Nanoemulsion-based intranasal drug delivery system of saquinavir mesylate for brain targeting.

摘要: The central nervous system (CNS) is an immunological privileged sanctuary site-providing reservoir for HIV-1 virus. Current anti-HIV drugs, although effective in reducing plasma viral levels, cannot eradicate the virus completely from body. low permeability of drugs across blood-brain barrier (BBB) leads to insufficient delivery. Therefore, developing a novel approaches enhancing CNS delivery are required treatment neuro-AIDS. aim this study was develop intranasal nanoemulsion (NE) enhanced bioavailability and targeting saquinavir mesylate (SQVM). SQVM protease inhibitor which poorly soluble drug widely used as antiretroviral drug, with oral about 4%. spontaneous emulsification method prepare drug-loaded o/w nanoemulsion, characterized by droplet size, zeta potential, pH, content. Moreover, ex-vivo permeation studies were performed using sheep nasal mucosa. optimized NE showed significant increase rate compared plain suspension (PDS). Cilia toxicity on mucosa no adverse effect SQVM-loaded NE. Results vivo biodistribution show higher concentration brain after administration than intravenous delivered PDS. percentage efficiency (% DTE) nose-to-brain direct transport DTP) indicated via route. Gamma scintigraphy imaging rat conclusively demonstrated at larger extent