Extraction of Chlorogenic Acid Using Single and Mixed Solvents.

Chlorogenic acid, which is extracted from a wide range of natural sources, is attracting the attention of many researchers in the pharmaceutical and biomedical fields due to its various positive effects, such as such as anti-inflammatory and antibacterial properties. Considering the effects of economics and solvent toxicity, water, ethanol, and their mixtures were selected as the solvents for extracting chlorogenic acid at various temperatures (298~318 K) and over a whole range of concentrations. The solubility of chlorogenic acid increased with temperature regardless of the solvents, and the solubility was higher in pure ethanol than in pure water.

Deep Eutectic Solvents Enhancing Drug Solubility and Its Delivery.

Deep eutectic solvents (DES) are environmentally friendly solvents with the potential to dissolve bioactive compounds without affecting their characteristics. DES has special qualities that can be customized to meet the unique characteristics of a biomolecule/active pharmaceutical ingredient (API) in accordance with various therapeutic needs, providing a reliable approach in opening the door for the creation of cutting-edge drug formulations by resolving solubility issues in pharmaceutics. This study outlines newly developing approaches to solve the problem of inefficient API extraction due to poor solubility.

Toxicity test profile for deep eutectic solvents: A detailed review and future prospects.

Deep eutectic solvents (DESs) are preferable in terms of starting materials, storage and synthesis, simplicity, and component material affordability. In several industries ranging from chemical, electrochemical, biological, biotechnology, material science, etc., DES has demonstrated remarkable potential.

Nanotechnology for Treatment of Glioblastoma Multiforme.

Glioblastoma multiforme (GBM), a grade IV astrocytoma as defined by the World Health Organization (WHO) criteria, is the most common primary central nervous system tumor in adults. After treatment with the current standard of care consisting of surgical resection, concurrent temozolomide (TMZ), and radiation, the median survival is only 15 months. The limited and less-effective treatment options for these highly aggressive GBMs call for the development of new techniques and the improvement of existing technologies.

The Origin of Ion-Pairing and Redissociation of Ionic Liquid.

We address the possible occurrence of a minimum extent of dissociation (α) of ionic liquid (IL) in IL-solvent mixtures. This phenomenon, known as the redissociation of IL, is responsible for many interesting composition-dependent properties in such mixtures. A thermodynamic model is developed to provide a semiquantitative prediction on the change of α with solvent concentration.

Reactive oxygen species-activated nanoprodrug of Ibuprofen for targeting traumatic brain injury in mice.

Traumatic brain injury (TBI) is an enormous public health problem, with 1.7 million new cases of TBI recorded annually by the Centers for Disease Control. However, TBI has proven to be an extremely challenging condition to treat.

Reactive oxygen species responsive nanoprodrug to treat intracranial glioblastoma.

Chemotherapy for intracranial gliomas is hampered by limited delivery of therapeutic agents through the blood brain barrier (BBB). An optimal therapeutic agent for brain tumors would selectively cross the BBB, accumulates in the tumor tissue and be activated from an innocuous prodrug within the tumor. Here we show brain tumor-targeted delivery and therapeutic efficacy of a nanometer-sized prodrug (nanoprodrug) of camptothecin (CPT) to treat experimental glioblastoma multiforme (GBM).

The role of long-range interactions in the phase behavior of ionic liquids.

The COSMO-type liquid activity coefficient models are among the most successful methods for the prediction of the phase behaviours of fluids containing ionic liquids. However, these models consider only interactions between species that are in close contact; in other words, the long-range Coulomb interactions, which are known to be important for systems containing charged species, are completely ignored. Here we show that the inclusion of long-range terms (with, e.

Nanoprodrugs of NSAIDs: Preparation and Characterization of Flufenamic Acid Nanoprodrugs.

We demonstrated that hydrophobic derivatives of the nonsteroidal anti-inflammatory drug (NSAID)flufenamic acid (FA), can be formed into stable nanometer-sized prodrugs (nanoprodrugs) that inhibit the growth of glioma cells, suggesting their potential application as anticancer agent. We synthesized highly hydrophobic monomeric and dimeric prodrugs of FA via esterification and prepared nanoprodrugs using spontaneous emulsification mechanism. The nanoprodrugs were in the size range of 120 to 140 nm and physicochemically stable upon long-term storage as aqueous suspension, which is attributed to the strong hydrophobic interaction between prodrug molecules.

Oxidative stimuli-responsive nanoprodrug of camptothecin kills glioblastoma cells.

The purpose of this study was to prepare and characterize nanometer-sized prodrug (nanoprodrug) of camptothecin. The camptothecin prodrug was synthesized using tetraethylene glycol spacer linked via carbonate bond to camptothecin and via ester bond to alpha-lipoic acid. The nanoprodrug was prepared through the spontaneous emulsification mechanism using the mixture of camptothecin prodrug and alpha-tocopherol which served as a structural matrix.

