| Autor: |
Abdel-Bar HM; Department of Pharmaceutics, Faculty of Pharmacy, University of Sadat City, Sadat City 32897, Egypt.; Institute of Pharmaceutical Science, Faculty of Life Sciences & Medicine, King's College London, London SE1 9NH, UK., Tulbah AS; Department of Pharmaceutics, College of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi Arabia., Darwish HW; Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia., Salama R; Macquarie Medical School, Faculty of Medicine, Health and Human Sciences, Macquarie University, Sydney, NSW 2109, Australia.; Woolcock Institute of Medical Research, Glebe, NSW 2037, Australia., Naguib IA; Department of Pharmaceutical Chemistry, College of Pharmacy, Taif University, Taif 21944, Saudi Arabia., Yassin HA; Department of Pharmaceutics, Faculty of Pharmacy, Badr University in Cairo (BUC), Badr City 11829, Egypt., Abo El-Enin HA; Department of Pharmaceutics, National Organization of Drug Control and Research (NODCAR) (Previously), Egyptian Drug Authority (Currently), Giza 12511, Egypt. |
| Abstrakt: |
Quetiapine (QP) is a second-generation short-acting antipsychotic drug extensively metabolized in the liver, producing pharmacologically inactive metabolites and leading to diminished bioavailability. Therefore, this study aimed to develop an intravenous QP albumin nanoparticles (NPs) system for improving QP antipsychotic activity and brain targeting. QP-loaded albumin NPs were prepared by the desolvation method. The fabricated NPs were characterized in terms of particle size, zeta potential, entrapment efficiency (EE%), and in vitro drug release. In vivo pharmacokinetics and biodistribution in rats were studied. In addition, the antipsychotic activity of the optimized platform was also investigated. Human serum albumin (HSA) concentration, pH, and stirring time were modulated to optimize QP albumin NPs with a particle size of 103.54 ± 2.36 nm and a QP EE% of 96.32 ± 3.98%. In addition, the intravenous administration of QP albumin NPs facilitated QP brain targeting with a 4.9-fold increase in targeting efficiency compared to the oral QP solution. The QP albumin NPs improved the QP antipsychotic activity, indicated by suppressing rats' hypermobility and reducing the QP's extrapyramidal side effects. The obtained results proposed that intravenous QP- NPs could improve QP brain targeting and its antipsychotic efficiency. |
