Abstract
Self-assembling block copolymers (poloxamers, PEG/PLA and PEG/PLGA diblock and triblock copolymers, PEG/polycaprolactone, polyether modified poly(Acrylic Acid)) with large solubility difference between hydrophilic and hydrophobic moieties have the property of forming temperature dependent micellar aggregates and, after a further temperature increase, of gellifying due to micelle aggregation or packing. This property enables drugs to be mixed in the sol state at room temperature then the solution can be injected into a target tissue, forming a gel depot in-situ at body temperature with the goal of providing drug release control. The presence of micellar structures that give rise to thermoreversible gels, characterized by low toxicity and mucomimetic properties, makes this delivery system capable of solubilizing water-insoluble or poorly soluble drugs and of protecting labile molecules such as proteins and peptide drugs.
Highlights
Amphiphilic block copolymers (AB or ABA-type) with large solubility differences between hydrophilic and hydrophobic moieties, in aqueous medium are able to self-assemble into polymericPolymers 2011, 3 micelles characterized by mesoscopic size range
Recent studies have focused on thermogelling polymeric micelles made of self-assembling block copolymers such as poloxamers, multiblock copolymers prepared from poly(lactide), polycaprolactone, poly(glycolic acid), and polyether modified poly(acrylic acid) [5,6,7], These polymers have the ability to form temperature dependent micellar aggregates and, after a further temperature increase, gels due to micelles aggregation or packing
The aim of this review is to illustrate the relevance of different self assembling block copolymers used in the pharmaceutical field as drug targeting systems, by means of their chemical synthesis, description of their applications, together with some of the analitycal techniques used for physicochemical characterization
Summary
Amphiphilic block copolymers (AB or ABA-type) with large solubility differences between hydrophilic and hydrophobic moieties, in aqueous medium are able to self-assemble into polymeric. Recent studies have focused on thermogelling polymeric micelles made of self-assembling block copolymers such as poloxamers, multiblock copolymers prepared from poly(lactide), polycaprolactone, poly(glycolic acid), and polyether modified poly(acrylic acid) [5,6,7], These polymers have the ability to form temperature dependent micellar aggregates and, after a further temperature increase, gels due to micelles aggregation or packing. With these polymers it is possible to mix drugs in the sol state and at room temperature and the solution can be injected into a target tissue. The aim of this review is to illustrate the relevance of different self assembling block copolymers used in the pharmaceutical field as drug targeting systems, by means of their chemical synthesis, description of their applications, together with some of the analitycal techniques used for physicochemical characterization
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