Chemokine CXC receptor 4--mediated glioma tumor tracking by bone marrow--derived neural progenitor/stem cells.

Malignant gliomas manifest frequent tumor recurrence after surgical resection and/or other treatment because of their nature of invasiveness and dissemination. The recognized brain tumor-tracking property of neural progenitor/stem cells opened the possibility of targeting malignant brain tumors using neural progenitor/stem cells. We and others have previously shown that fetal neural progenitor/stem cells can be used to deliver therapeutic molecules to brain tumors.

Preparation and characterization of antioxidant nanospheres from multiple alpha-lipoic acid-containing compounds.

The purpose of this study was to prepare and characterize antioxidant nanospheres composed of multiple alpha-lipoic acid-containing compounds (mALAs). It was found that the nanospheres were remarkably stable under physiologic conditions, maintained the antioxidant property of alpha-lipoic acid, and could be destabilized oxidatively and enzymatically. The preparations were simple and highly reproducible providing a new strategy for the development of nanometer-sized antioxidant biomaterials.

Stimuli-responsive antioxidant nanoprodrugs of NSAIDs.

A novel group of alpha-lipoic acid-containing hydrophobic prodrugs of non-steroidal anti-inflammatory drugs (NSAIDs) was synthesized and transformed into nanometer-sized prodrugs (nanoprodrugs). Three NSAIDs, indomethacin, ibuprofen and naproxen were linked to alpha-lipoic acid via tetraethylene glycol through hydrolytically degradable ester bonds. The three bifunctional derivatives were dissolved in organic solvents and capable of forming stable nanoprodrugs upon addition of the organic solutions into aqueous phase through the spontaneous emulsification mechanism.

Brain tumor tandem targeting using a combination of monoclonal antibodies attached to biopoly(beta-L-malic acid).

Tumor-specific targeting using achievements of nanotechnology is a mainstay of increasing efficacy of anti-tumor drugs. To improve drug targeting we covalently conjugated for the first time two different monoclonal antibodies, an anti-mouse transferrin receptor antibody and a mouse autoimmune anti-nucleosome antibody 2C5, onto the drug delivery nanoplatform, poly(beta-L-malic acid). The active anti-tumor drug components attached to the same carrier molecule were antisense oligonucleotides to vascular protein laminin-8.

Nanoconjugate based on polymalic acid for tumor targeting.

A new prototype of polymer-derived drug delivery system, the nanoconjugate Polycefin, was tested for its ability to accumulate in tumors based on enhanced permeability and retention (EPR) effect and receptor mediated endocytosis. Polycefin was synthesized for targeted delivery of Morpholino antisense oligonucleotides into certain tumors. It consists of units that are covalently conjugated with poly(beta-l-malic acid) (M(w) 50,000, M(w)/M(n) 1.

Inhibition of laminin-8 in vivo using a novel poly(malic acid)-based carrier reduces glioma angiogenesis.

We have previously shown that laminin-8, a vascular basement membrane component, was overexpressed in human glioblastomas multiforme and their adjacent tissues compared to normal brain. Increased laminin-8 correlated with shorter glioblastoma recurrence time and poor patient survival making it a potential marker for glioblastoma diagnostics and prediction of disease outcome. However, laminin-8 therapeutic potential was unknown because the technology of blocking the expression of multi-chain complex proteins was not yet developed.

Polycefin, a new prototype of a multifunctional nanoconjugate based on poly(beta-L-malic acid) for drug delivery.

A new prototype of nanoconjugate, Polycefin, was synthesized for targeted delivery of antisense oligonucleotides and monoclonal antibodies to brain tumors. The macromolecular carrier contains: 1. biodegradable, nonimmunogenic, nontoxic beta-poly(L-malic acid) of microbial origin; 2.

Stage specific expression of poly(malic acid)-affiliated genes in the life cycle of Physarum polycephalum. Spherulin 3b and polymalatase.

Polymalic acid is receiving interest as a unique biopolymer of the plasmodia of mycetozoa and recently as a biogenic matrix for the synthesis of devices for drug delivery. The acellular slime mold Physarum polycephalum is characterized by two distinctive growth phases: uninucleated amoebae and multinucleated plasmodia. In adverse conditions, plasmodia reversibly transform into spherules.

The DNA-polymerase inhibiting activity of poly(beta-l-malic acid) in nuclear extract during the cell cycle of Physarum polycephalum.

The naturally synchronous plasmodia of myxomycetes synthesize poly(beta-l-malic acid), which carries out cell-specific functions. In Physarum polycephalum, poly(beta-l-malate) [the salt form of poly(beta-l-malic acid)] is highly concentrated in the nuclei, repressing DNA synthetic activity of DNA polymerases by the formation of reversible complexes. To test whether this inhibitory activity is cell-cycle-dependent, purified DNA polymerase alpha of P.