title: Pep-1 peptide-conjugated elastic liposomal formulation of taxifolin glycoside for the treatment of atopic dermatitis in NC/Nga mice.
abstract: In order to develop topical preparations of taxifolin glycoside (TXG) for the treatment of atopic dermatitis (AD), formulations of Pep-1 peptide-conjugated elastic liposomes (Pep1-EL) were examined for their in vitro skin permeation profile and in vivo therapeutic efficacy. TXG-loaded Pep1-EL - a nanovesicle consisting of phosphatidylcholine, Tween 80, N-[4-(p-maleimidophenyl)butyryl]-phosphatidylethanolamine (MPB-PE), and Pep-1 peptide - is 130nm in size, and has a zeta potential of 25mV and a deformability index value of 60. Here, we examined the skin permeability of several topical preparations using a Franz diffusion cell mounted with depilated mouse skin and found that formulations of Pep1-EL exhibited superior absorption when compared to aqueous solution, EL or Pep-1 peptide-admixed EL formulations. Both transepidermal water loss and skin surface hydration were also measured using AD-induced NC/Nga mice, and the TXG-loaded Pep1-EL treatment group displayed a significantly expedited recovery in skin barrier function when compared to the controls treated with a TXG aqueous solution (p<0.05). AD-associated immune responses - including serum interleukine-4, immunoglobulin E, and interferon-gamma - were also regulated by topical application of TXG-loaded Pep1-EL. In conclusion, the novel Pep1-EL formulation of TXG shows substantial promise in the treatment of AD as a result of its desirable skin delivery-promoting capability.
authors.affiliation: College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong, Dongjak-gu, Seoul 156 756, Republic of Korea.
authors.forename: Myung Joo
authors.initials: MJ
authors.lastname: Kang
authors.forename: Jae Yoon
authors.initials: JY
authors.lastname: Eum
authors.forename: Sang Han
authors.initials: SH
authors.lastname: Park
authors.forename: Mean Hyung
authors.initials: MH
authors.lastname: Kang
authors.forename: Kwan Hee
authors.initials: KH
authors.lastname: Park
authors.forename: Sun Eun
authors.initials: SE
authors.lastname: Choi
authors.forename: Min Won
authors.initials: MW
authors.lastname: Lee
authors.forename: Kyung Ho
authors.initials: KH
authors.lastname: Kang
authors.forename: Chil Hwan
authors.initials: CH
authors.lastname: Oh
authors.forename: Young Wook
authors.initials: YW
authors.lastname: Choi
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D003543:Cysteamine / Q000031:analogs & derivatives* / Q000737:chemistry; D003876:Dermatitis, Atopic / Q000188:drug therapy* / Q000276:immunology; D004195:Disease Models, Animal; D004337:Drug Carriers / Q000737:chemistry; D004548:Elasticity; D005079:Excipients / Q000737:chemistry; D005960:Glucosides / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D008081:Liposomes; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010455:Peptides / Q000737:chemistry*; D010539:Permeability; D011794:Quercetin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D012869:Skin Absorption
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D005079:Excipients; D005960:Glucosides; D008081:Liposomes; C503924:Pep-1 peptide; D010455:Peptides; C067156:taxifolin-3-glucopyranoside; D003543:Cysteamine; D011794:Quercetin