Pep-1 peptide-conjugated elastic liposomal formulation of taxifolin glycoside for the treatment of atopic dermatitis in NC/Nga mice.
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.
Kang
Myung Joo
MJ
College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong, Dongjak-gu, Seoul 156 756, Republic of Korea.
Eum
Jae Yoon
JY
Park
Sang Han
SH
Kang
Mean Hyung
MH
Park
Kwan Hee
KH
Choi
Sun Eun
SE
Lee
Min Won
MW
Kang
Kyung Ho
KH
Oh
Chil Hwan
CH
Choi
Young Wook
YW
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
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