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载药胶束化固体脂质纳米粒的环糊精修饰明胶干混悬型原位给药系统用于红花(Carthamus tinctorius. L)中生物活性化合物的控制释放:生物相关介质中的概念验证研究。

Solid lipid nanoparticles cyclodextrin-decorated incorporated into gellan gum-based dry floating in situ delivery systems for controlled release of bioactive compounds of safflower (Carthamus tinctorius. L): A proof of concept study in biorelevant media.

机构信息

Faculty of Pharmacy, Hasanuddin University, Makassar 90245, Indonesia.

Faculty of Pharmacy, Hasanuddin University, Makassar 90245, Indonesia.

出版信息

Int J Biol Macromol. 2023 May 15;237:124084. doi: 10.1016/j.ijbiomac.2023.124084. Epub 2023 Mar 20.

Abstract

Safflower (Carthamus tinctorius L.) has been explored as a source of natural antioxidant. However, quercetin 7-O-beta-D-glucopyranoside and luteolin 7-O-beta-D-glucopyranoside, as its bioactive compounds, possessed poor aqueous solubility, limiting its efficacy. Here, we developed solid lipid nanoparticles (SLNs) decorated with hydroxypropyl beta-cyclodextrin (HPβCD) incorporated into dry floating gel in situ systems to control the release of both compounds. Using Geleol® as a lipid matrix, SLNs were <200 nm in size with >80 % of encapsulation efficiency. Importantly, following the decoration using HPβCD, the stability of SLNs in gastric environment was significantly improved. Furthermore, the solubility of both compounds was also enhanced. The incorporation of SLNs into gellan gum-based floating gel in situ provided desired flow and floating properties, with <30 s gelation time. The floating gel in situ system could control the release of bioactive compounds in FaSSGF (Fasted-State Simulated Gastric Fluid). Furthermore, to assess the effect of food intake on release behavior, we found that the formulation could show a sustained release pattern in FeSSGF (Fed-State Simulated Gastric Fluid) for 24 h after being released in FaSGGF for 2 h. This indicated that this combination approach could be a promising oral delivery for bioactive compounds in safflower.

摘要

红花(Carthamus tinctorius L.)已被探索作为天然抗氧化剂的来源。然而,作为其生物活性化合物的槲皮素 7-O-β-D-吡喃葡萄糖苷和木樨草素 7-O-β-D-吡喃葡萄糖苷,其水溶性差,限制了其疗效。在这里,我们开发了固体脂质纳米粒(SLN),其表面用羟丙基-β-环糊精(HPβCD)修饰,并整合到干漂浮凝胶原位系统中,以控制两种化合物的释放。使用 Geleol®作为脂质基质,SLN 的粒径<200nm,包封效率>80%。重要的是,经过 HPβCD 修饰后,SLN 在胃环境中的稳定性得到了显著提高。此外,两种化合物的溶解度也得到了提高。将 SLN 掺入基于结冷胶的漂浮凝胶原位中提供了所需的流动和漂浮特性,凝胶化时间<30s。漂浮凝胶原位系统可以控制 FaSSGF(Fasted-State Simulated Gastric Fluid)中生物活性化合物的释放。此外,为了评估食物摄入对释放行为的影响,我们发现,在 FaSGGF 中释放 2 小时后,该制剂可以在 FeSSGF(Fed-State Simulated Gastric Fluid)中显示出 24 小时的持续释放模式。这表明这种组合方法可能是红花中生物活性化合物口服递送的一种有前途的方法。

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