Cyanocobalamin Ultraflexible Lipid Vesicles: Characterization and In Vitro Evaluation of Drug-Skin Depth Profiles

Pharmaceutics

M.Carmen Montesinos¹  Ana Melero²  Carmen Milián-Guimerá²  TeresaM. Garrigues²  Enrique Jornet-Mollá²  AntonioJosé Guillot²  Natalia Landsberg² 

[1] Department of Pharmacology, Faculty of Pharmacy, University of Valencia, Avda. Vicent Andrés Estellés s/n, 46100 Burjassot, Spain;Department of Pharmacy and Pharmaceutical Technology and Parasitology, Faculty of Pharmacy, University of Valencia, Avda. Vicent Andrés Estellés s/n, 46100 Burjassot, Spain;

关键词: cyanocobalamin;    vitamin B12;    atopic dermatitis;    psoriasis;    liposomes;    transferosomes;   

DOI  :  10.3390/pharmaceutics13030418

来源: DOAJ

【 摘 要 】

Atopic dermatitis (AD) and psoriasis are the most common chronic inflammatory skin disorders, which importantly affect the quality of life of patients who suffer them. Among other causes, nitric oxide has been reported as part of the triggering factors in the pathogenesis of both conditions. Cyanocobalamin (vitamin B₁₂) has shown efficacy as a nitric oxide scavenger and some clinical trials have given positive outcomes in its use for treating skin pathologies. Passive skin diffusion is possible only for drugs with low molecular weights and intermediate lipophilicity. Unfortunately, the molecular weight and hydrophilicity of vitamin B₁₂ do not predict its effective diffusion through the skin. The aim of this work was to design new lipid vesicles to encapsulate the vitamin B₁₂ to enhance its skin penetration. Nine prototypes of vesicles were generated and characterized in terms of size, polydispersity, surface charge, drug encapsulation, flexibility, and stability with positive results. Additionally, their ability to release the drug content in a controlled manner was demonstrated. Finally, we found that these lipid vesicle formulations facilitated the penetration of cyanocobalamin to the deeper layers of the skin. The present work shows a promising system to effectively administer vitamin B₁₂ topically, which could be of interest in the treatment of skin diseases such as AD and psoriasis.

【 授权许可】

Unknown