Rivastigmine is a reversible cholinesterase inhibitor used to treat Alzheimer’s or Parkinson’s disease. Since its location of action is in the brain and maintaining a controlled dose over time can enable better efficacy with minimal side effects, this drug would benefit from a controlled delivery system. Recently, researchers from North Dakota State University used PLA (AP047) from PolySciTech (www.polyscitech.com) as part of developing a Rivastigmine depot delivery system. This research holds promise to improve Alzheimer’s treatment. Read more: Lipp, Lindsey Dawn. "Evaluation of Smart Polymers for Controlled Release Delivery Systems." PhD diss., North Dakota State University, 2019. http://search.proquest.com/openview/f4049113c6e85e87a5b855ddf97e1000/1?pq-origsite=gscholar&cbl=18750&diss=y
“Abstract (Abbreviated ): Our goal was to develop a smart polymer, controlled release delivery system and evaluate its capabilities for use with salmon calcitonin and rivastigmine. Thermosensitive and phase sensitive smart polymers were evaluated for their potential as controlled release delivery systems. Thermosensitive triblock copolymers were synthesized with increasing lactide to glycolide ratios of 3.5:1, 4.5:1, and 5:1. Characterization was via analytical techniques including proton nuclear magnetic resonance, gel permeation chromatography, critical micellar concentration, sol-gel transition test tube inversion, and cellular biocompatibility assay. Only the 5:1 lactide to glycolide copolymer transitioned into gel at body temperature. Release duration in vitro was 70 days when salmon calcitonin was incorporated at 40% (w/v) in 5:1 thermosensitive copolymer while retaining the native conformation of salmon calcitonin as analyzed via micro bicinchioninic acid assay, circular dichroism, and differential scanning calorimetry. For phase sensitive polymer, we found the best formulation after optimization was that of 5% (w/v) 50:50 poly(lactic-co-glycolic acid) in 95:5 benzyl benzoate to benzyl alcohol with rivastigmine base incorporated at 216 mg/ml. Release was observed over the course of ~ 42 days. The results demonstrate that controlled release rivastigmine was accomplished and shows promise as a method to increase dosing interval and improve quality of life for those suffering from Alzheimer’s Disease.”
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