University of Greifswald, Department of Pharmacy, Institute of Biopharmaceutics and Pharmaceutical Technology, Felix-Hausdorff-Straße 3, 17489, Greifswald, Germany.
Evonik Operations GmbH, Research, Development & Innovation, Kirschenallee, 64293, Darmstadt, Germany.
AAPS PharmSciTech. 2022 Aug 3;23(6):213. doi: 10.1208/s12249-022-02347-0.
Self-nanoemulsifying drug delivery systems (SNEDDS) represent an interesting platform for improving the oral bioavailability of poorly soluble lipophilic drugs. While Liquid-SNEDDS (L-SNEDDS) effectively solubilize the drug in vivo, they have several drawbacks, including poor storage stability. Solid-SNEDDS (S-SNEDDS) combine the advantages of L-SNEDDS with those of solid dosage forms, particularly stability. The aim of the present study was to convert celecoxib L-SNEDDS into S-SNEDDS without altering their release behavior. Various commercially available adsorptive carrier materials were investigated, as well as novel cellulose-based microparticles prepared by spray drying from an aqueous dispersion containing Diacel 10 and methyl cellulose or gum arabic as a binder prior to their use. Particle size and morphology of the carrier materials were screened by scanning electron microscopy and their effects on the loading capacity for L-SNEDDS were investigated, and comparative in vitro dissolution studies of celecoxib L-SNEDDS and the different S-SNEDDS were performed immediately after preparation and after 3 months of storage. Among the adsorptive carrier materials, the novel cellulose-based microparticles were found to be the most suitable for the preparation of celecoxib S-SNEDDS from L-SNEDDS, enabling the preparation of a solid, stable formulation while preserving the in vitro release performance of the L-SNEDDS formulation.
自微乳药物传递系统（SNEDDS）代表了改善脂溶性差的药物口服生物利用度的一种很有前途的平台。虽然液态 SNEDDS（L-SNEDDS）可以有效地在体内溶解药物，但它们存在一些缺点，包括储存稳定性差。固态 SNEDDS（S-SNEDDS）结合了 L-SNEDDS 的优点和固态剂型的优点，特别是稳定性。本研究的目的是在不改变其释放行为的情况下将塞来昔布 L-SNEDDS 转化为 S-SNEDDS。研究了各种市售的吸附性载体材料，以及通过喷雾干燥从含有 Diacel 10 和甲基纤维素或阿拉伯胶作为粘合剂的水性分散体制备的新型纤维素基微球，然后再使用它们。通过扫描电子显微镜筛选载体材料的粒径和形态，并研究其对 L-SNEDDS 的载药量的影响，同时对塞来昔布 L-SNEDDS 和不同 S-SNEDDS 的体外溶出度进行了比较，即在制备后立即和储存 3 个月后进行。在吸附性载体材料中，新型纤维素基微球被发现最适合从 L-SNEDDS 制备塞来昔布 S-SNEDDS，能够制备出稳定的固体制剂，同时保持 L-SNEDDS 制剂的体外释放性能。
