4-hydroxy-n-desmethyltamoxifen and mangostin

Endoxifen, an anti-estrogenic agent, has been recently implicated in the use of breast cancer. Its physicochemical properties make it a good candidate for transdermal delivery. However, as an investigative drug, its limited supply makes it difficult to conduct extensive pre-formulation studies. To address this issue, a miniaturized flow-through diffusion cell has been fabricated that utilized minimal amounts of the drug for in vitro skin permeation studies. The novel flow-through cells have been validated against horizontal diffusion cells and shown to cause no noticeable damage to the applied skin, as observed by histological sectioning. The cells were also demonstrated to be useful in search of suitable enhancers for endoxifen. Endoxifen permeation using permeation enhancers was tested by using this new device and limonene was found to achieve highest flux, attaining the requirement for clinical applications. The fabricated cells can thus be useful in carrying out pre-formulation studies for expensive, new drug entities, both in industrial as well as academic research.

Topics: Animals; Cyclohexenes; Diffusion; Estrogen Antagonists; Excipients; In Vitro Techniques; Limonene; Models, Biological; Permeability; Rats; Rhodamines; Skin Absorption; Tamoxifen; Terpenes; Xanthones