Mesoporous Silica Nanoparticles: Drug Delivery Vehicles for Antidiabetic Molecules

Mesoporous silica nanoparticles (MSNs) are promising nanomaterials that are widely used in biomedical applications like drug delivery, diagnosis, bio-sensing and cell tracking. MSNs have been investigated meticulously in the drug-delivery field due to their unique chemical and pharmacokinetic properties, such as highly ordered mesopores, high surface area and pore volume, tuneable pore size, stability, surface functionalisation, and biocompatibility. MSN-based nanocomposites have been used to deliver therapeutic molecules like insulin, GLP-1, exenatide, DPP-4 inhibitor and plasmid-containing GLP-1 genes for managing diabetes mellitus for the last decade. The functionalisation properties of MSNs make them substantially capable of the co-delivery, controlled delivery and stimuli-responsive delivery of antidiabetic drugs. This review focuses on the delivery of antidiabetic therapeutics with special emphasis on the functionalisation of MSNs and stimuli-responsive delivery.     

Triantennary GalNAc-Functionalized Multi-Responsive Mesoporous Silica Nanoparticles for Drug Delivery Targeted at Asialoglycoprotein Receptor

In recent years, mesoporous silica particles have been revealed as promising drug delivery systems combining high drug loading capacity, excellent biocompatibility, and easy and affordable synthetic and post-synthetic procedures. In fact, the straightforward functionalization approaches of these particles allow their conjugation with targeting moieties in order to surpass one of the major challenges in drug administration, the absence of targeting ability of free drugs that reduces their therapeutic efficacy and causes undesired side effects. In this context, the main goal of this work was to develop a new targeted mesoporous silica nanoparticle formulation with the capability to specifically and efficiently deliver an anticancer drug to hepatocellular carcinoma (HCC) cells. To this purpose, and as proof of concept, we developed redox-responsive mesoporous silica nanoparticles functionalized with the targeting ligand triantennary N-acetylgalactosamine (GalNAc) cluster, which has high affinity to asialoglycoprotein receptors overexpressed in HCC cells, and loaded them with epirubicin, an anthracycline drug. The produced nanocarrier exhibits suitable physicochemical properties for drug delivery, high drug loading capacity, high biocompatibility, and targeting ability to HCC cells, revealing its biopharmaceutical potential as a targeted drug carrier for therapeutic applications in liver diseases.     

Oral Drug Delivery Systems Based on Ordered Mesoporous Silica Nanoparticles for Modulating the Release of Aprepitant

Two different types of ordered mesoporous nanoparticles, namely MCM-41 and MCM-48, with similar pore sizes but different pore connectivity, were loaded with aprepitant via a passive diffusion method. The percentage of the loaded active agent, along with the encapsulation efficiency, was evaluated using High-performance Liquid Chromatography (HPLC) analysis complemented by Thermogravimetric Analysis (TGA). The determination of the pore properties of the mesoporous particles before and after the drug loading revealed the presence of confined aprepitant in the pore structure of the particles, while Powder X-ray Diffractometry(pXRD), Differential Scanning Calorimetry (DSC), and FTIR experiments indicated that the drug is in an amorphous state. The release profiles of the drug from the two different mesoporous materials were studied in various release media and revealed an aprepitant release up to 45% when sink conditions are applied. The cytocompatibility of the silica nanoparticles was assessed in Caco-2 cell monolayers, in the presence and absence of the active agent, suggesting that they can be used as carriers of aprepitant without presenting any toxicity in vitro.     

