Tat peptide-admixed elastic liposomal formulation of hirsutenone for the treatment of atopic dermatitis in NC/Nga mice.

Abstract

BACKGROUND:

The aim of the present study was to enhance a topical delivery of hirsutenone (HST), a naturally occuring immunomodulator, employing Tat peptide-admixed elastic liposomes (EL/T).

METHODS:

HST-loaded EL, consisting of phosphatidylcholine and Tween 80 (85:15 w/w%), were prepared using thin film hydration method. By adding Tat peptide to EL (0.16 w/w%), EL/T were formulated. The in vitro skin permeation of HST was examined using a Franz diffusion cell mounted with depilated mouse skin. Lesions for atopic dermatitis (AD) were induced by a topical application of diphenylcyclopropenone to NC/Nga mice. Therapeutic improvements of AD were evaluated by clinical skin severity scores. Immunological analyses on inducible nitric oxide synthase and cyclooxygenase-2 levels in the skin and interleukin (IL)-4, IL-13, immunoglobulin E, and eosinophil levels in the blood were also performed.

RESULTS:

EL systems were superior to conventional cream, revealing greater flux values in a permeation study. The addition of Tat peptide further increased the skin permeation of HST. In an efficacy study with AD-induced NC/Nga mice, an HST-containing EL/T formulation brought a significant improvement in both skin severity score and immune-related responses for the levels of nitric oxide synthase, cyclooxygenase-2, IL-4, IL-13, immunoglobulin E, and eosinophils.

CONCLUSION:

A novel EL/T formulation was successfully developed for topical delivery of HST to treat AD.

• Authors: Myung Joo Kang, Jae Yoon Eum, Mi Sook Jeong, Sang Han Park, Ki Young Moon, Mean Hyung Kang, Min Soo Kim, Sun Eun Choi, Min Won Lee, Do Ik Lee, Hyoweon Bang, Chung Soo Lee, Seong Soo Joo, Kapsok Li, Mi-Kyung Lee, Seong Jun Seo, Young Wook Choi
• Journal: International journal of nanomedicine (Int J Nanomedicine) Vol. 6 Pg. 2459-67 ( 2011) ISSN: 1178-2013 [Electronic] New Zealand
• PMID: 22072881 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Catechols
• Diarylheptanoids
• Gene Products, tat
• Interleukin-13
• Liposomes
• Phosphatidylcholines
• Polysorbates
• hirsutenone
• Interleukin-4
• Immunoglobulin E
• Nitric Oxide Synthase
• Cyclooxygenase 2

Topics

• Animals
• Catechols (administration & dosage, chemistry, pharmacology)
• Cyclooxygenase 2 (metabolism)
• Dermatitis, Atopic (blood, drug therapy, metabolism)
• Diarylheptanoids (administration & dosage, chemistry, pharmacology)
• Eosinophils (drug effects, metabolism)
• Gene Products, tat (administration & dosage, chemistry, pharmacology)
• Immunoglobulin E (blood)
• Interleukin-13 (blood)
• Interleukin-4 (blood)
• Liposomes (administration & dosage, chemistry, pharmacology)
• Male
• Mice
• Nitric Oxide Synthase (metabolism)
• Phosphatidylcholines
• Polysorbates
• Skin Absorption (drug effects)