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Characterization of Solid Maltose Microneedles and their Use for Transdermal Delivery

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Abstract

Purpose

To characterize solid maltose microneedles and assess their ability to increase transdermal drug delivery.

Materials and Methods

Microneedles and microchannels were characterized using methylene blue staining and scanning electron microscopy. Diffusion pattern of calcein was observed using confocal scanning laser microscopy. Transepidermal water loss (TEWL) measurements were made to study the skin barrier recovery after treatment. Uniformity in calcein uptake by the pores was characterized and percutaneous penetration of nicardipine hydrochloride (NH) was studied in vitro and in vivo across hairless rat skin.

Results

Microneedles were measured to be 508.46 ± 9.32 μm long with a radius of curvature of 3 μm at the tip. They penetrated the skin while creating microchannels measuring about 55.42 ± 8.66 μm in diameter. Microchannels were visualized by methylene blue staining. Pretreatment with microneedles resulted in the migration of calcein into the microchannels. TEWL increased after pretreatment and uptake of calcein by the pores was uniform as measured by the pore permeability index values. NH in vitro transport across skin increased significantly after pretreatment (flux 7.05 μg/cm2/h) as compared to the untreated skin (flux 1.72 μg/cm2/h) and the enhanced delivery was also demonstrated in vivo in hairless rats.

Conclusion

Maltose microneedles were characterized and shown to create microchannels in the skin, which were also characterized and shown to improve the transdermal delivery of NH.

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Abbreviations

NH:

Nicardipine hydrochloride

PPI:

Pore Permeability Index

SC:

Stratum corneum

SEM:

Scanning electron microscope

TEWL:

Transepidermal water loss

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Acknowledgements

Microneedles required for the study were developed and supplied by Texmac Inc. We thank Dr. Lisa Hoskin and Gautam Patel (Georgia Tech Research Institute, Atlanta, GA) for their help with SEM and Videomicroscope images; Janice Taylor, University of Nebraska Medical center (Omaha, NE) for help with confocal microscopy and David Farquhar, Altea Therapeutics (Tucker, GA), for help in image processing.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, 3001 Mercer University Drive, Atlanta, Georgia, 30341, USA

    Chandra Sekhar Kolli & Ajay K. Banga

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  1. Chandra Sekhar Kolli
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  2. Ajay K. Banga
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Correspondence to Ajay K. Banga.

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Kolli, C.S., Banga, A.K. Characterization of Solid Maltose Microneedles and their Use for Transdermal Delivery. Pharm Res 25, 104–113 (2008). https://doi.org/10.1007/s11095-007-9350-0

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  • DOI: https://doi.org/10.1007/s11095-007-9350-0

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