新一代自纳米乳化体系的Pluronic F-68三嵌段共聚物结构:克服坎地沙坦西莱西酯的药物捕获和剂量挑战

IF 4.3 3区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
ACS Omega Pub Date : 2025-09-11 DOI:10.1021/acsomega.5c06315
Abdelrahman Y. Sherif*,  and , Mohamed Abbas Ibrahim, 
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引用次数: 0

摘要

液体自纳米乳化给药系统(L-SNEDDS)的固化通常用于避免药物在储存过程中泄漏。然而,传统的吸附固化方法存在一定的局限性,包括药物在吸附剂孔隙中的捕获和所需的总剂量高。以三嵌段共聚物Pluronic F-68为原料,以坎地沙坦西莱西酯为模型药物,制备了具有原位液化性能的聚合物SNEDDS (IL-SNEDDS)。考察药物溶解度,选择L-SNEDDS的最佳处方。然后制备S-SNEDDS和IL-SNEDDS并进行理化表征。采用体外溶出度法,探讨不同剂型对坎地沙坦西蕾蒂酯(CC)溶出度的影响。优选出的L-SNEDDS最佳配方为:Tween-80:Imwitor-308:丙二醇(2:1:1)。选择含7.5% w/w Pluronic-F-68的IL-SNEDDS为最佳配方,液化温度为34℃,液化时间为75 s。此外,物理化学表征表明坎地沙坦西莱西酯在制备的S-SNEDDS和IL-SNEDDS配方中以无定形存在,没有化学相互作用的迹象。与S-SNEDDS相比,IL-SNEDDS能够增强坎地沙坦西莱西地酯的溶解,而没有药物捕获的迹象。本研究提出了一种新的方法,可以克服传统固体SNEDDS的局限性,促进SNEDDS作为药物剂型的应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pluronic F-68 Triblock Copolymer Architecture for a Next-Generation Self-Nanoemulsifying System: Overcoming Drug Trapping and Dosage Challenges of Candesartan Cilexetil

Solidification of liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) is commonly used to avoid formulation leakage during storage. However, traditional solidification using the adsorption method has limitations, including the trapping of drugs within adsorbent pores and the high total dosage required. Pluronic F-68, a triblock copolymer, was utilized to prepare a polymeric SNEDDS with an in situ liquefying property (IL-SNEDDS) using candesartan cilexetil as a model drug. Drug solubility was examined to choose the optimum L-SNEDDS formulation. Afterward, S-SNEDDS and IL-SNEDDS were prepared and subjected to physicochemical characterization. In vitro dissolution was conducted to explore the influence of the formulation type on the dissolution profile of candesartan cilexetil (CC). The selected optimum L-SNEDDS formulation consisted of Tween-80:Imwitor-308:propylene glycol (2:1:1). The IL-SNEDDS formulation containing 7.5% w/w Pluronic-F-68 was selected as the optimum formulation with a liquefying temperature (34 °C) and liquefying time (75 s). Furthermore, physicochemical characterization revealed that candesartan cilexetil was present in the amorphous state within the prepared S-SNEDDS and IL-SNEDDS formulations, with no indication of a chemical interaction. In contrast to S-SNEDDS, IL-SNEDDS was able to enhance the dissolution of candesartan cilexetil with no sign of drug trapping. The present study presents a new approach that can overcome the limitations of traditional solid SNEDDS and enhance the application of SNEDDS as a pharmaceutical dosage form.

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来源期刊
ACS Omega
ACS Omega Chemical Engineering-General Chemical Engineering
CiteScore
6.60
自引率
4.90%
发文量
3945
审稿时长
2.4 months
期刊介绍: ACS Omega is an open-access global publication for scientific articles that describe new findings in chemistry and interfacing areas of science, without any perceived evaluation of immediate impact.
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