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Polymer-Coated Polymeric (PCP) Microneedles for Controlled Dermal Delivery of 5-Fluorouracil

  • Research Article
  • Active and Passive Permeation Enhancement Strategies for Transdermal Delivery of Bioactive Compounds
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Abstract

Polymeric microneedles were prepared with Polyvinyl Pyrrolidone (PVP) K-30 using the mold casting technique. The core microneedles were coated with Eudragit E-100 by dip and spin method. The amount of 5-fluorouracil (FU) loaded in the core microneedles was 604 ± 35.4 µg. The coating thickness was 24.12 ± 1.12 µm. The objective was to deliver the 5-FU gradually in a controlled release manner at the target site in the sub-stratum corneum layer. This approach is anticipated to improve the safety and efficacy of topical melanoma treatment. The release of the drug was prolonged for up to 3 h from the polymer-coated polymeric (PCP) microneedles. The entire amount was found to release within 15 min in uncoated MNs. Likewise, the permeation of the drug from the uncoated microneedles was rapid, whereas the PCP microneedles were able to prolong the permeation up to 420 min. The PCP microneedles were subjected to stability studies at 25°C ± 2°C/60%RH, and 40°C ± 2°C/75%RH condition for 3 months. The formulations were found intact, and the release rate was not significantly different form the fresh formulation. The drug content was found to meet the acceptability criteria as well (98.12 ± 1.8% and 97.8 ± 2.1% at 25 and 40°C respectively after 3 months). Overall, this study demonstrated the feasibility of fabrication of PCP microneedles using Eudragit E100 for intraregional controlled delivery of drugs.

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Funding

Authors declare that there were no external fundings received for the submitted research article.

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Author notes

  1. Anusha V. Matadh and Deeksha Jakka have equal contribution.

Authors and Affiliations

  1. Institute for Drug Delivery and Biomedical Research, Bengaluru, India

    Anusha V. Matadh, S. G. Pragathi, H. N. Shivakumar & S. Narasimha Murthy

  2. University of Mississippi, Oxford, Mississippi, USA

    Deeksha Jakka

  3. Topical Products Testing LLC, Oxford, Mississippi, USA

    Srinath Rangappa, N. M. Reena & S. Narasimha Murthy

  4. KLE College of Pharmacy, Bengaluru, India

    H. N. Shivakumar

  5. University of California, San Francisco, California, USA

    Howard Maibach

Authors
  1. Anusha V. Matadh
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  2. Deeksha Jakka
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  3. S. G. Pragathi
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  4. Srinath Rangappa
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  5. H. N. Shivakumar
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  6. Howard Maibach
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  7. N. M. Reena
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  8. S. Narasimha Murthy
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Contributions

Conceptualization: S Narasimha Murthy, Shivakumar H N; methodology: Anusha V Matadh, Deeksha Jakka; formal analysis and investigation: Anusha V Matadh, Deeksha Jakka, Pragathi SG; writing—original draft preparation: S Narasimha Murthy, Anusha V Matadh, Deeksha Jakka; writing—review and editing: Howard Maibach, S Narasimha Murthy, Shivakumar H N, Srinath Rangappa, Reena N. M; supervision and advise: Howard Maibach.

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Correspondence to S. Narasimha Murthy.

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Matadh, A.V., Jakka, D., Pragathi, S.G. et al. Polymer-Coated Polymeric (PCP) Microneedles for Controlled Dermal Delivery of 5-Fluorouracil. AAPS PharmSciTech 24, 9 (2023). https://doi.org/10.1208/s12249-022-02471-x

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