¹Department of Pharmaceutics and Pharmaceutical Technology, Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology, Changa- 388421, Anand, Gujarat, India
²Department of Pharmaceutics and Pharmaceutical Technology, S.K. Patel College of Pharmaceutical Education & Research, Ganpat University, Ganpat Vidyanagar- 384012, Mehsana, Gujarat, India DOI : 10.29228/jrp.2022.00 Levosulpiride (LSP) has been studied for its wide medicinal potential. One of its uses is in the treatment of schizophrenia. LSP has limited oral bioavailability because of its low permeability, dissolvability, and P-Glycoprotein (Pgp) efflux effect. Contrary to conventional methods, the intranasal route provides safe and effective treatment as well as targeted action. It can also prevent the P-gp efflux effect and increase brain bioavailability. In this research, we aimed to develop LSP-loaded Phospholipid Magnesomes (PMs), a novel vesicular nanosystem, recently fabricated for brain targeting by the Ultra-sonication method with materials including Phospholipon 90G, the combination of Propylene glycol and ethanol, magnesium sulphate (MgSO4) and water. The Box-Behnken design was utilized with 29 runs to optimize the LSP-PMs formulation. The formulation was confirmed and evaluated by the FTIR, DSC, PXRD, and TEM study. The formulation was investigated in vitro at pH 6.4, and the results showed that the formulation had improved drug release. The optimized LSP-PMs formula had a vesicle sizing of 85.035 ± 2.77 nm, a PDI of 0.392 ± 0.69, and a %EE of 76.024 %. Spherical and multilamellar morphology of LSP-PMs were visible by the TEM. The optimized LSP-PMs had the quickest medication diffusing profile, achieving 100% in one hour. The LSP-PMs formulation was stable at room temperature for 50 days when screened for the stability study. Thus, to sum up, the nano-vesicular system of LSP-PMs demonstrated to be a promising formulation for enhancing drug release of the poorly water-soluble and permeable LSP. Further investigation to analyze nasal transport to the brain, pharmacokinetic and pharmacodynamic effects, local safety, and the behavior of the developed carrier will require additional research. Keywords : Levosulpiride; schizophrenia; phospholipid magnesomes; antipsychotic drug; intranasal drug delivery systems; brain targeting; box-behnken design