By in-situ forming cocrystal, chemically stable amorphous solid dispersions were prepared by MM and HME at a depressed processing temperature. This method provides an attractive opportunity for HME of heat-sensitive drugs.
The cultivation of single crystals from solution is usually a time-consuming trial-and-error game. Here, we report a general strategy for rapidly cultivating single crystals from melt microdroplets within tens of...
Some kinds of amphiphilic lipids can spontaneously self-assemble with a proper ratio of water to form liquid crystalline, also known as cubic phase. With a curved bi-continuous lipid bilayer and two congruent networks of water channels, cubic phases can enclose hydrophilic, amphiphilic and hydrophobic drugs for delivery. Nanostructured cubosomes, prepared by fragmentation of bulk cubic phase gels or lyotropic methods, retain the same inner structure of cubic phase and possess much larger specific surface area and lower viscosity. These unique properties make cubosomes excellent delivery systems applicable for oral, mucosal, transdermal and parenteral drug delivery. This article gave an overview of the accelerated development and current status of cubosomes research, with respect to their preparation, characteristics and applications in pharmaceutics.
Objectives Hot melt extrusion (HME) as a technique for producing amorphous solid dispersion (ASD) has been widely used in pharmaceutical research. The biggest challenge for the application of HME is the thermal degradation of drug, poor physical stability of ASD and precipitation of drug during dissolution. Interactions between drugs and polymers may play an important role in overcoming these barriers. In this review, influence of drug-polymer interactions on HME and the methods for characterizing the drug-polymer interactions were reviewed. Key findings Strong drug-polymer interactions, especially ionic interactions and hydrogen bonds, are helpful to improving the thermal stability of drug during HME, enhancing the physical stability of ASD during storage and maintaining supersaturated solution after dissolution in gastrointestinal tract. The interactions can be quantitatively and qualitatively characterized by many analysing methods. Conclusions As many factors collectively determine the properties of HME products, drug-polymer interactions play an extremely important role. However, the action mechanisms of drug-polymer interactions need intensive investigation to provide more useful information for optimizing the formulation and the process parameters of HME.
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