Methylene Blue (MB) has found in various areas of medicine and biology. At present MB is the first line treatment methemoglobinemias. Recently, its ability to attenuate the formation of amyloid plaques and neurofibrillary tangles in vitro, and to partially repair impairments in mitochondrial function and cellular metabolism, makes MB a promising candidate for the treatment of Alzheimer disease and other cognitive disorders. After i.v. administration the drug accumulates principally in the brain, but other administration routes must be used in Alzheimer's disease patients. Nasal administration could represent an interesting alternative for drugs direct to brain. However, a drug delivery system is nedeed to optimize the amount of drug reaching the CNS. In this work MB loaded PLGA nanoparticles were prepared using O/W and W/O/W displacement methods. Amphyphylic cyclodextrin (eptakis-(2-O-oligo(etilenossido)-6-esiltio)-beta-cyclodextrin - SC6OH) was added, at different amounts, to PLGA nanoparticles to evaluate its influence on technological parameters of the system. The presence of SC6OH in the nanoparticles reduces the yields, but increases encapsulation efficiency percentage (from 10% to 30% for PLGA and PLGA/SC6OH nanoparticles, respectively), the sizes (from 220 to 170 nm) and modulates the release of the drug. In vitro studies are in progress to evaluate how the carrier influences the drug behaviour on amyloid plaques and neurofibrillary tangles.
PLGA/AMPHIPHILIC CYCLODEXTRIN NANOPARTICLES LOADING METHYLENE BLUE FOR NOSE-TO-BRAIN TARGETING IN ALZHEIMER'S DISEASE
CANNAVA', CARMELA;STANCANELLI, Rosanna;TOMMASINI, Silvana;VENTURA, Cinzia Anna
2012-01-01
Abstract
Methylene Blue (MB) has found in various areas of medicine and biology. At present MB is the first line treatment methemoglobinemias. Recently, its ability to attenuate the formation of amyloid plaques and neurofibrillary tangles in vitro, and to partially repair impairments in mitochondrial function and cellular metabolism, makes MB a promising candidate for the treatment of Alzheimer disease and other cognitive disorders. After i.v. administration the drug accumulates principally in the brain, but other administration routes must be used in Alzheimer's disease patients. Nasal administration could represent an interesting alternative for drugs direct to brain. However, a drug delivery system is nedeed to optimize the amount of drug reaching the CNS. In this work MB loaded PLGA nanoparticles were prepared using O/W and W/O/W displacement methods. Amphyphylic cyclodextrin (eptakis-(2-O-oligo(etilenossido)-6-esiltio)-beta-cyclodextrin - SC6OH) was added, at different amounts, to PLGA nanoparticles to evaluate its influence on technological parameters of the system. The presence of SC6OH in the nanoparticles reduces the yields, but increases encapsulation efficiency percentage (from 10% to 30% for PLGA and PLGA/SC6OH nanoparticles, respectively), the sizes (from 220 to 170 nm) and modulates the release of the drug. In vitro studies are in progress to evaluate how the carrier influences the drug behaviour on amyloid plaques and neurofibrillary tangles.Pubblicazioni consigliate
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