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基于明胶的水凝胶作为奥沙利铂结肠递药的潜在生物材料。

Gelatin-based hydrogels as potential biomaterials for colonic delivery of oxaliplatin.

机构信息

Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus 22060, Pakistan.

Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus 22060, Pakistan.

出版信息

Int J Pharm. 2019 Feb 10;556:236-245. doi: 10.1016/j.ijpharm.2018.12.020. Epub 2018 Dec 13.

Abstract

In present investigation, gelatin-based (AA-co-AMPS) hydrogels were prepared using N, N'-Methylenebisacrylamide (MBA) as a cross-linker and ammonium per sulfate (APS) as an initiator. The successful crosslinking and network formation was confirmed by Fourier transform infrared spectroscopy (FT IR). Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) investigations proved the higher thermal stability and successful entrapment of oxaliplatin (OXP) in the polymeric network. X-ray diffraction (XRD) confirmed the loss in crystallinity of the drug after loading in the hydrogel. Scanning electron microscopy (SEM) revealed the porous surface of the hydrogel. The newly formed hydrogels were responsive to change in pH. The swelling, drug loading and drug release was increased with increase in concentration of acrylic acid (AA) while gelatin and 2-acrylamido 2-methylpronesulfonic acid (AMPS) were found to act inversely. The in-vitro enzymatic degradation study showed that the blank hydrogels were more stable against the blank PBS than the collagenase and lysozyme. MTT-assay proved that the blank hydrogels were cyto-compatible while free OXP as well as OXP-loaded hydrogels showed dose dependent controlled cytotoxicity against Vero, MCF-7 and HCT-116 cell lines. The preliminary safety evaluation and oral tolerability showed that the hydrogel suspension was biocompatible and well tolerable upto 4000 mg/kg of body weight without causing any hematological or histopathological changes in rabbits.

摘要

在本研究中,使用 N,N'-亚甲基双丙烯酰胺(MBA)作为交联剂和过硫酸铵(APS)作为引发剂制备了基于明胶的(AA-co-AMPS)水凝胶。傅里叶变换红外光谱(FTIR)证实了成功的交联和网络形成。差示扫描量热法(DSC)和热重分析(TGA)研究证明了更高的热稳定性和奥沙利铂(OXP)在聚合物网络中的成功包埋。X 射线衍射(XRD)证实了药物在水凝胶中负载后结晶度的损失。扫描电子显微镜(SEM)显示了水凝胶的多孔表面。新形成的水凝胶对 pH 值的变化有响应。随着丙烯酸(AA)浓度的增加,水凝胶的溶胀、载药量和药物释放都增加,而明胶和 2-丙烯酰胺-2-甲基丙磺酸(AMPS)则表现出相反的作用。体外酶降解研究表明,空白水凝胶对空白 PBS 的稳定性高于胶原酶和溶菌酶。MTT 测定证明,空白水凝胶具有细胞相容性,而游离 OXP 以及负载 OXP 的水凝胶对 Vero、MCF-7 和 HCT-116 细胞系表现出剂量依赖性的可控细胞毒性。初步的安全性评价和口服耐受性表明,水凝胶混悬液具有生物相容性,在兔子体内高达 4000mg/kg 体重时耐受良好,不会引起任何血液学或组织病理学变化。

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