School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.
Int J Pharm. 2014 Jun 5;467(1-2):9-18. doi: 10.1016/j.ijpharm.2014.03.045. Epub 2014 Mar 24.
The purpose of this study was to prepare and characterize nanoporous silica@poly(ethyleneimine)s (NS@P) xerogel and methanol modified NS@P xerogel synthesized with biomimetic method, and investigate controlled release behavior of propranolol hydrochloride (PNH) loaded carrier materials in vitro and in vivo. Preparation was conducted at ambient conditions, and NS@P xerogel as well as PNH loaded NS@P xerogel were characterized using Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD) and differential scanning calorimeter (DSC). Investigations on morphology and porous characteristics of NS@P xerogel and methanol modified NS@P xerogel were evaluated with scanning electron microscopy (SEM), transmission electron microscopy (TEM) and nitrogen adsorption. The results showed that the order of morphology compactness was NS@P xerogel>25%NS@P xerogel>75%NS@P xerogel because PEIs scaffold ability for silica condensation and forming hydrogen bond weakened with increasing volume ratio of methanol modification. Moreover, SBET decreased and uniformity of pore size distribution was interrupted after methanol modification. PNH loaded carrier materials displayed controlled release, and release effect was related with pore size of materials and PEIs scaffold ability. In vivo pharmacokinetic study demonstrated that release of PNH was delayed due to the PNH incorporated inside carrier materials and controlled release effect was in accordance with in vitro results.
本研究旨在制备和表征仿生法合成的纳米多孔硅@聚(亚乙基亚胺)(NS@P)气凝胶和甲醇改性 NS@P 气凝胶,并研究载有盐酸普萘洛尔(PNH)的载体材料在体外和体内的控制释放行为。制备在环境条件下进行,采用傅里叶变换红外光谱(FT-IR)、X 射线衍射(XRD)和差示扫描量热法(DSC)对 NS@P 气凝胶和负载 PNH 的 NS@P 气凝胶进行了表征。采用扫描电子显微镜(SEM)、透射电子显微镜(TEM)和氮吸附对 NS@P 气凝胶和甲醇改性 NS@P 气凝胶的形貌和多孔特性进行了研究。结果表明,由于甲醇改性增加了 PEI 缩合和形成氢键的能力减弱,形态致密性的顺序为 NS@P 气凝胶>25% NS@P 气凝胶>75% NS@P 气凝胶。此外,甲醇改性后 SBET 降低,孔径分布均匀性受到干扰。载药材料显示出控制释放,释放效果与材料的孔径和 PEI 的支架能力有关。体内药代动力学研究表明,由于 PNH 被包裹在载体材料内部,PNH 的释放被延迟,释放效果与体外结果一致。