT保持在85℃左右,同时在25℃下逐渐用水稀释,借助低频超声引发纳米颗粒(水包油)的形成。油相的组成和浓度对粒径有重大影响,并导致液滴尺寸增加。显示出较高药物溶解度的脂质也显示出较大的粒径。另一方面,在表面活性剂浓度超过极限之前,增加表面活性剂浓度会减小液滴尺寸,超过极限后,由于过量表面活性剂可能产生聚集体,颗粒尺寸会增加。所使用的方法制备的纳米乳液在长期储存过程中保持纳米级液滴<50nm。我们的研究结果对于设计用于包裹亲脂性分子的纳米载体系统具有重要意义。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b65/7766092/020ad510ba49/pharmaceutics-12-01223-g001.jpg

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