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<p>Parkinson’s disease (PD) is a progressive neurodegenerative disorder characterized by the gradual loss of motor function. Current treatments, such as orally administered benztropine mesylate (BEZ), are limited by poor bioavailability, extensive first-pass metabolism, and suboptimal patient compliance. To address these challenges, this study presents a novel transdermal delivery system utilizing dissolving microneedles (DMNs) loaded with BEZ nanoparticles (NP). BEZ-NP were synthesized via ionic gelation using chitosan and sodium tripolyphosphate (STPP), and optimized through a 3<sup>2</sup> factorial design with chitosan (X₁) and STPP (X₂) concentrations as independent variables. Particle size (Y₁) and zeta potential (Y₂) served as critical response parameters. The optimized formulation yielded NP with a size of 229.4 ± 8.34&#xa0;nm and a zeta potential of 41.4 ± 2.68&#xa0;mV. Hydrophilic polymers such as hydroxypropyl methylcellulose (E5, E15) and polyethylene glycol 400 (PEG 400) were employed to fabricate DMN arrays, facilitating the effective transdermal delivery of BEZ-NP. ATR-FTIR analysis confirmed no significant drug–excipient interactions, while SEM revealed uniformly structured microneedles (~ 600&#xa0;µm height). Penetration force testing validated mechanical integrity and skin insertion capability. In vitro release studies indicated sustained BEZ release over 12&#xa0;h, and ex vivo porcine skin studies demonstrated enhanced and faster drug permeation using BEZ-NP-DMNs within 7&#xa0;h. These findings support the potential of BEZ-NP-loaded DMNs as a promising transdermal platform for improving BEZ delivery and therapeutic outcomes in PD management.</p> Graphical Abstract <p></p>

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Breaking the Barrier: Enhanced Transdermal Benztropine Delivery Using Nanoparticle-loaded Dissolving Microneedles

  • 期刊论文

  • 发表日期：

    2025年8月1日

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  • Rajdit Singh,
  • Harsh P. Nijhawan,
  • Khushwant S. Yadav

摘要

Parkinson’s disease (PD) is a progressive neurodegenerative disorder characterized by the gradual loss of motor function. Current treatments, such as orally administered benztropine mesylate (BEZ), are limited by poor bioavailability, extensive first-pass metabolism, and suboptimal patient compliance. To address these challenges, this study presents a novel transdermal delivery system utilizing dissolving microneedles (DMNs) loaded with BEZ nanoparticles (NP). BEZ-NP were synthesized via ionic gelation using chitosan and sodium tripolyphosphate (STPP), and optimized through a 32 factorial design with chitosan (X₁) and STPP (X₂) concentrations as independent variables. Particle size (Y₁) and zeta potential (Y₂) served as critical response parameters. The optimized formulation yielded NP with a size of 229.4 ± 8.34 nm and a zeta potential of 41.4 ± 2.68 mV. Hydrophilic polymers such as hydroxypropyl methylcellulose (E5, E15) and polyethylene glycol 400 (PEG 400) were employed to fabricate DMN arrays, facilitating the effective transdermal delivery of BEZ-NP. ATR-FTIR analysis confirmed no significant drug–excipient interactions, while SEM revealed uniformly structured microneedles (~ 600 µm height). Penetration force testing validated mechanical integrity and skin insertion capability. In vitro release studies indicated sustained BEZ release over 12 h, and ex vivo porcine skin studies demonstrated enhanced and faster drug permeation using BEZ-NP-DMNs within 7 h. These findings support the potential of BEZ-NP-loaded DMNs as a promising transdermal platform for improving BEZ delivery and therapeutic outcomes in PD management.

Graphical Abstract