聚合物胶束型抗癌药物给药系统研究进展

综述了聚合物胶束的性质、制备、以及影响胶束性能的因素,对聚合物胶束在抗肿瘤药物药系统中的研究实例作了简要介绍。     

The Effect of pH and Sodium Caseinate on the Aqueous Solubility,Stability, and Crystallinity of Rutin towards Concentrated Colloidally Stable Particles for the Incorporation into Functional Foods

Poor water solubility and low bioavailability of hydrophobic flavonoids such as rutin remain as substantial challenges to their oral delivery via functional foods. In this study, the effect of pH and the addition of a protein (sodium caseinate; NaCas) on the aqueous solubility and stability of rutin was studied, from which an efficient delivery system for the incorporation of rutin into functional food products was developed. The aqueous solubility, chemical stability, crystallinity, and morphology of rutin (0.1–5% w/v) under various pH (1–11) and protein concentrations (0.2–8% w/v) were studied. To manufacture the concentrated colloidally stable rutin–NaCas particles, rutin was dissolved and deprotonated in a NaCas solution at alkaline pH before its subsequent neutralisation at pH 7. The excess water was removed using ultrafiltration to improve the loading capacity. Rutin showed the highest solubility at pH 11, while the addition of NaCas resulted in the improvement of both solubility and chemical stability. Critically, to achieve particles with colloidal stability, the NaCas:rutin ratio (w/w) had to be greater than 2.5 and 40 respectively for the lowest (0.2% w/v) and highest (4 to 8% w/v) concentrations of NaCas. The rutin–NaCas particles in the concentrated formulations were physically stable, with a size in the range of 185 to 230 nm and zeta potential of −36.8 to −38.1 mV, depending on the NaCas:rutin ratio. Encapsulation efficiency and loading capacity of rutin in different systems were 76% to 83% and 2% to 22%, respectively. The concentrated formulation containing 5% w/v NaCas and 2% w/v rutin was chosen as the most efficient delivery system due to the ideal protein:flavonoid ratio (2.5:1), which resulted in the highest loading capacity (22%). Taken together, the findings show that the delivery system developed in this study can be a promising method for the incorporation of a high concentration of hydrophobic flavonoids such as rutin into functional foods.     

Synthesis and aggregational behavior of acidic proteinoid

Polypeptide-based acidic proteinoid containing L -glutamic acid and L -aspartic acid in excess and five other neutral and basic amino acids in minor proportions have been synthesized and found that it forms organized aggregates in an aqueous solution. The proteinoid aggregate has been characterized using ¹³C-NMR, IR, and fluorescence spectroscopic techniques. The c.m.c. of the proteinoid has been determined by conductometric and pH metric methods. The aggregation studies were carried out at different temperatures and varying ionic strengths of the medium. The phase transition of the proteinoid aggregate has been determined using the fluorescence absorbance method. The aggregation behavior is shown to be dependent on the pH of the solution. This was also supported by conductivity measurements. Using methylene blue as a model drug, the drug delivery property of the proteinoid micelles were studied in acidic (pH 4.5) and neutral (pH 7.4) mediums. Using biphasic model thermochemical parameters, ΔG, ΔH, ΔS, and ΔC_p have been evaluated. © 1996 John Wiley & Sons, Inc.     

新一代的业务交付平台架构研究

本文首先详细介绍了业务交付平台(service delivery platform,SDP)的架构,重点描述了SDP的分层结构、组成和功能,然后介绍了基于SDP/IMS的融合业务方案.最后本文提出了新一代的SDP的架构,指出SDP的水平分层结构在促进网络能力集的开放、网络融合和业务融合等方面对电信运营商建设新一代的业务管理平台具有较好的参考价值.     

Porphyrin-like porous nanomaterials as drug delivery systems for ibuprofen drug

In recent years, nanomaterial-based drug delivery carriers have become some of the most attractive to be studied. The purpose of this study is to investigate the interaction of C60 fullerene, carbon nanotube and graphene having porphyrin-like FeN4 clusters with a non-steroidal anti-inflammatory drug (ibuprofen) by means of the density functional theory. Results showed that the graphene with FeN4 clusters could remarkably increase the tendency of graphene for adsorption of ibuprofen drug. Also, our ultraviolet–visible results show that the electronic spectra of the complexes exhibit a blue shift toward lower wavelengths (higher energies). It was found that Ibp/FeN4-graphene had high chemical reactivity, which was important for binding of the drug onto the target site. In order to go further and gain insight into the binding features of considered systems with ibuprofen drug, the Atoms in Molecules analysis was performed. Our results determine the electrostatic features of the Ibp/FeN4-graphene bonding. Consequently, the results demonstrated that the FeN4-graphene could be used as potential carriers for the delivery of ibuprofen drug.     

