氨基功能化介孔氧化硅材料的合成及药物缓释性能研究

采用水热的方法合成了3种不同孔径介孔氧化硅材料,并通过3-氨丙基三乙氧基硅烷对其进行表面修饰。采用TEM、N2吸附-脱附曲线、FT-IR以及元素分析等多种手段对材料进行表征。以阿霉素为模型药物,重点考察了孔径和表面功能化对材料药物吸附和缓释性能的影响。结果表明,孔径尺寸对药物的吸附性能影响不大,而对药物释放的影响较大,孔径越大,释放越快;氨基功能化材料的吸附性能较功能化前明显增强,其控制缓释行为更加明显。     

阿司匹林表面印迹微球的制备与药物缓释性能评价

采用表面印迹技术,选取γ-氨丙基三甲氧基硅烷(APTS)和甲基丙烯酰氯修饰的硅胶为载体,以阿司匹林(Asp)为模板分子,丙烯酰胺(AM)为功能单体,乙二醇二甲基丙烯酸酯(EDGMA)为交联剂,在乙腈溶液中合成了阿司匹林表面分子印迹聚合物微球(MIPs)和非印迹聚合物微球(NIPs)。通过紫外、红外光谱、扫描电镜、透射电镜、热重分析以及吸附实验进行了表征并进行了药物扩散实验。结果表明,MIPs平衡吸附量可达164.40μmol/g,对苯甲酸(BA)和水杨酸(SA)的分离因子达到3.15和3.32,有很好的热稳定性和选择性吸附能力;MIPs持续释药时间是NIPs的2.6倍,有很好的缓释效果和应用价值。     

Evaluation and Controlled Release Characteristics of Modified Xanthan Films for Transdermal Delivery of Atenolol

ABSTRACT

The present study was performed to evaluate the possibility of using modified xanthan films as a matrix system for transdermal delivery of atenolol (ATL), which is an antihypertensive drug. Acrylamide was grafted onto xanthan gum (XG) by free radical polymerization using ceric ion as an initiator. Fourier transform infrared spectroscopy and differential scanning calorimetry indicated the formation of the graft copolymer. The obtained graft copolymer was loaded with ATL and films were fabricated by solution casting method for transdermal application. Various formulations were prepared by varying the grafting ratio, drug loading, and different penetration enhancers. The formulations prepared were characterized for weight, thickness uniformity, water vapor transmission rate, and uniformity in drug content of the matrix. All the thin films were slightly opaque, smooth, flexible, and permeable to water vapor, indicating their permeability characteristics suitable for transdermal studies. Fourier transform infrared spectroscopy and differential scanning calorimetry studies indicated no significant interactions between drug and polymer. Drug is distributed uniformly in the matrix but showed a slight amorphous nature. Drug-loaded films were analyzed by X-ray diffraction to understand the drug polymorphism inside the films. Scanning electron microscopic studies of the placebo and drug-loaded films demonstrated a remarkable change in their surface morphology. The skin irritation tests were performed in mice and these results suggested that both placebo and drug-loaded films produced negligible erythema and edema compared to formalin (0.8% v/v) as the standard irritant. The in vitro drug release studies were performed in phosphate buffer saline using a Keshary-Chien diffusion cell. Different formulations were prepared and variations in drug release profiles were observed. Release data were analyzed by using the Ritger and Peppas equation to understand the mechanism of drug release as well as the estimation of n values, which ranged between 0.41 and 0.53, suggesting a Fickian diffusion trend.     

正己烷辅助合成小孔径大孔容介孔泡沫氧化硅材料

在正己烷-三嵌段共聚物(EO_(20)-PO_(70)-EO_(20),P123)体系中合成了小孔径大孔容介孔泡沫(MCF)氧化硅材料.采用高分辨扫描电镜、透射电镜、N_2吸附-脱附和小角XRD,对其孔道结构、型貌、比表面积、孔容等进行了表征.对合成条件的研究表明,在静置条件下水解TEOS合成的样品,其比表面积、孔径、孔容都比在搅拌下水解合成的样品明显增加,其中孔容可增加68%,达到2.32cm~3/g.     

Multi‐Responsive and Logic Controlled Release of DNA‐Gated Mesoporous Silica Vehicles Functionalized with Intercalators for Multiple Delivery

Novel DNA‐gated mesoporous silica nanoparticle (MSN) vehicles functionalized with disulfide‐linked acridinamine intercalators are constructed for multi‐responsive controlled release. The DNA‐gated MSN vehicles release cargo encapsulated in the MSN pores under different stimuli, including disulfide reducing agents, elevated temperature, and deoxyribonuclease I (DNase I), for codelivery of drugs and DNA/genes in different forms. Furthermore, the cascade release of encapsulated and intercalative drugs is controlled by AND logic gates in combination of dual stimuli. The ingeniously designed DNA‐gated MSN vehicles integrates multiple responses and AND logic gate operations into a single smart nanodevice not only for codelivery of drugs and DNA/genes but also for cascade release of two drugs and has promising biological applications to meet diverse requirements of controlled release.     

Gold Nanorods Coated with Mesoporous Silica Shell as Drug Delivery System for Remote Near Infrared Light‐Activated Release and Potential Phototherapy

In this study, we report the synthesis of a nanoscaled drug delivery system, which is composed of a gold nanorod‐like core and a mesoporous silica shell (GNR@MSNP) and partially uploaded with phase‐changing molecules (1‐tetradecanol, TD, T_m 39 °C) as gatekeepers, as well as its ability to regulate the release of doxorubicin (DOX). Indeed, a nearly zero premature release is evidenced at physiological temperature (37 °C), whereas the DOX release is efficiently achieved at higher temperature not only upon external heating, but also via internal heating generated by the GNR core under near infrared irradiation. When tagged with folate moieties, GNR@MSNPs target specifically to KB cells, which are known to overexpress the folate receptors. Such a precise control over drug release, combining with the photothermal effect of GNR cores, provides promising opportunity for localized synergistic photothermal ablation and chemotherapy. Moreover, the performance in killing the targeted cancer cells is more efficient compared with the single phototherapeutic modality of GNR@MSNPs. This versatile combination of local heating, phototherapeutics, chemotherapeutics and gating components opens up the possibilities for designing multifunctional drug delivery systems.     

New Triblock Copolymer Templates,PEO‐PB‐PEO,for the Synthesis of Titania Films with Controlled Mesopore Size,Wall Thickness,and Bimodal Porosity

The synthesis and properties of a series of new structure‐directing triblock copolymers with PEO‐PB‐PEO structure (PEO = poly(ethylene oxide) and PB = polybutadiene) and their application as superior pore‐templates for the preparation of mesoporous titania coatings are reported. Starting from either TiCl₄ or from preformed TiO₂ nanocrystalline building blocks, mesoporous crystalline titanium oxide films with a significant degree of mesoscopic ordered pores are derived, and the pore size can be controlled by the molecular mass of the template polymer. Moreover, the triblock copolymers form stable micelles already at very low concentration, i.e., prior to solvent evaporation during the evaporation‐induced self‐assembly process (EISA). Consequently, the thickness of pore walls can be controlled independently of pore size by changing the polymer‐to‐precursor ratio. Thus, unprecedented control of wall thickness in the structure of mesoporous oxide coatings is achieved. In addition, the micelle formation of the new template polymers is sufficiently distinct from that of typical commercial PPO‐PEO‐PPO polymers (Pluronics; PPO = poly(propylene oxide)), so that a combination of both polymers facilitates bimodal porosity via dual micelle templating.