Sarfraz Muhammad, Tulain Ume Ruqia, Erum Alia, Malik Nadia Shamshad, Mahmood Arshad, Aslam Sidra, Sandhu Mansur Abdullah, Tayyab Muhammad
College of Pharmacy, Al Ain University, Al Ain Campus, Al Ain 64141, United Arab Emirates.
Faculty of Pharmacy, University of Sargodha, Punjab 40100, Pakistan.
Pharmaceutics. 2023 Oct 10;15(10):2445. doi: 10.3390/pharmaceutics15102445.
The primary objective of this study was to assess the potential utility of quince seed mucilage as an excipient within a graft copolymer for the development of an oral-controlled drug delivery system. The -mucilage-based graft copolymer was synthesized via a free radical polymerization method, employing potassium per sulfate (KPS) as the initiator and N, N-methylene bisacrylamide (MBA) as the crosslinker. Various concentrations of monomers, namely acrylic acid (AA) and methacrylic acid (MAA), were used in the graft copolymerization process. Metoprolol tartarate was then incorporated into this graft copolymer matrix, and the resultant drug delivery system was subjected to comprehensive characterization using techniques such as Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The swelling behavior of the drug delivery system was evaluated under different pH conditions, and in vitro drug release studies were conducted. Furthermore, pharmacokinetic parameters including the area under the curve (AUC), maximum plasma concentration (Cmax), time to reach Cmax (Tmax), and half-life (t1/2) were determined for metoprolol-loaded hydrogel formulations in rabbit plasma, and these results were compared with those obtained from a commercially available product. The key findings from the study include observations that higher concentrations of acrylic acid (AA) and mucilage (CM) in the graft copolymer enhanced swelling, while the opposite trend was noted at elevated concentrations of methacrylic acid (MAA) and N, N-methylene bisacrylamide (MBA). FTIR analysis confirmed the formation of the graft copolymer and established the compatibility between the drug and the polymer. SEM imaging revealed a porous structure in the prepared formulations. Additionally, the swelling behavior and drug release profiles indicated a pH-sensitive pattern. The pharmacokinetic assessment revealed sustained release patterns of metoprolol from the hydrogel network system. Notably, the drug-loaded formulation exhibited a higher Cmax (156.48 ng/mL) compared to the marketed metoprolol product (96 ng/mL), and the AUC of the hydrogel-loaded metoprolol was 2.3 times greater than that of the marketed formulation. In conclusion, this study underscores the potential of quince seed mucilage as an intelligent material for graft-copolymer-based oral-controlled release drug delivery systems.
本研究的主要目的是评估榅桲籽黏液作为接枝共聚物中的一种辅料用于开发口服控释给药系统的潜在效用。基于黏液的接枝共聚物通过自由基聚合法合成,使用过硫酸钾(KPS)作为引发剂,N,N - 亚甲基双丙烯酰胺(MBA)作为交联剂。在接枝共聚过程中使用了不同浓度的单体,即丙烯酸(AA)和甲基丙烯酸(MAA)。然后将酒石酸美托洛尔掺入该接枝共聚物基质中,并使用傅里叶变换红外光谱(FTIR)和扫描电子显微镜(SEM)等技术对所得药物递送系统进行全面表征。在不同pH条件下评估了药物递送系统的溶胀行为,并进行了体外药物释放研究。此外,还测定了兔血浆中载有美托洛尔的水凝胶制剂的药代动力学参数,包括曲线下面积(AUC)、最大血浆浓度(Cmax)、达到Cmax的时间(Tmax)和半衰期(t1/2),并将这些结果与市售产品的结果进行了比较。该研究的主要发现包括观察到接枝共聚物中较高浓度的丙烯酸(AA)和黏液(CM)会增强溶胀,而在甲基丙烯酸(MAA)和N,N - 亚甲基双丙烯酰胺(MBA)浓度升高时则观察到相反的趋势。FTIR分析证实了接枝共聚物的形成,并确定了药物与聚合物之间的相容性。SEM成像显示所制备制剂中存在多孔结构。此外,溶胀行为和药物释放曲线表明存在pH敏感模式。药代动力学评估显示美托洛尔从水凝胶网络系统中持续释放。值得注意的是,与市售美托洛尔产品(96 ng/mL)相比,载药制剂的Cmax更高(156.48 ng/mL),载有美托洛尔的水凝胶的AUC是市售制剂的2.3倍。总之,本研究强调了榅桲籽黏液作为基于接枝共聚物的口服控释药物递送系统的智能材料的潜力。