Abstract
Polymeric micelles are potentially efficient in encapsulating and performing the controlled release of various hydrophobic drug molecules. Understanding the fundamental physicochemical properties behind drug–polymer systems in terms of interaction strength and compatibility, drug partition coefficient (preferential solubilization), micelle size, morphology, etc., encourages the formulation of polymeric nanocarriers with enhanced drug encapsulating capacity, prolonged circulation time, and stability in the human body. In this review, we systematically address some open issues which are considered to be obstacles inhibiting the commercial availability of polymer-based therapeutics, such as the enhancement of encapsulation capacity by finding better drug–polymer compatibility, the drug-release kinetics and mechanisms under chemical and mechanical conditions simulating to physiological conditions, and the role of preparation methods and solvents on the overall performance of micelles.
Highlights
Block copolymers are a fascinating class of polymeric materials that consist of two or more covalently bonded blocks forming a variety of architectures [1]
These values were taken at drug/polymer = 1/10. b These values depend on the drug/polymer weight ratio and the solvent used in the dialysis method. c The drug-loaded micelle size and loading efficiency at drug/micelle = 8/20
It is of significant interest to design polymeric micelles that are capable of acting as true delivery vehicles for various potent drugs, which are not in therapeutic formulations due to their water-insoluble, hydrophobic natures
Summary
Block copolymers are a fascinating class of polymeric materials that consist of two or more covalently bonded blocks forming a variety of architectures (e.g., linear diblock and triblock copolymers, star block copolymers, and miktoarm star copolymers) [1]. The main obstacles to the circulation of polymeric micelles are the filtration in the kidney and recognition by the reticuloendothelial system (RES) located in the liver, spleen, and lung (Figure 2) [30] This can be overcome when corona-forming blocks are highly biocompatible [31] and the total molecular weight of the block copolymer is higher than 42–50 kDa—the molecular weight threshold for water-soluble synthetic polymers to be filtered or recognized [32]. In the 2000s, several significant, related physicochemical and clinical studies got after the leading trials for the enhancement in in vivo pharmacological activities [39,51] and targeting [40,52] of drugs through the use of polymeric micelles. PEG-PBCL [67,93,100], and poly(ethylene glycol)-poly(δ-valerolactone) PEG-PVL [106,107]
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