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<p>Solid drug-hydroxypropyl-β-cyclodextrin (HPβCD) inclusion complexes are used to enhance drug solubility and microneedle (MN)-mediated delivery efficiency. However, mechanistic understanding of HPβCD effects in solution on drug transport across pathways in MN-pretreated skin remains limited. This study investigated the <i>in vitro</i> permeation of rhein (RN) across MN-pretreated neonatal porcine skin from saturated RN solutions containing 0–200&#xa0;mM HPβCD. Phase solubility, total flux (<i>J</i><sub>total</sub>), and permeability coefficient through the microchannel pathway (<i>P</i><sub>MCP</sub>) were determined, along with dermal transport at varying HPβCD concentrations. Permeation experiments under asymmetric and symmetric donor–receiver HPβCD conditions were conducted to elucidate potential interactions between HPβCD and skin transport pathways. RN solubility increased from 241.9 ± 16.4&#xa0;µg/mL (0&#xa0;mM HPβCD) to 1,092.5 ± 54.9&#xa0;µg/mL (200&#xa0;mM HPβCD), showing a linear trend up to 50&#xa0;mM. MN permeation studies confirmed that RN transport occurred predominantly through microchannels. The highest <i>J</i><sub>total</sub> (3.87 ± 0.40&#xa0;μg/cm<sup>2</sup>/h) was achieved at 25&#xa0;mM HPβCD, with no further enhancement at higher concentration. Although increasing HPβCD concentration improved RN solubility, <i>P</i><sub>MCP</sub> and dermal transport decreased. Identical permeation profiles under symmetric and asymmetric conditions at 50&#xa0;mM HPβCD indicated no direct interaction between HPβCD and MN-pretreated skin. In summary, HPβCD-mediated solubility enhancement increased RN flux across MN-pretreated skin, but not microchannel permeability or dermal diffusion.</p> Graphical Abstract <p></p>

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In vitro Evaluation of Hydroxypropyl-β-cyclodextrin Effects on Rhein Flux Across Microneedle-pretreated Skin

  • 期刊论文

  • 发表日期：

    2026年5月15日

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  • Kamchai Saepang,
  • Puwich Chaikhumwang,
  • Benjaporn Buranrat,
  • Tasana Pitaksuteepong,
  • Supavadee Boontha

摘要

Solid drug-hydroxypropyl-β-cyclodextrin (HPβCD) inclusion complexes are used to enhance drug solubility and microneedle (MN)-mediated delivery efficiency. However, mechanistic understanding of HPβCD effects in solution on drug transport across pathways in MN-pretreated skin remains limited. This study investigated the in vitro permeation of rhein (RN) across MN-pretreated neonatal porcine skin from saturated RN solutions containing 0–200 mM HPβCD. Phase solubility, total flux (Jtotal), and permeability coefficient through the microchannel pathway (PMCP) were determined, along with dermal transport at varying HPβCD concentrations. Permeation experiments under asymmetric and symmetric donor–receiver HPβCD conditions were conducted to elucidate potential interactions between HPβCD and skin transport pathways. RN solubility increased from 241.9 ± 16.4 µg/mL (0 mM HPβCD) to 1,092.5 ± 54.9 µg/mL (200 mM HPβCD), showing a linear trend up to 50 mM. MN permeation studies confirmed that RN transport occurred predominantly through microchannels. The highest Jtotal (3.87 ± 0.40 μg/cm2/h) was achieved at 25 mM HPβCD, with no further enhancement at higher concentration. Although increasing HPβCD concentration improved RN solubility, PMCP and dermal transport decreased. Identical permeation profiles under symmetric and asymmetric conditions at 50 mM HPβCD indicated no direct interaction between HPβCD and MN-pretreated skin. In summary, HPβCD-mediated solubility enhancement increased RN flux across MN-pretreated skin, but not microchannel permeability or dermal diffusion.

Graphical Abstract