Extreme makeover of cholesterol : Cholesterol exchange is a major reason for the instability of liposomes in blood. The formation of a covalent hybrid between cholesterol and glycerophosphocholine preserves the bilayer‐stabilizing effect of free cholesterol but prevents its transfer from the bilayer. Thus, disterolphospholipids (e.g. 1 ) are valuable new components for liposome formulation.
Water molecules doing time : Atomic‐resolution crystal structures of the PPIase domain of cyclophilin G, alone and in complex with cyclosporin A, and together with MD simulations and calorimetry, reveal how trapped water molecules influence the thermodynamic profile of a protein–ligand interaction.
Mind how you go : The current strategies for the development of therapies for Alzheimer's disease are very diverse. Particular attention is given to the search for inhibitors (see picture for two examples) of the proteolytic enzyme β‐ and γ‐secretase, which inhibits the cleavage of the amyloid precursor proteins into amyloid β peptides, from which the disease‐defining deposits of plaque in the brains of Alzheimer's patients originates.
Forces to reckon with : Supramolecular complexes, such as the one shown, are normally based on a combination of different interactions such as ion pairing, hydrogen bonds, and stacking interactions. The not always simple characterization of the nature and strength of intermolecular forces provides assistance to the understanding of biomimetic systems, as well as for the design of synthetic receptors, drugs, and intelligent materials.
Poly[(D ,L ‐lactide)‐co‐glycolide] nanoparticles coated with polyethyleneimine on their surface were prepared by an emulsification‐solvent evaporation method and subsequently surface modified by LBL assembly. The assembly of poly(acrylic acid) and polyethyleneimine on a planar substrate and on the PLGA nanoparticles was monitored by QCM‐D, ζ‐potential, flow cytometry and TEM. Carboxylic and amino groups in the multilayers were crosslinked by carbodiimide condensation, which was also later used to graft poly(ethylene glycol) (PEG). Rhodamine 6G, 5(6)‐carboxyfluorescein and fluorescein were incorporated into the nanoparticles and their release profiles were recorded at 60 °C and at 37 °C for rhodamine 6G, for nanoparticles with a multilayer coating, and those that were crosslinked and grafted with PEG.
Size tunable amphiphilic NPs composed of poly(γ‐PGA) and hydrophobic amino acids, such as Phe or Trp, were prepared. To prepare these size‐regulated NPs, γ‐PGA‐g‐Phe or γ‐PGA‐g‐Trp dissolved in DMSO was added to various concentrations of NaCl solution. The γ‐PGA‐Phe and γ‐PGA‐Trp formed monodispersed NPs, and the size of NPs can be easily controlled by NaCl concentration. The different‐sized NPs showed the same structure. The encapsulation of protein into the different‐sized NPs was successfully achieved and the size of protein‐encapsulated γ‐PGA‐Phe NPs was increased when protein was encapsulated.
Development of a novel formulation of anticancer drugs to improve their water‐solubility and bioavailability remains a great challenge. Herein, the potential anticancer agent 2‐methoxyestradiol (2‐ME) was selected as a model drug and was encapsulated within polyelectrolyte (PE) multilayers by layer‐by‐layer deposition of oppositely charged PEs onto the drug microcrystal surfaces. Cell viability and morphology observation of two cell lines reveal that the PE multilayer‐encapsulated 2‐ME microcrystals markedly decrease the cell viability, displaying similar inhibitory effect to that of the conventional formulation of 2‐ME dissolved in ethanol. The current approach to encapsulate hydrophobic drug microparticles may be useful for formulating different drugs for a variety of biological applications.
Cationic polymers have been chemically modified with a variety of targeting molecules such as peptides, proteins, antibodies, sugars and vitamins for targeted delivery of nucleic acid drugs to specific cells. Stimuli‐sensitive polymers exhibiting different size, charge and conformation in response to physiological signals from specific cells have also been utilized for targeted delivery. To achieve target‐specific delivery of nucleic acids, conjugation chemistry is critical to produce stable nanosized polyplexes tethered with cell‐recognizable ligands for facile cellular uptake via a receptor‐mediated endocytic pathway. In this review, synthetic strategies of functional cationic polymers with various targeting ligands are presented.
Surface-enhance Raman (SER) spectra of pyrazinamide (PZA), isoniazid (INAZ), and isonicotiamide (INCT) in silver sols have been studied over a range of solution concentration and pH. A linear calibration curve has been obtained for each of the sample molecules, and the lower limits of detection are estimated to be 5 ng for PZA and INAZ, and 10 ng for INCA. The variation of SER intensity with the sample solution pH is explained in terms of the charge of the sample species and the stability of the sols. The normal Raman and infrared spectra for the pure drug samples have also been collected, from which some vibration assignments for the molecules are given. The absorption behaviors of the molecules on the silver particle surfaces are also suggested. 相似文献
