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.
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