Brain Targeting of Quetiapine Fumarate via Intranasal Delivery of Loaded Lipospheres: Fabrication, In-Vitro Evaluation, Optimization, and In-Vivo Assessment

Randa Mohammed Zaki; Mohammed F Aldawsari; Manal A Alossaimi; Shaikah F Alzaid; Vidya Devanathadesikan Seshadri; Alanood S Almurshedi; Basmah Nasser Aldosari; Rehab Mohammad Yusif; Ossama M Sayed

doi:10.3390/ph15091083

Brain Targeting of Quetiapine Fumarate via Intranasal Delivery of Loaded Lipospheres: Fabrication, In-Vitro Evaluation, Optimization, and In-Vivo Assessment

Pharmaceuticals (Basel). 2022 Aug 30;15(9):1083. doi: 10.3390/ph15091083.

Affiliations

¹ Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Al-Kharj 11942, Saudi Arabia.
² Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef P.O. Box 62514, Egypt.
³ Department of Pharmaceutical Chemistry, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Al-Kharj 11942, Saudi Arabia.
⁴ Department of Pharmacology and Toxicology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Al-Kharj 11942, Saudi Arabia.
⁵ Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
⁶ Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
⁷ Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Al-Madinah Al-Munawarah 41411, Saudi Arabia.
⁸ Department of Pharmaceutics, Faculty of Pharmacy, Sinai University-Kantara Branch, Ismailia 41612, Egypt.

Abstract

A liposphere system for intranasal delivery of quetiapine fumarate (QTF) was created to assess the potential for enhanced drug delivery. We investigated the effects of particle size, entrapment effectiveness, poly dispersibility index, and pluronic incorporation percentage on these variables. The optimal formula was examined using a TEM, and investigations into DSC, XRD, and FTIR were made. Optimized liposphere formulation in vitro dissolution investigation with a mean diameter of 294.4 ± 18.2 nm revealed about 80% drug release in 6 h. The intranasal injection of QTF-loaded lipospheres showed a shorter T_max compared to that of intranasal and oral suspension, per the findings of an in vivo tissue distribution investigation in Wistar mice. Lipospheres were able to achieve higher drug transport efficiency (DTE %) and direct nose-to-brain drug transfer (DTP %). A potentially effective method for delivering QTF to specific brain regions is the liposphere system.

Keywords: DTE%; brain targeting; intranasal; lipospheres; quetiapine fumarate.

Grants and funding

This research received no external funding.