Khodir Wan Khartini Wan Abdul, Ismail Mohamad Wafiuddin, Hamid Shafida Abd, Daik Rusli, Susanti Deny, Taher Muhammad, Guarino Vincenzo
Department of Chemistry, Kulliyyah of Science, International Islamic University Malaysia Kuantan Campus, Bandar Indera Mahkota, Kuantan 25200, Pahang, Malaysia.
Synthetic and Functional Materials Research Group (SYNTOF), Kulliyyah of Science, International Islamic University Malaysia Kuantan Campus, Bandar Indera Mahkota, Kuantan 25200, Pahang, Malaysia.
Micromachines (Basel). 2023 Jul 6;14(7):1382. doi: 10.3390/mi14071382.
The administration of poorly water-soluble drugs represents a relevant problem due to the low body fluids transport efficiency through hydrophilic hydrogels. Star-shaped co-polymers, i.e., amphiphilic polymers such as those with a hydrophobic core and a hydrophilic outer shell, can be used to improve weak interactions with drugs, with relevant benefits in terms of administration and controlled delivery. In this work, two different co-polymers, four-arm star-shaped PCL-PEG and six-arm star-shaped PCL-PEG, were synthesized via ring-opening polymerization to be loaded with ciprofloxacin. H-NMR and FTIR analyses confirmed that PCL arms were successfully grafted to the mPEG backbone, while DSC analysis indicated similar crystallinity and melting point, ranging from 56 to 60 °C, independent of the different co-polymer architecture. Therefore, both star-shaped PCL-PEGs were investigated as cargo device for ciprofloxacin. No significant differences were observed in terms of drug entrapment efficiency (>95%) and drug release, characterized by a pronounced burst followed by a slow sustained release, only slightly affected by the co-polymer architecture. This result was also confirmed with curve fitting via the Korsmeyer-Peppas model. Lastly, good antibacterial properties and biocompatibility exhibited in both star-shaped PCL-PEG co-polymers suggest a promising use for oral delivery applications.
由于亲水性水凝胶对体液的运输效率较低,水溶性差的药物的给药是一个相关问题。星形共聚物,即两亲性聚合物,如具有疏水核心和亲水外壳的聚合物,可用于改善与药物的弱相互作用,在给药和控释方面具有相关益处。在这项工作中,通过开环聚合合成了两种不同的共聚物,四臂星形PCL-PEG和六臂星形PCL-PEG,用于负载环丙沙星。1H-NMR和FTIR分析证实PCL臂已成功接枝到mPEG主链上,而DSC分析表明结晶度和熔点相似,范围为56至60°C,与不同的共聚物结构无关。因此,两种星形PCL-PEG都被研究作为环丙沙星的载药装置。在药物包封效率(>95%)和药物释放方面未观察到显著差异,其特征是有明显的突释,随后是缓慢的持续释放,仅受共聚物结构的轻微影响。通过Korsmeyer-Peppas模型进行曲线拟合也证实了这一结果。最后,两种星形PCL-PEG共聚物均表现出良好的抗菌性能和生物相容性,这表明它们在口服给药应用中具有广阔的应用前景。