Heck, Rouven;Lukic, Milica Z.;Savic, Snezana D.;Daniels, Rolf;Lunter, Dominique J. published 《Ex vivo skin permeation and penetration of nonivamide from and in vivo skin tolerability of film-forming formulations containing porous silica》 in 2017. The article was appeared in 《European Journal of Pharmaceutical Sciences》. They have made some progress in their research.Category: amides-buliding-blocks The article mentions the following:
The purpose of this study was to evaluate skin permeation and penetration of nonivamide which has been formulated in novel film-forming formulations (FFFs). These formulations aim to prolong the availability of capsaicinoids which are used in long-term treatment of chronic pruritus. An oily solution of nonivamide was loaded into porous silica particles which then were suspended in an aqueous dispersion of a sustained release polymer. Permeation and penetration experiments were performed ex vivo with postauricular porcine skin using modified Franz diffusion cells. The penetrated drug amount was assessed ex vivo by skin surface biopsy followed by cryo-sectioning. Furthermore, in vivo skin irritation experiments were performed to compare the potential skin irritation caused by the FFFs to conventionally used semi-solid formulations. Permeation rates of nonivamide from FFF through the skin are comparable to that from clin. used immediate release formulations. This elucidates the therapeutic safety profile of the novel FFF. Penetration studies confirmed the prolonged drug availability at the site of action. FFFs were found not to irritate the skin of healthy volunteers. FFFs with sustained nonivamide penetration represent safe and easy-to-use formulations. They therefore may improve the treatment of chronic pruritus with capsaicinoids by enhancing patient compliance through a sustained release regime. The experimental procedure involved many compounds, such as N-Vanillylnonanamide (cas: 2444-46-4) .
N-Vanillylnonanamide(cas:2444-46-4) is a capsaicin analog that has been used to study the effects of capsaicin on energy metabolism and bowel disease.Category: amides-buliding-blocks It has been shown to be effective in the treatment of bowel disease, by inhibiting the production of proinflammatory cytokines and prostaglandins.
Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics