Nyavanandi Dinesh, Mandati Preethi, Narala Sagar, Alzahrani Abdullah, Kolimi Praveen, Vemula Sateesh Kumar, Repka Michael A
Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA.
Pii Center for Pharmaceutical Technology, The University of Mississippi, Oxford, MS 38677, USA.
Pharmaceutics. 2023 Sep 1;15(9):2267. doi: 10.3390/pharmaceutics15092267.
The current research aims to improve the solubility of the poorly soluble drug, i.e., ibuprofen, by developing self-emulsifying drug delivery systems (SEDDS) utilizing a twin screw melt granulation (TSMG) approach. Gelucire 44/14, Gelucire 48/16, and Transcutol HP were screened as suitable excipients for developing the SEDDS formulations. Initially, liquid SEDDS (L-SEDDS) were developed with oil concentrations between 20-50% / and surfactant to co-surfactant ratios of 2:1, 4:1, 6:1. The stable formulations of L-SEDDS were transformed into solid SEDDS (S-SEDDS) using a suitable adsorbent carrier and compressed into tablets (T-SEDDS). The S-SEDDS has improved flow, drug release profiles, and permeability compared to pure drugs. The existence of the drug in an amorphous state was confirmed by differential scanning calorimetry (DSC) and powder X-ray diffraction analysis (PXRD). The formulations with 20% / and 30% / of oil concentration and a 4:1 ratio of surfactant to co-surfactant have resulted in a stable homogeneous emulsion with a globule size of 14.67 ± 0.23 nm and 18.54 ± 0.55 nm. The compressed tablets were found stable after six months of storage at accelerated and long-term conditions. This shows the suitability of the TSMG approach as a single-step continuous manufacturing process for developing S-SEDDS formulations.
当前的研究旨在通过采用双螺杆熔融制粒（TSMG）方法开发自乳化药物递送系统（SEDDS）来提高难溶性药物布洛芬的溶解度。筛选了Gelucire 44/14、Gelucire 48/16和Transcutol HP作为开发SEDDS制剂的合适辅料。最初，开发了油浓度在20%-50%之间且表面活性剂与助表面活性剂比例为2:1、4:1、6:1的液体SEDDS（L-SEDDS）。使用合适的吸附载体将L-SEDDS的稳定制剂转化为固体SEDDS（S-SEDDS），并压制成片剂（T-SEDDS）。与纯药物相比，S-SEDDS具有改善的流动性、药物释放曲线和渗透性。通过差示扫描量热法（DSC）和粉末X射线衍射分析（PXRD）证实了药物以无定形状态存在。油浓度为20%和30%且表面活性剂与助表面活性剂比例为4:1的制剂形成了稳定的均匀乳液，其球粒尺寸分别为14.67±0.23 nm和18.54±0.55 nm。在加速和长期条件下储存六个月后，发现压制片剂稳定。这表明TSMG方法作为开发S-SEDDS制剂的单步连续制造工艺是合适的。
