Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.
Department of Chemistry and Chemical Technologies, University of Calabria, Via P. Bucci Edificio Polifunzionale, 87036 Arcavacata di Rende, Cosenza, Italy.
J Pharm Sci. 2021 Apr;110(4):1676-1686. doi: 10.1016/j.xphs.2020.10.033. Epub 2020 Oct 22.
Buccal matrices represent a widely accepted dosage form permitting a convenient, easy, reliable drug administration and reducing administration errors. The aim of this study was the development of mucoadhesive buccal matrices for propranolol administration in children. Matrices were obtained by freeze-drying of drug loaded polymeric solutions based on gum tragacanth (GT), pectin (PEC), hydroxypropylmethylcellulose (HPMC), sodium hyaluronate (HA), gelatin (GEL), chitosan (CH) or a mixture of CH and HPMC (CH/HPMC). Matrices were characterized for drug solid state, morphology, water-uptake, mucoadhesion ability, in vitro drug release and permeation through porcine epithelium. The most promising formulations were tested for in vitro biocompatibility in human dental pulp fibroblasts. The preparative method and the polymeric composition influenced the drug solid state, as a complete amorphization as well as different polymorphic forms were observed. GEL and PEC guaranteed a fast and complete drug release due to their rapid dissolution, while for the other matrices the release was influenced by drug diffusion through the viscous gelled matrix. Moreover, matrices based on CH and CH/HPMC showed the best mucoadhesive properties, favoured the drug permeation, in virtue of CH ability to interfere with the lipid organization of biological membrane, and were characterized by a good biocompatibility profile.
颊黏膜片代表了一种广泛接受的剂型,它可以方便、轻松、可靠地给药,并减少给药错误。本研究的目的是开发用于儿童普萘洛尔给药的粘膜粘附颊黏膜片。通过冷冻干燥基于刺槐豆胶(GT)、果胶(PEC)、羟丙基甲基纤维素(HPMC)、透明质酸钠(HA)、明胶(GEL)、壳聚糖(CH)或 CH 和 HPMC 的混合物的载药聚合物溶液来获得基质(CH/HPMC)。对基质的药物固体状态、形态、吸水率、粘膜粘附能力、体外药物释放和通过猪上皮的渗透进行了表征。对最有前途的制剂进行了人牙髓成纤维细胞体外生物相容性测试。制备方法和聚合物组成影响药物的固体状态,因为观察到完全非晶态和不同的多晶型。GEL 和 PEC 由于其快速溶解而保证了药物的快速和完全释放,而对于其他基质,释放受到药物通过粘性凝胶基质扩散的影响。此外,基于 CH 和 CH/HPMC 的基质表现出最好的粘膜粘附性能,有利于药物渗透,这得益于 CH 干扰生物膜脂质组织的能力,并且具有良好的生物相容性特征。