title: Intradermal drug delivery by nanogel-peptide conjugates; specific and efficient transport of temoporfin.
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.
authors.affiliation: Institute of Chemistry and Biochemistry, Freie Universität Berlin, Takustr. 3, D-14195 Berlin, Germany; Institute of Pharmacy (Pharmacology and Toxicology), Freie Universität Berlin, 14195 Berlin, Germany.
authors.forename: Fatemeh
authors.initials: F
authors.lastname: Zabihi
authors.affiliation: Department of Chemistry, Humboldt-Universität zu Berlin, Laboratory for Organic Synthesis of Functional Systems, Brook-Taylor-Str. 2, D-12489 Berlin, Germany.
authors.forename: Sebastian
authors.initials: S
authors.lastname: Wieczorek
authors.affiliation: Institute of Chemistry and Biochemistry, Freie Universität Berlin, Takustr. 3, D-14195 Berlin, Germany.
authors.forename: Mathias
authors.initials: M
authors.lastname: Dimde
authors.affiliation: Institute of Pharmacy (Pharmacology and Toxicology), Freie Universität Berlin, 14195 Berlin, Germany.
authors.forename: Sarah
authors.initials: S
authors.lastname: Hedtrich
authors.affiliation: Department of Chemistry, Humboldt-Universität zu Berlin, Laboratory for Organic Synthesis of Functional Systems, Brook-Taylor-Str. 2, D-12489 Berlin, Germany.
authors.forename: Hans G
authors.initials: HG
authors.lastname: Börner
authors.affiliation: Institute of Chemistry and Biochemistry, Freie Universität Berlin, Takustr. 3, D-14195 Berlin, Germany. Electronic address: haag@chemie.fu-berlin.de.
authors.forename: Rainer
authors.initials: R
authors.lastname: Haag
mesh_terms: D000279:Administration, Cutaneous; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005990:Glycerol / Q000737:chemistry; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008652:Mesoporphyrins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D053758:Nanoparticles; D010455:Peptides / Q000737:chemistry; D017319:Photosensitizing Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D011108:Polymers / Q000737:chemistry; D012869:Skin Absorption
chemical_list: D004337:Drug Carriers; D008652:Mesoporphyrins; D010455:Peptides; D017319:Photosensitizing Agents; D011108:Polymers; C043941:polyglycerol; C072269:temoporfin; D005990:Glycerol
keywords: Intradermal delivery; Nanogel; Peptide; Selective loading; Temoporfin