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Fabrication and Evaluation of Transdermal Delivery of Carbamazepine Dissolving Microneedles

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Abstract

This project aims to prepare hydrogel microneedle patches (MNs) as a painless method to deliver carbamazepine transdermally. This can be used as a sustained release system that offers the advantages of lower gastrointestinal side effects and avoids the first-pass metabolism of the drug. MNs were composed of two medicated layers, a microneedle layer and a base layer. MNs were fabricated using polyvinyl alcohol with or without polyvinylpyrrolidone Kollidon 30 as a matrix polymer and in the presence of selected solubilizing agent (polyethylene glycol 400, Tween 80, or α-tocopherol polyethylene glycol). Freezing–thawing cycle was evaluated as one of the processing parameters that may affect the drug release. The MNs were evaluated for their weight variation, base thickness, and content uniformity. The physicochemical compatibility between carbamazepine and the polymers was estimated by Fourier transform infrared spectroscopy, differential scanning calorimetry, thermogravimetric analysis, and X-ray powder diffraction. Evaluation for the in vitro release studies and ex vivo permeation studies was performed. The prepared MNs were flexible, clear, and uniform in weight, base thickness, and drug content. Physicochemical characterizations showed that carbamazepine was amorphous in most of the MNs. In vitro release and ex vivo permeation studies of carbamazepine were significantly higher for MNs containing a combination of 1:1 w/w of PEG 400 and Tween 80 as solubilizing agents where the release was extended over 96 h, with the release of 85.2% and 59.6% permeation percentage compared to other MNs. A significant effect of the freezing–thawing cycle on the release profile of the drug was observed. The hydrogel MNs are shown to be stable under the studied storage conditions.

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Abbreviations

ASD:

Anti-seizure drug

CBZ:

Carbamazepine

DSC:

Differential scanning calorimetry

FTIR:

Fourier transform infrared spectroscopy

MNs:

Microneedles

PEG:

400 Polyethylene glycol 400

PVA:

Polyvinyl alcohol

PVP K30:

Polyvinylpyrrolidone Kollidon 30

SEM:

Scanning electron microscope

TGA:

Thermogravimetric analysis

α-TPGS:

α-Tocopherol polyethylene glycol of vitamin E

XRPD:

X-ray powder diffraction

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Funding

For Deanship of Research at Jordan University of Science and Technology for funding this project with Fund number 517/2020.

Author information

Authors and Affiliations

  1. Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan

    Rana Obaidat, Fatima BaniAmer & Shereen M. Assaf

  2. Department of Neurosciences, Faculty of Medicine, Jordan University of Science and Technology, Irbid, Jordan

    Ahmed Yassin

Authors
  1. Rana Obaidat
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  2. Fatima BaniAmer
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  3. Shereen M. Assaf
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  4. Ahmed Yassin
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Contributions

Rana Obaidat: contributed to the conception, design, and interpretation. Fatima BaniAmer: performed the research in the lab, data analysis, and writing it as part of her master’s degree thesis. Shereen Assaf: contributed to design, characterization of the patches, and writing. Ahmed Yassin: contributed to the conception, design, and writing.

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Correspondence to Rana Obaidat.

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Obaidat, R., BaniAmer, F., Assaf, S.M. et al. Fabrication and Evaluation of Transdermal Delivery of Carbamazepine Dissolving Microneedles. AAPS PharmSciTech 22, 253 (2021). https://doi.org/10.1208/s12249-021-02136-1

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  • DOI: https://doi.org/10.1208/s12249-021-02136-1

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