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Formulation, Preparation, Characterization, and Evaluation of Dicarboxylic Ionic Liquid Donepezil Transdermal Patches.

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.

SUBMITTER: Dinh L

PROVIDER: S-EPMC8812279 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature

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Formulation, Preparation, Characterization, and Evaluation of Dicarboxylic Ionic Liquid Donepezil Transdermal Patches.

Dinh Linh L Lee Soohun S Abuzar Sharif Md SM Park Heejun H Hwang Sung-Joo SJ

Pharmaceutics 20220116 1

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 s ...[more]

PMID: 35057101

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Project description:Transdermal insulin delivery is a promising method for diabetes management, providing the potential for controlled, sustained release and prolonged insulin effectiveness. However, the large molecular weight of insulin hinders its passive absorption through the stratum corneum (SC) of the skin, and high doses of insulin are required, which limits the commercial viability. We developed ethosome (ET) and trans-ethosome (TET) nanovesicle formulations containing a biocompatible lipid-based ionic liquid, [EDMPC][Lin], dissolved in 35% ethanol. TET formulations were obtained by adding isopropyl myristate (IPM), Tween-80, or Span-20 as surfactants to ET formulations. Dynamic light scattering, ζ-potential, transmission electron microscopy, and confocal laser scanning microscopy studies revealed that the nanovesicles had a stable particle size. The formulations remained stable at 4 °C for more than 3 months. ET and TET formulations containing IPM (TET1) significantly (p < 0.0001) enhanced the transdermal penetration of FITC-tagged insulin (FITC-Ins) in both mouse and pig skin, compared with that of the control FITC-Ins solution and other TET formulations, by altering the molecular structure of the SC layer. These nanovesicles were found to be biocompatible and nonirritants (cell viability >80%) in the in vitro and in vivo studies on three-dimensional (3D) artificial human skin and a diabetic mouse model, respectively. The ET and TET1 formulations were applied to the skin of diabetic mice at an insulin dosage of 30 IU/kg. The nanovesicle formulations significantly reduced blood glucose levels (BGLs) compared with the initial high BGL value (>150 mg/dL). The nanovesicle-treated mice maintained low BGLs for over 15 h, as opposed to only 2 h in the injection group. The ET and TET1 formulations reduced the BGLs by 62 and 34%, respectively, of the initial value. These ET and TET1 formulations have a high potential for use in commercial transdermal insulin patches, enhancing comfort and adherence in diabetes treatment.

Dataset Information

Formulation, Preparation, Characterization, and Evaluation of Dicarboxylic Ionic Liquid Donepezil Transdermal Patches.

Publications

Formulation, Preparation, Characterization, and Evaluation of Dicarboxylic Ionic Liquid Donepezil Transdermal Patches.

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