Acidity and Glutathione Dual-Responsive Polydopamine-Coated Organic-Inorganic Hybrid Hollow Mesoporous Silica Nanoparticles for Controlled Drug Delivery

Controversial biodegradability and nonspecific pre-drug leakage are major limitations for inorganic nanoparticles in cancer treatment. To solve these problems, we developed organic-inorganic hybridized hollow mesoporous silica nanoparticles with polydopamine modifications on the surface to simultaneously achieve enhanced biodegradability and controllable drug release. The morphology and chemical structure of the nanoparticles were characterized by TEM, N₂ adsorption-desorption isotherms, TEM-mapping and XPS. Moreover, the release behavior of nanoparticles under various pH conditions and the degradation behavior in the presence of GSH were evaluated. With effective controlled release, HMONs-PTX@PDA were shown to significantly inhibit cancer cell proliferation and achieve antitumor effects in vivo through dual-response release in the tumor microenvironment. Overall, this nanoplatform has significant potential to achieve tumor microenvironment-responsive degradation and release to enhance tumor accumulation, which is very promising for cancer treatment.     

Kidney-Protector Lipidic Cilastatin Derivatives as Structure-Directing Agents for the Synthesis of Mesoporous Silica Nanoparticles for Drug Delivery

Mesoporous silica nanomaterials have emerged as promising vehicles in controlled drug delivery systems due to their ability to selectively transport, protect, and release pharmaceuticals in a controlled and sustained manner. One drawback of these drug delivery systems is their preparation procedure that usually requires several steps including the removal of the structure-directing agent (surfactant) and the later loading of the drug into the porous structure. Herein, we describe the preparation of mesoporous silica nanoparticles, as drug delivery systems from structure-directing agents based on the kidney-protector drug cilastatin in a simple, fast, and one-step process. The concept of drug-structure-directing agent (DSDA) allows the use of lipidic derivatives of cilastatin to direct the successful formation of mesoporous silica nanoparticles (MSNs). The inherent pharmacological activity of the surfactant DSDA cilastatin-based template permits that the MSNs can be directly employed as drug delivery nanocarriers, without the need of extra steps. MSNs thus synthesized have shown good sphericity and remarkable textural properties. The size of the nanoparticles can be adjusted by simply selecting the stirring speed, time, and aging temperature during the synthesis procedure. Moreover, the release experiments performed on these materials afforded a slow and sustained drug release over several days, which illustrates the MSNs potential utility as drug delivery system for the cilastatin cargo kidney protector. While most nanotechnology strategies focused on combating the different illnesses this methodology emphasizes on reducing the kidney toxicity associated to cancer chemotherapy.     

二氧化硅介孔膜材料的研究进展及应用前景

重点介绍了国内外近年来在二氧化硅介孔膜的制备与应用方面的最新进展,并对其制备与应用研究前景进行了展望。     

介孔SiO_2表面的氨基修饰及吸附性能研究

以十六胺为模板剂、正硅酸乙酯为硅源合成了多孔球形结构的介孔SiO2,用γ-氨基丙基三乙氧基硅烷(ATES)对介孔SiO2进行了表面修饰,得到了氨基嫁接介孔ATES-SiO2。利用XRD、BET、IR等方法分别测定了SiO2和ATES-SiO2的结构与性质,结果表明-NH2已成功接枝于介孔ATES-SiO2的孔道内表面。在常温常压下测得介孔SiO2和ATES-SiO2对CO2的吸附量分别为0.93 mmol/g和4.87 mmol/g。     

基于介孔二氧化硅纳米颗粒的新型造影剂研究进展

介孔二氧化硅纳米颗粒作为一种新型的纳米材料,已成为多个领域的研究热点。本文综述了以介孔二氧化硅纳米颗粒为载体合成的新型造影剂的研究进展,重点阐述基于介孔二氧化硅纳米颗粒造影剂在肿瘤相关疾病磁共振成像、光学成像及超声成像等模式中的应用,并对其未来的发展趋势做了展望。     

Preparation of Folic Conjugated Magnetic Silica Mesoporous Nanoparticles and Their Encapsulated 10-HCPT Anticancer Behavior

Journal of Inorganic and Organometallic Polymers and Materials - A novel folate-decorated and magnetic mediated drug delivery system was fabricated by combining folate and magnetic nanoparticles to...     

