Sucrose cocoate, a component of cosmetic preparations, enhances nasal and ocular peptide absorption

Abstract

Sucrose cocoate (SL-40), an emulsifier employed in emollient, skin-moisturizing cosmetic formulations, contains a mixture of sucrose esters of coconut fatty acids in aqueous ethanol solution. In order to determine its potential utility in enhancing nasal and ocular drug delivery, absorption studies were performed in anesthetized Sprague-Dawley male rats with calcitonin and insulin, two distinct therapeutic peptides. Administration of a nasal insulin formulation containing 0.5% sucrose cocoate caused a rapid and significant increase in plasma insulin levels, with a concomitant decrease in blood glucose levels. When insulin was administered ocularly in the presence of 0.5% sucrose cocoate, a smaller increase in plasma insulin levels, and a decrease in blood glucose levels, were observed. Administration of a nasal calcitonin formulation containing 0.5% sucrose cocoate caused a rapid increase in plasma calcitonin levels and a concomitant decrease in plasma calcium levels. Mass spectrometric analyses were used to characterize the nature of the sucrose fatty acid esters in the mixture. The most abundant sucrose ester in sucrose cocoate was sucrose monododecanoate, with smaller amounts of sucrose monodecanoate and sucrose monotetradecanoate. In vivo experiments confirmed that this ester was an effective enhancer of nasal peptide drug absorption.