Abstract | BACKGROUND: OBJECTIVE: Development of novel topical formulation of levocetirizine based on flexible vesicles (FVs) with an aim to have targeted peripheral antihistaminic effect. MATERIALS AND METHODS: The FVs were prepared by thin film hydration method and characterized for drug content, entrapment efficiency, pH, vesicular size, spreadability, morphological characteristics and drug leakage studies. Franz diffusion cell assembly was used to carry out the ex vivo permeation studies through mice skin and the permeation profile of the developed FV formulation was compared with conventional formulations of levocetirizine. RESULTS AND DISCUSSION: The ex vivo permeation studies revealed 1.78-fold increase in percent permeation of levocetirizine from FV formulation as compared to conventional formulations of levocetirizine in 8 h. Further, oxazolone induced atopic dermatitis murine model was selected to study the in vivo pharmacodynamic activity. The developed formulation was evaluated for scratching score, erythema score and histological evaluation. There was marked reduction in scratching score from 15.25 scratches/20 min with conventional levocetirizine cream to 6.75 scratches/20 min with application of levocetirizine FV formulation. Also, there was significant reduction in erythema score as well as dermal eosinophil count. Results of skin sensitivity and toxicity studies suggest that the developed formulation was dermally safe and nontoxic. CONCLUSION:
|
Authors | Shishu Goindi, Gautam Kumar, Amanpreet Kaur |
Journal | Journal of liposome research
(J Liposome Res)
Vol. 24
Issue 3
Pg. 249-57
(Sep 2014)
ISSN: 1532-2394 [Electronic] England |
PMID | 24646413
(Publication Type: Journal Article)
|
Chemical References |
- Liposomes
- Oxazolone
- levocetirizine
- Cetirizine
|
Topics |
- Administration, Cutaneous
- Animals
- Cetirizine
(administration & dosage)
- Chemistry, Pharmaceutical
- Dermatitis, Atopic
(chemically induced, drug therapy, pathology)
- Elasticity
- Female
- Liposomes
(therapeutic use)
- Mice, Inbred BALB C
- Oxazolone
- Skin
(metabolism)
|