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324863 occurrences (No.63 in the rank) during 5 years in the PubMed. [cache]
9) Due to extreme aqueous solubility, rivastigmine shows poor penetration and lesser concentration in the brain thus requiring frequent oral dosing.
--- ABSTRACT ---
PMID:24467601 DOI:10.3109/10717544.2013.878857
2015 Drug delivery
* Nose to brain microemulsion-based drug delivery system of rivastigmine: formulation and ex-vivo characterization.
- Alzheimer's disease (AD) is a progressive neurodegenerative disorder leading to irreversible loss of neurons, cognition and formation of abnormal protein aggregates. Rivastigmine, a reversible cholinesterase inhibitor used for the treatment of AD, undergoes extensive first-pass metabolism, thus limiting its absolute bioavailability to only 36% after 3-mg dose. Due to extreme aqueous solubility, rivastigmine shows poor penetration and lesser concentration in the brain thus requiring frequent oral dosing. This investigation was aimed to formulate microemulsion (ME) and mucoadhesive microemulsions (MMEs) of rivastigmine for nose to brain delivery and to compare percentage drug diffused for both systems using in-vitro and ex-vivo study. Rivastigmine-loaded ME and MMEs were prepared by titration method and characterized for drug content, globule size distribution, zeta potential, pH, viscosity and nasal ciliotoxicity study. Rivastigmine-loaded ME system containing 8% w/w Capmul MCM EP, 44% w/w Labrasol:Transcutol-P (1:1) and 48% w/w distilled water was formulated, whereas 0.3% w/w chitosan (CH) and cetyl trimethyl ammonium bromide (as mucoadhesive agents) were used to formulate MMEs, respectively. ME and MMEs formulations were transparent with drug content, globule size and zeta potential in the range of 98.59% to 99.43%, 53.8 nm to 55.4 nm and -2.73 mV to 6.52 mV, respectively. MME containing 0.3% w/w CH followed Higuchi model (r(2) = 0.9773) and showed highest diffusion coefficient. It was free from nasal ciliotoxicity and stable for three months. However, the potential of developed CH-based MME for nose to brain delivery of rivastigmine can only be established after in-vivo and biodistribution study.
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--- WordNet output for due --- =>1.予定の, 支払期日がきて, 当然支払われるべき, 2.支払[提出]期日, 満期日, 会費 Overview of noun due The noun due has 2 senses (first 1 from tagged texts) 1. (4) due -- (that which is deserved or owed; "give the devil his due") 2. due -- (a payment that is due (e.g., as the price of membership); "the society dropped him for non-payment of dues") Overview of adj due The adj due has 4 senses (first 2 from tagged texts) 1. (6) due -- (owed and payable immediately or on demand; "payment is due") 2. (1) due -- (scheduled to arrive; "the train is due in 15 minutes") 3. due -- (suitable to or expected in the circumstances; "all due respect"; "due cause to honor them"; "a long due promotion"; "in due course"; "due esteem"; "exercising due care") 4. ascribable, due, imputable, referable -- (capable of being assigned or credited to; "punctuation errors ascribable to careless proofreading"; "the cancellation of the concert was due to the rain"; "the oversight was not imputable to him") Overview of adv due The adv due has 1 sense (no senses from tagged texts) 1. due -- (directly or exactly; straight; "went due North") --- WordNet end ---