多重乳液超分子微组装对其生物制药特性及体内治疗反应的影响

Title:Influence of the Supramolecular Micro-Assembly of Multiple Emulsions on their Biopharmaceutical Features and In vivo Therapeutic Response

Volume: 16 Issue: 14

Author(s): Felisa Cilurzo, Maria Chiara Cristiano, Luisa Di Marzio, Donato Cosco, Maria Carafa, Cinzia Anna Ventura, Massimo Fresta and Donatella Paolino

Affiliation:

关键词: 诱导发红反应，体外经皮渗透，体内疗效，烟酸甲酯，多重乳状液，反射光谱法，超分子微组装。

摘要: The ability of some surfactants to self-assemble in a water/oil bi-phase environment thus forming supramolecular structure leading to the formation of w/o/w multiple emulsions was investigated. The w/o/w multiple emulsions obtained by self-assembling (one-step preparation method) were compared with those prepared following the traditional two-step procedure. Methyl-nicotinate was used as a hydrophilic model drug. The formation of the multiple emulsion structure was evidenced by optical microscopy, which showed a mean size of the inner oil droplets of 6 μm and 10 μm for one-step and two-step multiple emulsions, respectively. The in vitro biopharmaceutical features of the various w/o/w multiple emulsion formulations were evaluated by means of viscosimetry studies, drug release and in vitro percutaneous permeation experiments through human stratum corneum and viable epidermis membranes. The self-assembled multiple emulsions allowed a more gradual percutaneous permeation (a zero-order permeation rate) than the two-step ones. The in vivo topical carrier properties of the two different multiple emulsions were evaluated on healthy human volunteers by using the spectrophotometry of reflectance, an in vivo non invasive method. These multiple emulsion systems were also compared with conventional emulsion formulations. Our findings demonstrated that the multiple emulsions obtained by self-assembling were able to provide a more sustained drug delivery into the skin and hence a longer therapeutic action than two-step multiple emulsions and conventional emulsion formulations. Finally, our findings showed that the supramolecular micro-assembly of multiple emulsions was able to influence not only the biopharmaceutical characteristics but also the potential in vivo therapeutic response.

Cite this article as:

Felisa Cilurzo, Maria Chiara Cristiano, Luisa Di Marzio, Donato Cosco, Maria Carafa, Cinzia Anna Ventura, Massimo Fresta and Donatella Paolino , Influence of the Supramolecular Micro-Assembly of Multiple Emulsions on their Biopharmaceutical Features and In vivo Therapeutic Response, Current Drug Targets 2015; 16 (14) . https://dx.doi.org/10.2174/138945011614151119124234