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THE DEVELOPMENT OF A BRAIN TARGETED MUCOADHESIVE AMISULPRIDE LOADED NANOSTRUCTURED LIPID CARRIER

MANAR ADNAN TAMER *, HANAN JALAL KASSAB

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This research aimed to create and refine intranasal mucoadhesive amisulpride-loaded nanostructured lipid carriers (AMS-MNLCs) to increase efficacy and safety by increasing nasal-mucosal adhesion and facilitating direct brain targetability. Using HPMC K4M, Carbopol 934, and Hyaluronic acid (HA), AMS-MNLCs were made by applying modified melt-emulsification and ultra-sonication procedures. The results of the pH, osmolarity, and mucoadhesive tests on the optimized formulation were 6.3 ± 0.02, 304.53 ± 2.15, and 26.07 ± 0.37, respectively. Rheological investigation, in-vitro release and ex-vivo permeation study of the optimized formulation revealed a shear-thinning behaviour, significantly higher release, and the flux of the drug from the formula was 975.2 ± 12.45. Based on the pharmacokinetic analyses in rats, intranasal AMS-MNLCs were reported to have a brain Cmax about 14 times higher than intravenous AMS-solution. In addition, two weeks of intranasal administration of formulation did not affect haematological parameters in the in vivo research. The histopathological investigation showed that there was no disruption of the naso-mucosal membrane structure. Therefore, the created and optimized intranasal MNLCs showed a promised venue for the efficient and secure delivery of AMS as an antiemetic drug for the prevention and treatment of preoperative nausea and vomiting (PONV).