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Impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system and self nano-emulsifying granule system
International Journal of Pharmaceutics ( IF 5.3 ) Pub Date : 2023-11-04 , DOI: 10.1016/j.ijpharm.2023.123578
Jung Suk Kim 1 , Fakhar Ud Din 2 , Hyuk Jun Cho 1 , Yoo Jin Choi 1 , Mi Ran Woo 1 , Seunghyun Cheon 1 , Sang Hun Ji 1 , Seonghyeon Park 1 , Yu Seok Youn 3 , Kyung Taek Oh 4 , Soo-Jeong Lim 5 , Sung Giu Jin 6 , Han-Gon Choi 1
Affiliation  

The purpose of this study was to investigate the impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system (SNEDDS) and self nano-emulsifying granule system (SEGS). The mesoporous calcium silicate (Ca-silicate) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were utilised as hydrophobic carrier and hydrophilic carrier, respectively. The liquid SNEDDS formulation, composed of Tween80/Kollipohr EL/corn oil (35/50/15%) with 31% (w/w) dexibuprofen, was spray-dried and fluid-bed granulated together with Avicel using Ca-silicate or HP- β-CD as a solid carrier, producing four different solid SNEDDS and SEGS formulations. Unlike the Ca-silicate-based systems, spherical shape and aggregated particles were shown in HP-β-CD-based solid SNEDDS and SEGS, respectively. Molecular interaction was detected between Ca-silicate and the drug; though, none was shown between HP-β-CD and the drug. Each system prepared with either carrier gave no significant differences in micromeritic properties, crystallinity, droplet morphology, size, dissolution and oral bioavailability in rats. However, the HP-β-CD-based system more significantly improved the drug solubility than did the Ca-silicate-based system. Therefore, both carriers hardly affected the properties of both solid SNEDDS and SEGS; though, there were differences in the aspect of appearance, molecular interaction and solubility.



中文翻译:


载体亲水性对固体自纳米乳化给药系统和自纳米乳化颗粒系统的影响



本研究的目的是探讨载体亲水性对固体自纳米乳化给药系统(SNEDDS)和自纳米乳化颗粒系统(SEGS)的影响。介孔硅酸钙(Ca-silicate)和羟丙基-β-环糊精(HP-β-CD)分别用作疏水性载体和亲水性载体。液体 SNEDDS 制剂由 Tween80/Kollipohr EL/玉米油 (35/50/15%) 和 31% (w/w) 右布洛芬组成,使用硅酸钙或 HP 与 Avicel 一起进行喷雾干燥和流化床造粒- β-CD作为固体载体,产生四种不同的固体SNEDDS和SEGS制剂。与硅酸钙基体系不同,HP-β-CD 基固体 SNEDDS 和 SEGS 中分别显示出球形和聚集颗粒。检测到硅酸钙与药物之间存在分子相互作用;然而,HP-β-CD 和药物之间没有显示任何结果。用任一载体制备的每个系统在微粒特性、结晶度、液滴形态、大小、溶出度和大鼠口服生物利用度方面没有显着差异。然而,基于 HP-β-CD 的系统比基于硅酸钙的系统更显着地提高了药物溶解度。因此,两种载体对固体SNEDDS和SEGS的性能几乎没有影响;但在外观、分子相互作用和溶解度方面存在差异。

更新日期:2023-11-04
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