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Zein Microneedles for Localized Delivery of Chemotherapeutic Agents to Treat Breast Cancer: Drug Loading, Release Behavior, and Skin Permeation Studies

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Abstract

Localized delivery of chemotherapeutic agents to treat breast cancer could limit their adverse drug reactions. The aim of this study was to investigate the influence of physico-chemical properties of chemotherapeutic agents in their loading, release behavior, and skin permeation using microneedles. Zein microneedles were fabricated using the micromolding technique containing 36 microneedles in a 1-cm2 area. These microneedles were loaded with two anti-breast cancer drugs, tamoxifen and gemcitabine, having different water solubilities. Entrapment or surface coating of chemotherapeutic agents in zein microneedles was optimized to achieve greater loading efficiency. The greatest loading achieved was 607 ± 21 and 1459 ± 74 μg for tamoxifen and gemcitabine using the entrapment approach, respectively. Skin permeation studies in excised porcine skin showed that the coating on microneedles approach results in greater skin deposition for tamoxifen; while the poke-and-patch approach would provide greater skin permeation for gemcitabine. Taken together, it can be concluded that different loading strategies and skin penetration approaches have to be studied for delivery of small molecules using polymeric microneedles.

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Acknowledgements

This work was financially supported by BITS Pilani. The texture analyzer and multimode plate reader were procured using a grant from the Department of Science and Technology—Fund for Improvement of Science and Technology infrastructure (DST FIST).

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  1. Pooja Kumari and Srijanaki Paravastu Pattarabhiran contributed equally to this work.

Authors and Affiliations

  1. Department of Pharmacy, Birla Institute of Technology and Science (BITS) Pilani, Hyderabad Campus, Hyderabad, Telangana, 500078, India

    Shubhmita Bhatnagar, Pooja Kumari, Srijanaki Paravastu Pattarabhiran & Venkata Vamsi Krishna Venuganti

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  1. Shubhmita Bhatnagar
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Correspondence to Venkata Vamsi Krishna Venuganti.

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Bhatnagar, S., Kumari, P., Pattarabhiran, S.P. et al. Zein Microneedles for Localized Delivery of Chemotherapeutic Agents to Treat Breast Cancer: Drug Loading, Release Behavior, and Skin Permeation Studies. AAPS PharmSciTech 19, 1818–1826 (2018). https://doi.org/10.1208/s12249-018-1004-5

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