DRUG DELIVERY TO THE BRAIN BY WAY OF NASAL ADMINISTRATION, TWENTY EFFECTIVE DRUGS, THEIR PROPERTIES, AND SCREENING METHOD TO IDENTIFY DRUGS FOR SIMILAR DELIVERY

The blood-brain barrier imposes restrictions on delivery of drugs to the brain. To circumvent these restrictions and to target the brain, investigators have pursued the study and implementation of nasal delivery of various drugs. This study examines the molecular properties of 20 pharmaceuticals that are administered through the nose in order to maximize delivery, achieve higher doses, and/or increase the speed of reaching the brain. The pathologies that can be treated in this manner include: Parkinsons’s disease, brain stroke, Alzheimer’s disease, depression, epilepsy, migraines, seizures, and sedation (as part of clinical treatment). Specific molecular properties determined and evaluated, will include: mass, Log P, polar surface area, hydrogen bond acceptors, hydrogen bond donors, number of atoms, refractivity, and violations of the Rule of 5. These are properties associated with evaluating drug-likeness (referring to drug absorption or permeation). Summary statistics of the molecular properties for these 20 pharmaceuticals is accomplished, to include mean, minimum, maximum, and 95% confidence interval of properties, which in turn can be utilized to evaluate other drugs for potential nasal administration. Pattern recognition methods such as nearest neighbor cluster analysis, Convex Hull, and box plots, shows interrelationships within their molecular properties of this group of 20 nasal administered drugs. Multiple regression analysis produces a mathematical equation accounting for a high level of variance within this multivariate table of molecular properties and can be applied in the design of similar acting pharmaceuticals. Altogether, this study presents an approach to identify other drugs that can be anticipated to be successful for nasal administration.