开发和评估装载三联疗法的固化过饱和 SNEDDS,用于治疗代谢综合征。

IF 3.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Abdelrahman Y. Sherif, Doaa Hasan Alshora, Mohamed Abbas Ibrahim, Adel Jreebi
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引用次数: 0

摘要

本研究旨在开发和优化固化过饱和自纳米乳化给药系统(SNEDDS),用于联合给药抗高血压、抗高血糖和抗高血脂药物,以提高这些药物在治疗代谢综合征期间的溶解度和溶出度。我们制备了各种 SNEDDS 制剂,并对其进行了药物评估。评估了坎地沙坦(CC)、格列本脲(GB)和洛伐他汀(RC)在 SNEDDS 和过饱和 SNEDDS 制剂中的溶解度。优化后的制剂使用 Syloid 吸附剂按不同比例进行固化。制剂的药物表征包括粒度、ZETA电位、体外溶解度、PXRD、FTIR和SEM分析。制备的优化配方(F6)能够形成均匀的纳米乳液液滴,且无相分离现象,其成分为吐温 20:PEG-400:Capmul MCM(4:3:3)。将其与 5% 的 PVP-K30 混合,制备出一种过饱和液体 SNEDDS 配方(F9)。此外,研究还发现,添加 PVP-K30 后,CC 和 GB 的溶解度分别从 20.46 ± 0.48 毫克/克和 6.73 ± 0.05 毫克/克显著提高到 27.67 ± 1.72 毫克/克和 9.45 ± 0.32 毫克/克。体外溶出度研究表明,与纯药相比,液体和固体 SNEDD 制剂显著提高了 CC、GB 和 RC 的溶出率。XRPD 和傅立叶变换红外光谱分析显示,在制备的固态过饱和 SNEDD 配方中,所有药物都呈无定形状态。扫描电镜图像显示,液态 SNEDDS 配方成功吸附在 Syloid 表面。总之,优化的 F9 和固化过饱和 SNEDDS 制剂在提高药物溶解度和溶解速率方面表现优异。本研究表明,所提出的代谢综合征三联疗法是治疗代谢综合征的一种很有前景的策略。要评估固化过饱和 SNEDDS 制剂的疗效,还需要进一步的体内研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Development and Evaluation of Solidified Supersaturated SNEDDS Loaded with Triple Combination Therapy for Metabolic Syndrome

Development and Evaluation of Solidified Supersaturated SNEDDS Loaded with Triple Combination Therapy for Metabolic Syndrome

Development and Evaluation of Solidified Supersaturated SNEDDS Loaded with Triple Combination Therapy for Metabolic Syndrome

The present study aimed to develop and optimize solidified supersaturated self-nanoemulsifying drug delivery systems (SNEDDS) for the combined administration of antihypertensive, antihyperglycemic, and antihyperlipidemic drugs to enhance their solubility and dissolution during the treatment of metabolic syndrome. Various SNEDDS formulations were prepared and subjected to pharmaceutical assessment. The solubility of candesartan (CC), glibenclamide (GB), and rosuvastatin (RC) in SNEDDS and supersaturated SNEDDS formulations was evaluated. The optimized formulation was solidified using Syloid adsorbent at different ratios. Pharmaceutical characterization of the formulations included particle size, zeta potential, in-vitro dissolution, PXRD, FTIR, and SEM analysis. The prepared optimized formulation (F6) was able to form homogeneous nanoemulsion droplets without phase separation, which is composed of Tween 20: PEG-400: Capmul MCM (4: 3: 3). It was mixed with 5% PVP-K30 to prepare a supersaturated liquid SNEDDS formulation (F9). In addition, it was found that the addition of PVP-K30 significantly increased solubility CC and GB from 20.46 ± 0.48 and 6.73 ± 0.05 to 27.67 ± 1.72 and 9.45 ± 0.32 mg/g, respectively. In-vitro dissolution study revealed that liquid and solid SNEDD formulations remarkably improved the dissolution rates of CC, GB, and RC compared to pure drugs. XRPD and FTIR analysis revealed that all drugs present in an amorphous state within prepared solidified supersaturated SNEDDS formulation. SEM images showed that liquid SNEDDS formulation was successfully adsorbed on the surface of Syloid. Overall, optimized F9 and solidified supersaturated SNEDDS formulations showed superior performance in enhancing drug solubility and dissolution rate. The present study revealed that the proposed triple combination therapy of metabolic syndrome holds a promising strategy during the treatment of metabolic syndrome. Further in-vivo studies are required to evaluate the therapeutic efficacy of prepared solidified supersaturated SNEDDS formulation.

Graphical Abstract

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来源期刊
AAPS PharmSciTech
AAPS PharmSciTech 医学-药学
CiteScore
6.80
自引率
3.00%
发文量
264
审稿时长
2.4 months
期刊介绍: AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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