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538. Redox-Responsive Nanocarrier for Controlled Release of Drugs in Inflammatory Skin Diseases

K. Rajes, K. A. Walker, S. Hadam, F. Zabihi, F. Rancan, A. Vogt, R. Haag – 2021

A synthetic route for redox-sensitive and non-sensitive core multi-shell (CMS) carriers with sizes below 20 nm and narrow molecular weight distributions was established. Cyclic voltammetric measurements were conducted characterizing the redox potentials of reduction-sensitive CMS while showcasing its reducibility through glutathione and tris(2-carboxyethyl)-phosphine as a proof of concept. Measurements of reduction-initiated release of the model dye Nile red by time-dependent fluorescence spectroscopy showed a pronounced release for the redox-sensitive CMS nanocarrier (up to 90% within 24 h) while the non-sensitive nanocarriers showed no release in PBS. Penetration experiments using ex vivo human skin showed that the redox-sensitive CMS nanocarrier could deliver higher percentages of the loaded macrocyclic dye meso-tetra (m-hydroxyphenyl) porphyrin (mTHPP) to the skin as compared to the non-sensitive CMS nanocarrier. Encapsulation experiments showed that these CMS nanocarriers can encapsulate dyes or drugs with different molecular weights and hydrophobicity. A drug content of 1 to 6 wt% was achieved for the anti-inflammatory drugs dexamethasone and rapamycin as well as fluorescent dyes such as Nile red and porphyrins. These results show that redox-initiated drug release is a promising strategy to improve the topical drug delivery of macrolide drugs.

Title
538. Redox-Responsive Nanocarrier for Controlled Release of Drugs in Inflammatory Skin Diseases
Author
K. Rajes, K. A. Walker, S. Hadam, F. Zabihi, F. Rancan, A. Vogt, R. Haag
Date
2021
Identifier
DOI: 10.3390/pharmaceutics13010037
Source(s)
Citation
Pharmaceutics, 2021, 13 (1), 37
Type
Text