Intranasal delivery of nanoparticle encapsulated tarenflurbil: A potential brain targeting strategy for Alzheimer's disease

Poor brain penetration of tarenflurbil (TFB) was one of the major reasons for its failure in phase III clinical trials conducted on Alzheimer's patients. Thus there is a tremendous need of developing efficient delivery systems for TFB. This study was designed with the aim of improving drug deli...

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Bibliographic Details
Published in:European journal of pharmaceutical sciences 2016-09, Vol.92, p.224-234
Main Authors: Muntimadugu, Eameema, Dhommati, Raju, Jain, Anjali, Challa, Venu Gopala Swami, Shaheen, M., Khan, Wahid
Format: Article
Language:English
Subjects:
Administration, Intranasal
Alzheimer Disease - drug therapy
Alzheimer Disease - metabolism
Alzheimer's disease
Animals
Brain - metabolism
Brain targeting
Drug Carriers - administration & dosage
Drug Carriers - chemistry
Drug Delivery Systems
Drug Liberation
Drug Stability
Flurbiprofen - administration & dosage
Flurbiprofen - blood
Flurbiprofen - chemistry
Flurbiprofen - pharmacokinetics
Lactic Acid - chemistry
Lipids - chemistry
Liver - metabolism
Lung - metabolism
Male
Myocardium - metabolism
Nanoparticles
Nanoparticles - administration & dosage
Nanoparticles - chemistry
Nose to brain delivery
Pharmacokinetics
Polyglycolic Acid - chemistry
Rats, Sprague-Dawley
Spleen - metabolism
Tarenflurbil
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Summary:Poor brain penetration of tarenflurbil (TFB) was one of the major reasons for its failure in phase III clinical trials conducted on Alzheimer's patients. Thus there is a tremendous need of developing efficient delivery systems for TFB. This study was designed with the aim of improving drug delivery to brain through intranasally delivered nanocarriers. TFB was loaded into two different nanocarriers i.e., poly (lactide-co-glycolide) nanoparticles (TFB-NPs) and solid lipid nanoparticles (TFB-SLNs). Particle size of both the nanocarriers (TFB-SLNs (i.n.)>TFB solution (i.n.)>TFB suspension (oral). Brain targeting efficiency was determined in terms of %drug targeting efficiency (%DTE) and drug transport percentage (DTP). The higher %DTE (287.24) and DTP (65.18) were observed for TFB-NPs followed by TFB-SLNs (%DTE: 183.15 and DTP: 45.41) among all other tested groups. These encouraging results proved that therapeutic concentrations of TFB could be transported directly to brain via olfactory pathway after intranasal administration of polymeric and lipidic nanoparticles. [Display omitted]
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2016.05.012