Colloid-Bonded Medicinal Compounds (original) (raw)

Colloidal Aggregation Affects the Efficacy of Anticancer Drugs in Cell Culture

ACS Chemical Biology, 2012

Many small molecules, including bioactive molecules and approved drugs, spontaneously form colloidal aggregates in aqueous solution at micromolar concentrations. Though it is widely accepted that aggregation leads to artifacts in screens for ligands of soluble proteins, the effects of colloid formation in cell-based assays have not been studied. Here, seven anticancer drugs and one diagnostic reagent were found to form colloids in both biochemical buffer and in cell culture media. In cell-based assays, the antiproliferative activities of three of the drugs were substantially reduced when in colloidal form as compared to monomeric form; a new formulation method ensured the presence of drug colloids versus drug monomers in solution. We also found that Evans Blue, a dye classically used to measure vascular permeability and to demonstrate the "enhanced permeability and retention (EPR) effect" in solid tumors, forms colloids that adsorb albumin, as opposed to older literature that suggested the reverse.

Colloidal delivery of drugs: present strategies and conditions

2021

In this report, we give a description of a broad range of colloidal drug delivery systems with special focus on vesicles used in research or potentially useful as carrier systems for pharmaceutical drugs or active biomolecules or as therapeutic cell carriers. Colloidal drug delivery systems provide some essential descriptions of the drug delivery systems currently being built for academic or clinical applications. This series of systems are commonly used due to outstanding drug tracking, continuous and regulated release behavior, improved drug molecules clogging performance, avoidance of product hydrolysis or enzymatic degradation, and therapeutic efficacy improvements. Such characteristics aid in the discovery of suitable carrier structures for the transmission of medicines, cells, and genes in various fields.

Advanced colloidal technologies for the enhanced bioavailability of drugs

Cogent Medicine, 2018

Bioavailability of the colloidal particles is of great concern. It is because about 40% of the newly discovered colloidal agents are poorly water soluble and thus poorly bioavailable. Various colloidal technologies have been adopted to enhance the bioavailability of such drugs. In this review, advanced colloidal technologies are discussed to understand the mechanism of bioavailability enhancement of drugs, coding latest references from the literature. Additionally, advantages and disadvantages of the concerned colloidal technologies are discussed to understand the potential usage of each process. All these colloidal technologies effectively enhance the bioavailability of poorly bioavailable drugs, either by protecting them from the environment of the gastrointestinal or by prolonging their intended therapeutic effect. Furthermore, complexation of the drug molecule with potential carries, particle size reduction to nanoscale, co-crystallization and selfemulsifying drug delivery system are also discussed which not only enhance the bioavailability but also reduce the potential toxicities of the loaded drugs. It is therefore important to understand the vital colloidal technologies with their recent Front:

United States Patent ( 19 ) Hugl et al . ( 54 POLYMER-BOUND DYES

2017

A polymer-bound linkable dye comprising a) a water-soluble polymer backbone, b) a dye covalently bound thereto, and c) functional groups which enable the polymer-dye to link covalently with biological materials, in which the water-soluble polymer backbone is a co polymer which contains arcylamide, methacrylamide, N-C1-C4alkyl(meth)acrylamide, N,N-C1-C4dialkyla crylamide, N-vinylpyrrolidone, N-vinylpiperidone, N vinylcaprolactam, N-vinylformamide, N-vinylaceta mide, N-vinyl-N-methylacetamide, N-vinyl-O-methy lurethane, ethene or vinylmethylether as nonionic non omer blocks. The polymer-bound dye can be linked to a biologically active material such as an antibody or nu cleic acid and used analytically.

Colloidal Aggregation and the in vitro Activity of Traditional Chinese Medicines

Traditional Chinese Medicine (TCM) has been the sole source of therapeutics in China for two millennia. In recent drug discovery efforts, purified components of TCM formulations have shown activity in many in vitro assays, raising concerns of promiscuity. Here, we investigated fourteen bioactive small molecules isolated from TCMs for colloidal aggregation. At concentrations commonly used in cell-based or biochemical assay conditions, eight of these compounds formed particles detectable by dynamic light scattering and showed detergentreversible inhibition against β-lactamase and malate dehydrogenase, two counter-screening enzymes. When tested against their literature-reported molecular targets, three of these eight compounds showed similar reversal of their inhibitory activity in the presence of detergent. For three of the most potent aggregators, contributions to promiscuity via oxidative cycling were investigated – addition of 1 mM DTT had no effect on their activity, which is inconsistent with an oxidative mechanism. TCMs are often active at micromolar concentrations; this study suggests that care must be taken to control for artifactual activity when seeking their primary targets. Implications for the formulation of these molecules are considered.

Colloidal particles in drug delivery

Current Opinion in Colloid & Interface Science, 1998

Research into colloidal particles for drug delivery has, in the past few years, begun to focus on the delivery of biopolymers such as peptides, proteins and plasmids. Progress is being made in the sustained delivery of biopolymers and in the development of particulate delivery systems for alternative routes of administration, such as the lungs or nasal cavity.