Abbas Rahdar; Susan kazemi; Faezeh Askari
Abstract
A common approach for building a drug delivery system is to incorporate the drug within the nanocarrier that results in increased solubility, metabolic stability, and improved circulation time. However, recent developments indicate that selection of polymer nanomaterials can implement more than only ...
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A common approach for building a drug delivery system is to incorporate the drug within the nanocarrier that results in increased solubility, metabolic stability, and improved circulation time. However, recent developments indicate that selection of polymer nanomaterials can implement more than only inert carrier functions by being biological response modifiers. One representative of such materials is Pluronic block copolymers that cause various functional alterations in cells. The key attribute for the biological activity of Pluronics is their ability to incorporate into membranes followed by subsequent translocation into the cells and affecting various cellular functions, such as mitochondrial respiration, ATP synthesis, activity of drug efflux transporters, apoptotic signal transduction, and gene expression. As a result, Pluronics cause drastic sensitization to various anticancer agents based on multidrug resistant (MDR), enhance drug transport across the blood brain and intestinal barriers, and causes transcriptional activation of gene expression both in vitro and in vivo. On other hand, there has been a considerable research interest in the area of drug delivery using polymer based particulate delivery systems as carriers for small and large molecules. Particulate systems like nanoparticles and micelles have been used as a physical approach to alter and improve the pharmacodynamics and pharmacokinetic profiles of various types of drug molecules. Due to the wide compatibility with drug candidates of diverse nature and ingredients in formulations, poloxamers serve to be excellent polymer for drug delivery vehicles by different routes of administration. This review will highlight the poloxamers-based micelles/nanoparticles that have been developed to date.
Abbas Rahdar
Abstract
The development and design of the biocompatible and biodegradable thermodynamically stable micellar and microemulsion transparent dispersions to reduce the free and unbounded drugs concentration in the blood is a basic challenge in field of drug efficacy and bioavailability of drugs. In the current work, ...
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The development and design of the biocompatible and biodegradable thermodynamically stable micellar and microemulsion transparent dispersions to reduce the free and unbounded drugs concentration in the blood is a basic challenge in field of drug efficacy and bioavailability of drugs. In the current work, solubilization capacity of the drug (Tocopherol), oil (Ethyl Butyrate), and oil+drug (1:1 molar ratio) into F127 pluronic microemulsions was studied as a function of F127 concentration through simple turbidity or transparency experiments. Pluronic F127-based oil-in-water microemulsions of various compositions were synthesized and titrated with concentrated Tocopherol drug, Ethyl Butyrate oil, and oil+drug (1:1 molar ratio), separately, to determine clear /turbid transition zone. We observed that, at certain Pluronic F127 concentrations , microemulsions were gel-like. This specific concentration of F127 was different for three systems mentioned. We also observed that by increasing sodium caprylate fatty acid in the system , solutions became transparent. By the simple logic, we were able to determine the optimal binding ratio of F127 and/or SC to ethyl butyrate oil, Tocopherol drug, and oil+drug (1:1 molar ratio) in microemulsion. We also measured the dynamic surface tension and dynamic light scattering of the microemulsion formulations to further prove the hypothesis that all fatty acid is bound to the F127 in the microemulsion.