Carregant...
Fitxers
Tipus de document
ArticleVersió
Versió publicadaData de publicació
Llicència de publicació
Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/104356
Cyclic dipeptide shuttles as a novel skin penetration enhancement approach: preliminary evaluation with diclofenac
Títol de la revista
Director/Tutor
ISSN de la revista
Títol del volum
Recurs relacionat
Resum
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.
Matèries (anglès)
Citació
Citació
MOHAMMED, Yousuf, TEIXIDÓ TURÀ, Meritxell, NAMJOSHI, Sarika, GIRALT LLEDÓ, Ernest, BENSON, Heather. Cyclic dipeptide shuttles as a novel skin penetration enhancement approach: preliminary evaluation with diclofenac. _PLoS One_. 2016. Vol. 11, núm. 8, pàgs. e0160973. [consulta: 25 de febrer de 2026]. ISSN: 1932-6203. [Disponible a: https://hdl.handle.net/2445/104356]