Brain targeting of venlafaxine via intranasal transbilosomes thermogel for improved management of depressive disorder.

Autor:	Alsaidan OA; Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, 72341, Saudi Arabia. Electronic address: osaidan@ju.edu.sa., Elkomy MH; Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, 72341, Saudi Arabia. Electronic address: mhalkomy@ju.edu.sa., Zaki RM; Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Al-Kharj 11942, Saudi Arabia; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62511, Egypt. Electronic address: randazaki439@yahoo.com., Tulbah AS; Department of Pharmaceutical Sciences, College of Pharmacy, Umm al Qura University, Makkah 21955, Saudi Arabia. Electronic address: astulbah@uqu.edu.sa., Yusif RM; Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt; Department of Pharmaceutics and Pharmaceutical Industries, College of Pharmacy, Taibah University, P.O. Box 30039, Al-Madinah Al-Munawarah 41477, Saudi Arabia. Electronic address: rehabyusif@yahoo.com., Eid HM; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62511, Egypt. Electronic address: hussien.eid@pharm.bsu.edu.eg.
Jazyk:	angličtina
Zdroj:	Journal of pharmaceutical sciences [J Pharm Sci] 2024 Nov; Vol. 113 (11), pp. 3304-3314. Date of Electronic Publication: 2024 Aug 30.
DOI:	10.1016/j.xphs.2024.08.026
Abstrakt:	The current research aimed to design and optimize hyaluronic acid-coated transbilosomes containing venlafaxine (VLF-HA-TBLs) for nose-to-brain delivery for improved management of depressive disorder. Venlafaxine-loaded transbilosomes (VLF-TBLs) were developed according to the film hydration procedure, optimized for maximum efficiency using the quality by design-based Box-Behnken design (BBD), and then coated with hyaluronic acid (HA). The optimized VLF-HA-TBLs were subjected to in vitro characterization, integrated into a thermolabile gel, and then exposed to in vivo evaluation studies. The results revealed that the VLF-HA-TBLs formulation exhibited acceptable size (185.6 ± 4.9 nm), surface charge (-39.8 ± 1.7 mV), and entrapment efficiency (69.6 ± 2.6 %). The morphological study revealed that nanovesicles were spherical and displayed a consistent size distribution without particle aggregation. It also showed improved ex vivo nasal diffusion and a prolonged release profile. In addition, the formulated VLF-HA-TBLs were stable under the studied conditions and tolerable when applied intranasally. Compared to the intranasal administration of VLF solution (VLF-SOL), the biodistribution analysis showed that VLF-HA-TBLs delivered intranasally had a relative bioavailability of 441 % in the brain and 288 % in plasma. Moreover, the intranasal delivery of VLF-HA-TBLs demonstrated much higher bioavailability (512 %) in the brain compared to VLF-SOL administered intravenously. Collectively, it could be possible to infer that HA-TBLs might be an effective nanocarrier to administer VLF to the brain via the nasal route. Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. (Copyright © 2024 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.)
Databáze:	MEDLINE
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