University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre utca 7-9, H-1092 Budapest, Hungary.
Institute of Organic Chemistry, Research Centre for Natural Sciences, Hungarian Academy of Sciences, Magyar tudósok körútja 2, H-1117 Budapest, Hungary.
Eur J Pharm Sci. 2018 Sep 15;122:9-12. doi: 10.1016/j.ejps.2018.06.020. Epub 2018 Jun 20.
Papaverine hydrochloride loaded gels, films and electrospun fibers were prepared for buccal drug delivery with the aim of improving the oral bioavailability of the crystalline drug, which can be achieved by the increased solubility and by the circumvention of the intensive first pass metabolism. The water soluble hydroxypropyl cellulose (HPC) was chosen as a mucoadhesive polymer. In order to improve the electrospinnability of HPC, the similarly mucoadhesive poly(vinyl alcohol) (PVA) was used. Since the drying of gels is of decisive role in either the formation of drug-loaded cast films or electrospun fibers, a real time ortho-positronium (o-Ps) tracking of gels was applied in order to obtain information about the supramolecular changes of the drying-induced gel-film transition. An anomalous increase of o-Ps lifetime value in the gel-film transition region was observed which refers to the remaining intramolecularly bound water in the drug-loaded polymeric gel matrix. The latter could provide information about the characteristics of polymer-water interactions in the phase transition, consequently the storage stability of the formulated solid system.
盐酸罂粟碱凝胶、薄膜和静电纺纤维被制备用于口腔药物输送，目的是提高结晶药物的口服生物利用度，这可以通过增加溶解度和绕过密集的首过代谢来实现。水溶性羟丙基纤维素 (HPC) 被选为粘膜粘附聚合物。为了提高 HPC 的可纺性，同样具有粘膜粘附性的聚乙烯醇 (PVA) 被使用。由于凝胶的干燥对于载药浇铸薄膜或静电纺纤维的形成起着决定性的作用，因此应用实时正电子素 (o-Ps) 跟踪凝胶以获得关于干燥诱导的凝胶-薄膜转变的超分子变化的信息。在凝胶-薄膜转变区域观察到 o-Ps 寿命值的异常增加，这是指载药聚合物凝胶基质中残留的分子内结合水。后者可以提供有关相变中聚合物-水相互作用特征的信息，从而提供所制定的固体系统的储存稳定性。