Leucine-coated cobalt ferrite nanoparticles: Synthesis,characterization and potential biomedical applications for drug delivery

This work was primarily focused on the synthesis, characterization and biomedical applications of cobalt ferrite (CoFe₂O₄) nanoparticles, which were synthesized by a facile solvothermal method using an amino acid of Leucine (Leu) as the surface coating agents. The morphology, structure and properties of the as-synthesized uncoated and Leu-coated CoFe₂O₄ nanoparticles were characterized in detail by means of XRD, SEM, TEM, DLS, FTIR, XPS, TGA and SQUID. More importantly, it was found that the Leu-coated CoFe₂O₄ nanoparticles can be used as the efficient drug delivery with a drug loading capacity of 0.32 mg/mg for doxorubicin hydrochloride (DOX), and the loaded DOX demonstrated a sustained and progressive release manner. The in vitro cytotoxicity studies towards the HeLa cells were carried out, and the results indicated that the Leu-coated CoFe₂O₄ nanoparticles exhibited a relatively high cell viability compared with that of bare CoFe₂O₄ nanoparticles and the DOX loaded Leu-coated CoFe₂O₄ nanoparticles presented an obvious cytotoxic effect on HeLa cells.     

Mesoporous materials for drug delivery

Research on mesoporous materials for biomedical purposes has experienced an outstanding increase during recent years. Since 2001, when MCM-41 was first proposed as drug-delivery system, silica-based materials, such as SBA-15 or MCM-48, and some metal-organic frameworks have been discussed as drug carriers and controlled-release systems. Mesoporous materials are intended for both systemic-delivery systems and implantable local-delivery devices. The latter application provides very promising possibilities in the field of bone-tissue repair because of the excellent behavior of these materials as bioceramics. This Minireview deals with the advances in this field by the control of the textural parameters, surface functionalization, and the synthesis of sophisticated stimuli-response systems.     

Characterization of a Multi-responsive Magnetic Graphene Oxide Nanocomposite Hydrogel and Its Application for DOX Delivery

Nanocomposite hydrogels are one of the most important types of biomaterials which can be used in many different applications such as drug delivery and tissue engineering.Incorporation of nanoparticles within a hydrogel matrix can provide unique characteristics like remote stimulate and improved mechanical strength.In this study,the synthesis of graphene oxide and graphene oxide nanocomposite hydrogel has been studied.Nanocomposite hydrogel was synthesized using carboxymethyl cellulose as a natural base,acrylic acid as a comonomer,graphene oxide as a filler,ammonium persulfate as an initiator,and iron nanoparticles as a crosslinking agent.The effect of reaction variables such as the iron nanoparticles,graphene oxide,ammonium persulfate,and acrylic acid were examined to achieve a hydrogel with maximum absorbency.Doxorubicin,an anti-cancer chemotherapy drug,was loaded into this hydrogel and its release behaviors were examined in the phosphate buffer solutions with different pH values.The structure of the graphene oxide and the optimized hydrogel were confirmed by Fourier-transform infrared spectroscopy,Raman spectroscopy,X-ray diffraction,scanning electron microscopy,and atomic force microscopy.     

Teflon Magnetic Stirring Capsules (TMSC) as a Practical and Reusable Delivery System for Sensitive Reagents and Catalysts

The development of a user-friendly reusable laboratory equipment for the delivery of sensitive reagents and catalysts is described. The tightness of these Teflon Magnetic Stirring Capsules (TMSC) is ensured by the magnetic force and release of the reagent inside the solution is triggered by adjusting the stirring rate so that the centrifuge force exceeds the magnetic force. They can be loaded with several chemicals at the same time and do operate across a broad range of temperatures. The inertness of Teflon facilitates reaction purification.     

Circumvent PEGylation dilemma by implementing matrix metalloproteinase-responsive chemistry for promoted tumor gene therapy

Surface modification by poly(ethylene glycol) (PEGylation) has been acknowledged as a powerful strategy in minimizing non-specific reactions for biomedical devices. Once applied into manufacture of drug/gene delivery systems, PEGylation has demonstrated to significantly improve their biocompatibility and stealthiness in physiological environment. Nonetheless, reluctant cell membrane affinities thus cellular uptake efficiencies owing to PEGylation brought up further issues that are imperative to be resolved. Pertain to this PEGylation dilemma, we attempted to introduce peptide (GPLGVRG) linkage between block copolymer of PEG-poly{N'-[N-(2-aminoethyl)-2-aminoethyl]aspartamide} PAsp(DET), wherein the cationic PAsp(DET) could self-assemble with pDNA into nanoscaled complex core. Noteworthy was the peptide linkage whose amino acids sequence could be specifically recognized and degraded by matrix metalloproteinases (MMPs) (overexpressed in extracellular milieu of tumors). Therefore, our subsequent studies validated facile detachment of PEGylation from the aforementioned polyplex micelles upon treatment of MMPs, which elicited improved cytomembrane affinities and cellular uptake efficiencies. In addition, promoted escape from endosome entrapment was also confirmed through direct endosome membrane destabilization by PAsp(DET), which was further elucidated to be attributable to dePEGylation as well as elevated charged density of PAsp(DET) in acidic endosomes. These benefits from dePEGylation eventually contributed to promoted gene expression at the affected cells and potent tumor growth suppression based on anti-angiogenic approach. Therefore, our developed strategy has provided a facile approach in overcoming the dilemma of PEGylation, which could be informative in design of drug/gene delivery systems.