Department of Pharmacy, School of Applied Sciences, University of Huddersfield, Huddersfield, UK.
Department of Pharmacy, School of Applied Sciences, University of Huddersfield, Huddersfield, UK.
Int J Biol Macromol. 2020 Jul 15;155:835-845. doi: 10.1016/j.ijbiomac.2020.03.227. Epub 2020 Mar 30.
This study aims to explore the potential of gum extracted from okra fruit (Hibiscus esculentus) in developing hydrophilic matrices for controlled drug release applications, including determination of its percolation threshold. Flurbiprofen (poorly soluble), theophylline (sparingly soluble) and metformin (freely soluble) were employed as model drugs and incorporated using direct compression into matrices containing 40% w/w of three drugs with different physicochemical properties. Atomic force microscopy was used to study the surface texture properties of developed matrices; the surfaces of the flurbiprofen-based matrices were comparatively rough most likely as a consequence of its poor compactability. Swelling studies found that the swelling rate increased as the concentration of okra gum was increased. However, for all matrices, an increase in the gum concentration resulted in decreased drug release. The estimated percolation threshold of the okra gum calculated was found in the region of ~25% v/v plus initial porosity. Knowing the percolation threshold will enable formulators to use the minimal amount of polymer for sustain release matrices thus the controlling costs and maximising the sustainable potential of okra. This study will not only assist researchers in developing effective okra gum-based extended-release matrices but also expected to contribute towards its exploration at an industrial scale.
本研究旨在探索从秋葵果实(Hibiscus esculentus)中提取的胶体制备亲水性基质用于控制药物释放的潜力,包括测定其渗透阈值。氟比洛芬(难溶性)、茶碱(微溶性)和二甲双胍(游离溶解)被用作模型药物,并通过直接压缩的方式掺入含有 40%w/w 三种具有不同理化性质的药物的基质中。原子力显微镜用于研究开发的基质的表面纹理特性;基于氟比洛芬的基质表面相对较粗糙,这很可能是由于其压缩性差所致。溶胀研究发现,随着秋葵胶浓度的增加,溶胀率增加。然而,对于所有基质,胶浓度的增加导致药物释放减少。计算出的秋葵胶的估计渗透阈值位于约 25%v/v 加上初始孔隙率的区域内。了解渗透阈值将使配方设计师能够在持续释放基质中使用最小量的聚合物,从而控制成本并最大化秋葵的可持续潜力。这项研究不仅将帮助研究人员开发有效的基于秋葵胶的延长释放基质,而且有望为其在工业规模上的探索做出贡献。