Please use this identifier to cite or link to this item: http://hdl.handle.net/2445/104356
Title: Cyclic dipeptide shuttles as a novel skin penetration enhancement approach: preliminary evaluation with diclofenac
Author: Mohammed, Yousuf
Teixidó Turà, Meritxell
Namjoshi, Sarika
Giralt Lledó, Ernest
Benson, Heather
Keywords: Epidermis
Pell
Síntesi de pèptids
Cromatografia de líquids d'alta resolució
Epidermis
Skin
Peptide synthesis
High performance liquid chromatography
Issue Date: 22-Aug-2016
Publisher: Public Library of Science (PLoS)
Abstract: This study demonstrates the effectiveness of a peptide shuttle in delivering diclofenac into and through human epidermis. Diclofenac was conjugated to a novel phenylalanyl-N- methyl-naphthalenylalanine-derived diketopiperazine (DKP) shuttle and to TAT (a classical cell penetrating peptide), and topically applied to human epidermis in vitro . DKP and TAT effectively permeated into and through human epidermis. When conjugated to diclofenac, both DKP and TAT enhanced delivery into and through human epidermis, though DKP was significantly more effective. Penetration of diclofenac through human epidermis (to recep- tor) was increased by conjugation to the peptide shuttle and cell penetrating peptide with enhancement of 6x by DKP-diclofenac and 3x by TAT-diclofenac. In addition, the amount of diclofenac retained within the epidermis was significantly increased by peptide conjugation. COX-2 inhibition activity of diclofenac was retained when conjugated to DKP. Our study suggests that the peptide shuttle approach may offer a new strategy for targeted delivery of small therapeutic and diagnostic molecules to the skin.
Note: Reproducció del document publicat a: https://doi.org/10.1371/journal.pone.0160973
It is part of: PLoS One, 2016, vol. 11, num. 8, p. e0160973
Related resource: https://doi.org/10.1371/journal.pone.0160973
URI: http://hdl.handle.net/2445/104356
ISSN: 1932-6203
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)

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