Mucoadhesive nanoemulsion-based intranasal drug delivery system of olanzapine for brain targeting.
The objective of the present study was to optimize olanzapine nanoemulsion (ONE), for nose-to-brain delivery. The nanoemulsions and olanzapine mucoadhesive nanoemulsions (OMNEs) were prepared using water titration method and characterized for technical and electrokinetic properties. Biodistribution of nanoemulsions and olanzapine solution (OS) in the brain and blood of rats following intranasal (intranasal) and intravenous (intravenous) administrations were examined using optimized technetium-labeled ((99m)Tc-labeled) olanzapine formulations. The brain/blood uptake ratios of 0.45, 0.88, 0.80, and 0.04 of OS (intranasal), ONE (intranasal), OMNE (intranasal), ONE (intravenous), respectively, at 0.5 h are indicative of direct nose-to-brain transport (DTP). Higher % drug targeting efficiency (%DTE) and %DTP for mucoadhesive nanoemulsions indicated effective brain targeting of olanzapine among the prepared nanoemulsions. Gamma scintigraphy imaging of the rat brain conclusively demonstrated rapid and larger extent of transport of olanzapine by OMNE (intranasal), when compared with OS (intranasal), ONE (intranasal), and ONE (intravenous), into the rat brain.
Kumar
Mukesh
M
Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura, India.
Misra
Ambikanandan
A
Mishra
A K
AK
Mishra
Pushpa
P
Pathak
Kamla
K
D000281:Administration, Intranasal; D000818:Animals; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics; D001569:Benzodiazepines / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D001921:Brain / Q000378:metabolism*; D016503:Drug Delivery Systems; D004655:Emulsions / Q000008:administration & dosage* / Q000737:chemistry; D006220:Haloperidol; D007275:Injections, Intravenous; D008297:Male; D049329:Nanostructures / Q000008:administration & dosage* / Q000737:chemistry; D000077152:Olanzapine; D051381:Rats
D014150:Antipsychotic Agents; D004655:Emulsions; D001569:Benzodiazepines; D006220:Haloperidol; D000077152:Olanzapine