Duggan Sarah, O'Donovan Orla, Owens Eleanor, Duggan Elaine, Hughes Helen, Cummins Wayne
Pharmaceutical and Molecular Biotechnology Research Centre, Department of Chemical and Life Sciences, Waterford Institute of Technology, Waterford, Ireland.
Pharmaceutical and Molecular Biotechnology Research Centre, Department of Chemical and Life Sciences, Waterford Institute of Technology, Waterford, Ireland.
Int J Pharm. 2016 Feb 10;498(1-2):245-53. doi: 10.1016/j.ijpharm.2015.12.036. Epub 2015 Dec 15.
Synthetic polymers, polyacrylic acid (PAA) and polyallylamine (PAAm), were thiolated using different methods of thiolation. Both polymers resulted in comparable thiol contents, thus allowing for the direct comparison of mucoadhesive and cohesive properties between the well-established thiolated PAA and the more novel thiolated PAAm. Thiolation of both polymers improved the swelling ability and the cohesive and mucoadhesive properties in comparison to unmodified control samples. In this study, it was shown that the swelling abilities of the thiolated PAAm sample were far greater than that of the thiolated PAA sample which, in turn, affected the drug release profile of the thiolated PAAm sample. Importantly, however, the mucoadhesive properties of thiolated PAAm were equivalent to that of the thiolated PAA sample as demonstrated by both the adhesion times on porcine intestinal tissue as measured by the rotating cylinder method and by rheological studies with a mucin solution. This study demonstrates the potential thiolated polyallylamine has as a mucoadhesive drug delivery device.
使用不同的硫醇化方法对合成聚合物聚丙烯酸（PAA）和聚烯丙胺（PAAm）进行硫醇化。两种聚合物的硫醇含量相当，因此可以直接比较成熟的硫醇化PAA和更新颖的硫醇化PAAm之间的粘膜粘附性和内聚性。与未改性的对照样品相比，两种聚合物的硫醇化均提高了溶胀能力以及内聚性和粘膜粘附性。在本研究中，结果表明硫醇化PAAm样品的溶胀能力远大于硫醇化PAA样品，这反过来又影响了硫醇化PAAm样品的药物释放曲线。然而，重要的是，通过旋转圆筒法测量的在猪肠道组织上的粘附时间以及用粘蛋白溶液进行的流变学研究表明，硫醇化PAAm的粘膜粘附性与硫醇化PAA样品相当。本研究证明了硫醇化聚烯丙胺作为粘膜粘附性药物递送装置的潜力。
