Characterization of naproxen-loaded solid SMEDDSs prepared by spray drying: The effect of the polysaccharide carrier and naproxen concentration
Characterization of naproxen-loaded solid SMEDDSs prepared by spray drying: The effect of the polysaccharide carrier and naproxen concentration
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DOI：
10.1016/j.ijpharm.2015.03.015
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发表时间：
2015-05-15
影响因子：
5.8
通讯作者：
Gasperlin, Mirjana
中科院分区：
文献类型：
--
作者：
Cerpnjak, Katja;Zvonar, Alenka;Gasperlin, Mirjana
本研究的目的是使用麦芽糖糊精（MD）、羟丙甲纤维素（HPMC）以及两者的组合作为固体载体，通过喷雾干燥制备固体SMEDDS（sSMEDDS）颗粒。将萘普生 (NPX) 作为模型药物溶解（浓度为 6%）或部分悬浮（浓度为 18%）于由 Miglyol(R) 812、Peceol(TM)、Gelucire(R) 44/14 和 Solutol(R) HS 15 组成的液体 SMEDDS 中。在测试的 sSMEDDS 中，基于 MD 的 sSMEDDS（具有颗粒状、 光滑表面、微球形外观）保留了液体 SMEDDS 的自微乳化特性，并表现出与液体 SMEDDS 相似的溶出曲线，无论 NPX 的浓度如何。相比之下，由于载体的聚合性质，基于 HPMC 的 sSMEDDS（不规则形状的微粒）表现出稍微延长的释放时间。差示扫描量热法 (DSC)、X 射线粉末衍射 (XRPD) 和拉曼图分析证实了 NPX 分子溶解（载药量为 6%），而 NPX 载量为 18% 时，药物部分分子溶解，部分处于结晶状态。 (C) 2015 Elsevier B.V. 保留所有权利。
The purpose of this study was to prepare solid SMEDDS (sSMEDDS) particles produced by spray-drying using maltodextrin (MD), hypromellose (HPMC), and a combination of the two as a solid carrier. Naproxen (NPX) as the model drug was dissolved (at 6% concentration) or partially suspended (at 18% concentration) in a liquid SMEDDS composed of Miglyol(R) 812, Peceol(TM), Gelucire(R) 44/14, and Solutol(R) HS 15. Among the sSMEDDSs tested, the MD-based sSMEDDSs (with a granular, smooth-surfaced, microspherical appearance) preserved the self-microemulsifying properties of liquid SMEDDSs and exhibited dissolution profiles similar to those of liquid SMEDDSs, irrespective of the concentration of NPX. In contrast, HPMC-based sSMEDDSs (irregular-shaped microparticles) exhibited slightly prolonged release times due to the polymeric nature of the carrier. Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), and Raman mapping analysis confirmed molecularly dissolved NPX (at 6% of drug loading), whereas at 18% NPX loading drug is partially molecularly dissolved and partially in the crystalline state. (C) 2015 Elsevier B.V. All rights reserved.