pH敏感型改性葡聚糖/介孔硅纳米粒子载体的构建及药物控释性能的研究

基于肿瘤组织的弱酸性,本文报道了一种pH敏感型改性葡聚糖/介孔硅纳米粒子(MSN)复合药物载体系统。以MSN为药物存储器,通过pH敏感的亚胺键将氧化葡聚糖包覆在粒子表面得到载体。体外药物释放实验证明载体具备较好的pH敏感性,并具有一定的应用前景。     

Pore-Size Dependence of the Acidic Property of Mesoporous Silica FSM-16

The pore-size dependence of the acidic properties of mesoporous silica FSM-16 in the range from 1.8 to 3.8 nm was investigated with the catalysis of 2-butanol dehydration and using FTIR spectra of adsorbed pyridine. The activity was the highest for FSM-16 with a minimum pore diameter, and decreased with increasing pore size. Differences in the acid amounts of siliceous FSM-16 and the strength dependent on the pore diameter were not confirmed by FTIR characterization using pyridine as a probe molecule.     

硅石原料的物理性能和显微结构与相转变特性之关系

采用产自日本、中国、印度的硅石原料,对其物理性能及显微结构进行了研究。另外,把原料粉碎成所定粒度后进行成型,研究了烧成对热膨胀和相转变特性的影响。     

Design of Gelatin-Capped Plasmonic-Diatomite Nanoparticles with Enhanced Galunisertib Loading Capacity for Drug Delivery Applications

Inorganic diatomite nanoparticles (DNPs) have gained increasing interest as drug delivery systems due to their porous structure, long half-life, thermal and chemical stability. Gold nanoparticles (AuNPs) provide DNPs with intriguing optical features that can be engineered and optimized for sensing and drug delivery applications. In this work, we combine DNPs with gelatin stabilized AuNPs for the development of an optical platform for Galunisertib delivery. To improve the DNP loading capacity, the hybrid platform is capped with gelatin shells of increasing thicknesses. Here, for the first time, full optical modeling of the hybrid system is proposed to monitor both the gelatin generation, degradation, and consequent Galunisertib release by simple spectroscopic measurements. Indeed, the shell thickness is optically estimated as a function of the polymer concentration by exploiting the localized surface plasmon resonance shifts of AuNPs. We simultaneously prove the enhancement of the drug loading capacity of DNPs and that the theoretical modeling represents an efficient predictive tool to design polymer-coated nanocarriers.     

Synthesis of Gold-Platinum Core-Shell Nanoparticles Assembled on a Silica Template and Their Peroxidase Nanozyme Properties

Bimetallic nanoparticles are important materials for synthesizing multifunctional nanozymes. A technique for preparing gold-platinum nanoparticles (NPs) on a silica core template (SiO₂@Au@Pt) using seed-mediated growth is reported in this study. The SiO₂@Au@Pt exhibits peroxidase-like nanozyme activity has several advantages over gold assembled silica core templates (SiO₂@Au@Au), such as stability and catalytic performance. The maximum reaction velocity (V_max) and the Michaelis–Menten constants (K_m) were and 2.1 × 10⁻¹⁰ M⁻¹∙s⁻¹ and 417 µM, respectively. Factors affecting the peroxidase activity, including the quantity of NPs, solution pH, reaction time, and concentration of tetramethyl benzidine, are also investigated in this study. The optimization of SiO₂@Au@Pt NPs for H₂O₂ detection obtained in 0.5 mM TMB; using 5 µg SiO₂@Au@Pt, at pH 4.0 for 15 min incubation. H₂O₂ can be detected in the dynamic liner range of 1.0 to 100 mM with the detection limit of 1.0 mM. This study presents a novel method for controlling the properties of bimetallic NPs assembled on a silica template and increases the understanding of the activity and potential applications of highly efficient multifunctional NP-based nanozymes.     

