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Drug Delivery to the Skin From Sub-micron Polymeric Particle Formulations: Influence of Particle Size and Polymer Hydrophobicity

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Abstract

Purpose

To investigate the influence of particle size and polymer properties on the topical delivery of a lipophilic “active” species (Nile Red (NR)) from sub-micron polymeric particles.

Methods

Three poly-(ε-caprolactone) (CAPA) formulations were examined to assess the impact of particle size. Three other formulations, based on cellulose acetate butyrate (CAB), CAPA and polystyrene were studied to address the role of polymer hydrophobicity. In vitro skin permeation, and confocal microscopy and stratum corneum (SC) tape-stripping were used to evaluate the cutaneous disposition of NR.

Results

NR delivery into the SC was greater from the larger particles, the overall smaller surface area of which enhanced the “leaving tendency” of the lipophilic “active”. Skin uptake of NR (measured as “%payload released”) from polystyrene, CAPA and CAB particles increased with decreasing polymer hydrophobicity (polystyrene > CAPA > CAB) as expected. Confocal microscopy revealed that NR released from the particles accumulated in, and penetrated via, lipid domains between the SC corneocytes. The particles showed affinity for hairs, and concentrated on the skin surface at the follicular openings.

Conclusions

Delivery of a model drug to the skin from sub-micron polymeric particle formulations is sensitive to the particle size and the relative hydrophobicity of the carrier.

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Abbreviations

CAB:

cellulose acetate butyrate

CAPA:

poly-(ε-caprolactone)

LSCM:

laser scanning confocal microscopy

NR:

Nile Red

PI:

polydispersity index

PS:

polystyrene

SC:

stratum corneum

TEWL:

transepidermal water loss

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ACKNOWLEDGEMENTS

Supported by the European Commission 6th Research and Technological Development Framework Programme (NAPOLEON: NAnostructured waterborne POLymEr films with OutstaNding properties) and a University Research Scholarship for Xiao Wu.

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Author notes

  1. Xiao Wu

    Present address: College of Pharmacy, University of Kentucky, Lexington, Kentucky, 40536-0082, USA

Authors and Affiliations

  1. Department of Pharmacy & Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK

    Xiao Wu & Richard H. Guy

  2. L’Oréal Research, F-94550, Chevilly-Larue, France

    Bruno Biatry

  3. L’Oréal Research, F-93601, Aulnay-sous-Bois, France

    Colette Cazeneuve

Authors
  1. Xiao Wu
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  2. Bruno Biatry
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  3. Colette Cazeneuve
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  4. Richard H. Guy
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Corresponding author

Correspondence to Richard H. Guy.

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Wu, X., Biatry, B., Cazeneuve, C. et al. Drug Delivery to the Skin From Sub-micron Polymeric Particle Formulations: Influence of Particle Size and Polymer Hydrophobicity. Pharm Res 26, 1995–2001 (2009). https://doi.org/10.1007/s11095-009-9915-1

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  • DOI: https://doi.org/10.1007/s11095-009-9915-1

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