Sansom Institute for Health Research, Division of Health Sciences, University of South Australia, Adelaide.
Int J Nanomedicine. 2011;6:1245-51. doi: 10.2147/IJN.S19151. Epub 2011 Jun 20.
Poorly water-soluble drugs, such as phenylephrine, offer challenging problems for buccal drug delivery. In order to overcome these problems, particle size reduction (to the nanometer range) and cyclodextrin complexation were investigated for permeability enhancement. The apparent solubility in water and the buccal permeation of the original phenylephrine coarse powder, a phenylephrine-cyclodextrin complex and phenylephrine nanosuspensions were characterized. The particle size and particle surface properties of phenylephrine nanosuspensions were used to optimize the size reduction process. The optimized phenylephrine nanosuspension was then freeze dried and incorporated into a multi-layered buccal patch, consisting of a small tablet adhered to a mucoadhesive film, yielding a phenylephrine buccal product with good dosage accuracy and improved mucosal permeability. The design of the buccal patch allows for drug incorporation without the need to change the mucoadhesive component, and is potentially suited to a range of poorly water-soluble compounds.
对于口腔给药来说，水溶性差的药物（如苯肾上腺素）是一个挑战。为了克服这些问题，研究了粒径减小（达到纳米级）和环糊精络合来提高渗透性。对原始苯肾上腺素粗粉、苯肾上腺素-环糊精复合物和苯肾上腺素纳米混悬液的表观溶解度和口腔渗透进行了表征。使用苯肾上腺素纳米混悬液的粒径和颗粒表面特性来优化减小粒径的过程。然后将优化的苯肾上腺素纳米混悬液冷冻干燥并纳入多层口腔贴片中，该贴片由粘附在粘膜黏附膜上的小片剂组成，得到具有良好剂量准确性和改善的粘膜渗透性的苯肾上腺素口腔产品。口腔贴片的设计允许在不改变粘膜黏附成分的情况下加入药物，并且可能适用于一系列水溶性差的化合物。
