Abstract
Donepezil (DPZ) is generally administered orally to treat Alzheimer’s disease (AD). However, oral administration can cause gastrointestinal side effects. Therefore, to enhance compliance, a new way to deliver DPZ from transdermal patch was developed. Ionic bonds were created by dissolving dicarboxylic acid and DPZ in ethanol, resulting in a stable ionic liquid (IL) state. The synthesized ILs were characterized by differential scanning calorimetry, optical microscope, Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. The DPZ ILs were then transformed to a suitable drug-in-adhesive patch for transdermal delivery of DPZ. The novel DPZ ILs patch inhibits crystallization of the IL, indicating coherent design. Moreover, DPZ ILs and DPZ IL patch formulations performed excellent skin permeability compared to that of the DPZ free-base patch in both in vitro and ex vivo skin permeability studies.
Highlights
Donepezil (DPZ) is generally administered orally to treat Alzheimer’s disease (AD)
We developed a DPZ ionic liquid (IL) transdermal patch—a novel transdermal preparation of DPZ that can overcome the current drawbacks
Adipic acid and azelaic acid were chosen as model co-formers
Summary
Donepezil (DPZ) is generally administered orally to treat Alzheimer’s disease (AD). The DPZ ILs were transformed to a suitable drug-in-adhesive patch for transdermal delivery of DPZ. The most prescribed agents that can temporarily manage dementia are cholinesterase inhibitors (ChEIs) such as donepezil, galantamine, and rivastigmine [3] Among these ChEIs, donepezil (DPZ) has been reported to show beneficial effects in patients with more severe AD [4]. Since the oral DPZ therapy is associated with adverse events and plasma concentration fluctuations, DPZ transdermal patch has been employed as an alternative route of administration. Traditional DPZ transdermal preparations contain many permeation enhancers owing to its low skin permeability, which may cause skin irritation problems; solid crystals are generated during storage, resulting in reduce adhesion and a non-uniform skin permeation rate.
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