Applications of Amine-functionalized Mesoporous Silica in Fine Chemical Synthesis

SBA-15 silica containing homogeneously distributed amine-functional groups and of fiber or platelet morphology was prepared through a modified co-condensation method using P123 copolymer as template under acidic condition. Synthetic factors which led to well-ordered mesoporous materials with high loadings of various amine groups were discussed. The resultant mesoporous materials were efficient base catalysts in Knoevenagel and Claisen–Schmidt addition reactions. The activities over SBA-15 materials with different amino-functional groups are compared. Moreover, the advantage of ordered large mesopores of SBA-15 in catalyzing liquid phase reactions was demonstrated, and the reaction rate could be further increased when SBA-15 was with platelet morphology and short mesochannels.     

介孔硅材料在止血应用方面的研究进展

介绍了介孔硅材料的类型以及合成方法,综述了以介孔硅材料为基材的止血材料的研究现状,主要包括介孔硅材料、介孔硅与有机材料的复合、介孔硅与金属离子材料的复合,介孔硅材料均显示了良好的止血和抗菌性能,最后展望了介孔硅与其他材料复合在止血应用方面的前景。     

Novel Hybrid Nanorod Carriers of Fluorescent Hydroxyapatite Shelled with Mesoporous Silica Effective for Drug Delivery and Cell Imaging

Development of biocompatible multifunctional nanocarriers is necessary for the success of theranostics. Here, we report a novel hybrid nanorod with self‐fluorescent property, high drug loading capacity, and good biocompatibility. Fluorescent hydroxyapatite (fHA) nanorod was ensheathed with mesoporous silica (mSi). The mSi shell was uniformly layered and was tunable in thickness (10–30 nm) over the fHA nanorod. Highly mesoporous structure of mSi shell facilitated the loading of a large quantity of biological molecules, as confirmed with fluorescein isothiocynate; ~1% loading for fHA increased to ~10% loading for fHA@mSi. The self‐fluorescent property of the fHA resulting from CO₂^.? radicals was well preserved in the fHA@mSi hybrid, as analyzed by photoluminescence and electron paramagnetic resonance property. Cellular toxicity of the fHA@mSi hybrid nanorod showed favorable cell viability (>90% viability of control) up to a concentration of ~40 μg/mL. Intracellular uptake rate of the hybrid nanorod was as high as 80–90%, as analyzed by fluorescent‐assisted cell sorter. Results demonstrate the newly developed fHA@mSi nanocarriers have great potential for the effective loading of therapeutic molecules and delivery within intracellular compartments in concert with a capacity for in situ imaging.     

PMMA/PHEA Interpenetrating Network Embedded With Iron Oxide Nanoparticles for Drug Delivery Applications

Semi-interpenetrating polymer networks (IPNs) are prepared from poly methyl methacrylate and 2-hydroxy ethyl acrylate networks with the presence of super-paramagnetic ferric oxide nanoparticles (<30 nm) through free radical polymerization. PMMA/PHEA semi-IPNs having blend ratio 60:40, 50:50, 40:60 (wt/wt) are characterized with respect to swelling, crosslink density, FTIR, DSC, TGA, SEM, and drug loading and drug release properties. Bactericidal effect on IPNs is checked by cell growth study of E. coli.     

有序介孔二氧化硅薄膜的制备及性能

以十六烷基三甲基溴化铵(CTAB)为模板剂,正硅酸乙酯为无机前驱体,在酸性条件下,采用溶胶-凝胶技术,用蒸发诱导自组装(EISA)工艺制备了二氧化硅透明介孔薄膜. 透射电子显微镜图显示热处理后的薄膜具有高度有序的六方相结构孔道;由椭偏仪测得热处理后薄膜的折射率低至1.18,厚度在180 nm左右;阻抗分析仪测得薄膜的介电常数为2.14. 薄膜经过六甲基二硅胺烷(HMDS)表面修饰后具有良好的疏水性能和热稳定性,作为低介电材料能更好满足工业需求.