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Merck

Intradermal drug delivery by nanogel-peptide conjugates; specific and efficient transport of temoporfin.

Journal of controlled release : official journal of the Controlled Release Society (2016-07-30)
Fatemeh Zabihi, Sebastian Wieczorek, Mathias Dimde, Sarah Hedtrich, Hans G Börner, Rainer Haag
ABSTRACT

Nanogels offer many unique features rendering them as very attractive candidates for drug delivery. However, for their applications the loading capacity and specific encapsulation, in particular for hydrophobic drugs, in a complex media are two critical factors. In this work, we report for the first time on the preparation of nanogel-peptide conjugates with the ability of specific encapsulation of temoporfin (m-THPC). The peptide was selected based on combinatorial means and it was conjugated to polyglycerol as the nanogel precursor. We observed that the loading capacity of nanogels improved 16 times upon peptide conjugation. Skin penetrations tests in barrier deficient skin showed that nanogel-peptide conjugates enhance the penetration of m-THPC in the viable skin layers efficiently. This study indicates that nanogel-peptide conjugates could be used as unique carriers with high loading capacity for hydrophobic compounds, which provides the basis for the design of advanced topical drug delivery systems.

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N-(3-Dimethylaminopropyl)-N′-ethylcarbodiimide, ≥97.0% (T)
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HBTU, ≥98.0% (T)
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Fmoc-Leu-OH, ≥97.0%
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