Novel Particle Engineering Techniques in Drug Delivery : Review of Coformulations Using Supercritical Fluids and Liquefied Gases

This paper aimed to survey the numerous publications and patents issued in the fields of supercritical fluid assisted and cryogenic formulation techniques with special regard to coformulations of active substrate – excipient composites. These methods open new possibilities in formulation of drug carrier composites with targeted physical properties including particle size, morphology, crystallinity, polymorphism and residual solvent content Both methods were proved to be viable alternatives to conventional formulation techniques

Solid Dispersion of Oxeglitazar in PVP K17 and Poloxamer 407 by Supercritical Antisolvent and Coevaporation Methods

The objective of this work was to improve the dissolution rate and aqueous solubility of oxeglitazar. Solid dispersions of oxeglitazar in PVP K17 (polyvinilpyrrolidone) and Poloxamer 407 (polyoxyethylene-polyoxypropylene block copolymer) were prepared by supercritical antisolvent (SAS) and coevaporation (CoE) methods. Drug-carrier formulations were characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy, gas chromatography, UV/VIS spectroscopy and in vitro dissolution tests. The highest dissolution rate (nearly 3-fold higher than raw drug) was achieved by preparation of drug/PVP K17 coevaporate. Oxeglitazar/PVP K17 solid dispersions were stabilized by hydrogen bonding but contained higher amount of residual DCM than Poloxamer 407 formulations regardless of the method of preparation. SAS prepared oxeglitazar/Poloxamer 407 dissolved more than two times faster than raw drug. However, unlike PVP K17, Poloxamer 407 did not form a single phase amorphous solid solution with oxeglitazar which has been manifested in higher degrees of crystallinity, too. Among the two techniques, evaluated in this work, conventional coevaporation resulted in higher amorphous content but SAS reduced residual solvent content more efficiently

Comparison of solid dispersions produced by supercritical antisolvent and spray-freezing technologies

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Nanotechnology Applications to Improve Solubility of Bioactive Constituents of Foods for Health-Promoting Purposes

Foods-derived multifunctional compounds, such as carotenoids, vitamins, phytosterols, polyunsaturated lipids, curcuminoids, flavonoids and polyphenols, in addition to the basic nutritional value, own extra health benefits and are considered \u201cpharmaceutical-grade nutrients\u201d better known as \u201dnutraceuticals\u201d. Similarly, phytochemicals from plants, characterized by analogous chemical structures, can be considered \u201cpharmaceutical-grade molecules\u201d. They could provide both diseases preventive actions and remarkable therapeutic benefits but, the efforts for identifying their mode of action and for applying them into food industry with health-promoting purposes, are often unsuccessful. Solubility is essential for a good absorption in the gastrointestinal tract and to achieve the systemic concentration necessary for an effective therapeutic activity, but the majority of these compounds are water-insoluble. Consequently, when ingested, they encounter many difficulties in crossing the diverse barriers to reach the bloodstream and to distribute to cells and tissues. Their absorption at gastric or intestinal level is troubled and in addition, they suffer from early degradation or fast metabolism, so rarely they manage to reach the site of action in therapeutically effective concentration and their clinical applications result strongly limited. Toxic excipients and harmful solubilizing agents were and are extensively used for solubilizing and delivering non-soluble bioactive chemicals (BACs) despite the resulting unpleasant side effects complained of by patients. During last decades, several new techniques, often resorting to nanotechnology, aiming at enhancing BACs solubility, at solving their pharmacokinetics drawbacks, at avoiding their early inactivation or fast metabolism, have been developed. On this background, the following chapter provides an overview concerning nanotechnology contribute and its technological advancements in \u201cmanufacturing\u201d nutraceuticals and phytochemicals in more bioavailable nanoparticles. In addition, it is reviewed the involvement of nanoscience in developing and enhancing food-grade solid nanosized materials to be used as BACs \u201ccontainers\u201d and \u201cvehicles\u201d either for their safe and effective oral administration, in the frame of medical treatments, or for achieving smart food ingredients to improve the quality and shelf life of nourishments