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Investigation of Follicular and Non-follicular Pathways for Polyarginine and Oleic Acid-Modified Nanoparticles

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Abstract

Purpose

To investigate the percutaneous permeation pathways of cell penetrating peptide modified lipid nanoparticles and oleic acid modified polymeric nanoparticles.

Methods

Confocal microscopy was performed on skin cultures (EpiDermFT™) for modified and un-modified nanoparticles. Differential stripping was performed following in vitro skin permeation of Ibuprofen (Ibu) encapsulated nanoparticles to estimate Ibu levels in different skin layers and receiver compartment. The hair follicles (HF) were blocked and in vitro skin permeation of nanoparticles was then compared with unblocked HF. The surface modified nanoparticles were investigated for response on allergic contact dermatitis (ACD).

Results

Surface modified nanoparticles showed a significant higher (p < 0.05) in fluorescence in EpiDermFT™ cultures compared to controls. The HF play less than 5% role in total nanoparticle permeation into the skin. The Ibu levels were significantly high (p < 0.05) for surface modified nanoparticles compared to controls. The Ibu levels in skin and receiver compartment were not significantly different when HF were open or closed. Modified nanoparticles showed significant improvement in treatment of ACD compared to solution.

Conclusions

Our studies demonstrate that increased skin permeation of surface modified nanoparticles is not only dependent on a follicular pathway but also occur through non-follicular pathway(s).

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Abbreviations

CLSM:

confocal laser scanning microscopy

CPP:

cell Penetrating Peptide

DiO-NLC:

DiO-dye encapsulated NLC

DiO-NLC-R11:

polyarginine-11 (R11) coated DiO-NLC

DiO-NLC-YKA:

YKA coated DiO-NLC

DiO-NPS:

DiO encapsulated NPS

DiO-NPS+OA (PM):

DiO-NPS with OA physical mixture

DiO-NPS-OA:

OA coated DiO-NPS

DiO-Sol:

DiO containing solution

DXM:

dexamethasone

HF:

hair follicle

Ibu:

ibuprofen

Ibu-NLC:

Ibu-encapsulated NLC

Ibu-NLC-R11:

polyarginine-11 (R11) coated Ibu-NLC

Ibu-NLC-YKA:

YKA coated Ibu-NLC

Ibu-NPS:

Ibu-encapsulated NPS

Ibu-NPS+OA (PM):

Ibu-NPS with OA physical mixture

Ibu-NPS-OA:

OA coated Ibu-NPS

Ibu-Sol:

Ibu containing solution

NHEK:

normal human epidermal keratinocyte

NLC:

nano structured lipid carrier

NPS:

polymeric bilayered nanoparticles

OA:

oleic acid

PLGA:

poly(lactic-co-glycolic acid)

SC:

stratum corneum

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Acknowledgments and Disclosures

This project was supported by the National Center for Research Resources and the National Institute of Minority Health and Health Disparities of the National Institutes of Health through Grant Number 8 G12 MD007582-28 and 2 G12 RR003020. Pinaki R. Desai and Punit P. Shah contributed equally to this work.

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Authors and Affiliations

  1. College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, 1520 S MLK Jr. Blvd., Tallahassee, Florida, 32307, USA

    Pinaki R. Desai, Punit P. Shah & Mandip Singh

  2. MatTek Corporation, 200 Homer Avenue, Ashland, Massachusetts, 01721, USA

    Patrick Hayden

Authors
  1. Pinaki R. Desai
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  2. Punit P. Shah
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  3. Patrick Hayden
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  4. Mandip Singh
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Correspondence to Mandip Singh.

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Desai, P.R., Shah, P.P., Hayden, P. et al. Investigation of Follicular and Non-follicular Pathways for Polyarginine and Oleic Acid-Modified Nanoparticles. Pharm Res 30, 1037–1049 (2013). https://doi.org/10.1007/s11095-012-0939-6

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  • DOI: https://doi.org/10.1007/s11095-012-0939-6

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