Alshawwa Samar Zuhair, El-Masry Thanaa A, Elekhnawy Engy, Alotaibi Hadil Faris, Sallam Al-Sayed, Abdelkader Dalia H
Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia.
Pharmacology and Toxicology Department, Faculty of Pharmacy, Tanta University, Tanta 31527, Egypt.
Pharmaceuticals (Basel). 2023 Feb 8;16(2):258. doi: 10.3390/ph16020258.
Electrospraying (ES) technology is considered an efficient micro/nanoparticle fabrication technique with controlled dimensions and diverse morphology. Gelurice 48/16 (GLR) has been employed to stabilize the aqueous dispersion of Celecoxib (CXB) for enhancing its solubility and oral bioavailability. Our formula is composed of CXB loaded in polyvinylpyllodine (PVP) stabilized with GLR to formulate microparticles (MPs) (CXB-GLR-PVP MPs). CXB-GLR-PVP MPs display excellent in vitro properties regarding particle size (548 ± 10.23 nm), zeta potential (-20.21 ± 2.45 mV), and drug loading (DL, 1.98 ± 0.059 mg per 10 mg MPs). CXB-GLR-PVP MPs showed a significant ( < 0.05) higher % cumulative release after ten minutes (50.31 ± 4.36) compared to free CXB (10.63 ± 2.89). CXB exhibited good dispersibility, proved by X-ray diffractometry (XRD), adequate compatibility of all components, confirmed by Fourier-Transform Infrared Spectroscopy (FTIR), and spherical geometry as revealed in scanning electron microscopy (SEM). Concerning our anti-inflammatory study, there was a significant decrease in the scores of the inflammatory markers' immunostaining in the CXB-GLR-PVP MPs treated group. Also, the amounts of the oxidative stress biomarkers, as well as mRNA expression of interleukins (IL-1β and IL-6), considerably declined ( < 0.05) in CXB-GLR-PVP MPs treated group alongside an enhancement in the histological features was revealed. CXB-GLR-PVP MPs is an up-and-coming delivery system that could be elucidated in future clinical investigations.
电喷雾（ES）技术被认为是一种高效的微/纳米颗粒制造技术，能够控制颗粒尺寸并呈现多样的形态。已采用Gelurice 48/16（GLR）来稳定塞来昔布（CXB）的水分散体，以提高其溶解度和口服生物利用度。我们的配方由负载在经GLR稳定的聚乙烯吡咯烷酮（PVP）中的CXB组成，用于制备微粒（MPs）（CXB-GLR-PVP MPs）。CXB-GLR-PVP MPs在粒径（548±10.23 nm）、zeta电位（-20.21±2.45 mV）和载药量（DL，每10 mg MPs为1.98±0.059 mg）方面表现出优异的体外性能。与游离CXB（10.63±2.89）相比，CXB-GLR-PVP MPs在十分钟后的累积释放百分比显著更高（<0.05）（50.31±4.36）。X射线衍射（XRD）证明CXB具有良好的分散性，傅里叶变换红外光谱（FTIR）证实所有成分具有足够的相容性，扫描电子显微镜（SEM）显示其为球形几何形状。关于我们的抗炎研究，在CXB-GLR-PVP MPs治疗组中，炎症标志物免疫染色的评分显著降低。此外，在CXB-GLR-PVP MPs治疗组中，氧化应激生物标志物的量以及白细胞介素（IL-1β和IL-6）的mRNA表达显著下降（<0.05），同时组织学特征有所改善。CXB-GLR-PVP MPs是一种有前途的给药系统，有望在未来的临床研究中得到阐明。
