Solubility microsphere systems

Chitosan has been recently found to be soluble in alkaline media, viz. NH4HCO3 solutions, where it assumes the ammonium carbamate form Chit-NHC02 NH4, i.e., a transient anionic form that keeps it soluble at pH 9.6, while reversibly masking the polycationic nature of chitosan. Because ammonium carbamates and NH4HCO3 decompose thermally and liberate CO2, NH3 and water, this alkaline system is suitable for producing chitosan microspheres by spray-drying (Table 1) [206]. 

A large variety of drug delivery systems are described in the literature, such as liposomes (Torchilin, 2006), micro and nanoparticles (Kumar, 2000), polymeric micelles (Torchilin, 2006), nanocrystals (Muller et al., 2011), among others. Microparticles are usually classified as microcapsules or microspheres (Figure 8). Microspheres are matrix spherical microparticles where the drug may be located on the surface or dissolved into the matrix. Microcapsules are characterized as spherical particles more than Ipm containing a core substance (aqueous or lipid), normally lipid, and are used to deliver poor soluble molecules... 

Microspheres and nanoparticles often consist of biocompatible polymers and belong either to the soluble or the particle type carriers. Besides the aforementioned HPMA polymeric backbone, carriers have also been prepared using dextrans, ficoll, sepharose or poly-L-lysine as the main carrier body. More recently alginate nanoparticles have been described for the targeting of antisense oligonucleotides [28]. As with other polymeric carrier systems, the backbone can be modified with e.g. sugar molecules or antibody fragments to introduce cellular specificity. 

Many other delivery systems have been employed in attempts to improve the delivery of anticancer drugs. The major types include liposomes, microspheres, nanoparticles and immunotoxins. This review concentrates on soluble polymeric carriers. However, basic characteristics of alternate delivery systems have been included to permit the reader the comparison of different delivery systems. 

In order to overcome the main limitations of the impregnation processes, connected to the limited solubility of the compounds in the supercritical fluids, Perman [68] proposed an alternative method. A supercritical impregnation process was coupled with a liquid solvent (preferentially water) to enhance the drug solubilization. The system composed of a liquid drug solution and the polymeric support was pressurized with the supercritical fluid. Consequently, the swelled polymer allows rapid diffusional transport of the solute into the polymeric substrate. In different examples, bovine serum albumin microspheres were impregnated with insulin, trypsin and gentamicin (see Table 9.9-5). 

In pharmaceutical preparations, soybean oil emulsions are primarily used as a fat source in total parenteral nutrition (TPN) regimens. Although other oils, such as peanut oil, have been used for this purpose, soybean oil is now preferred because it is associated with fewer adverse reactions. Emulsions containing soybean oil have also been used as vehicles for the oral and intravenous administration of drugs drug substances that have been incorporated into such emulsions include amphotericin, " diazepam, retinoids, vitamins, poorly water-soluble steroids, fluorocarbons, and insulin. In addition, soybean oil has been used in the formulation of many drug delivery systems such as liposomes, microspheres, dry emulsions, self-emulsifying systems, and nanoemulsions and nanocapsules. ... 

Fluorescent naphthol-based polymers were prepared by HRP-catalyzed polymerization of 2-naphthol in AOT/isooctane reverse micelles to give the polymer microspheres.31 The precipitated polymer was soluble in a range of polar and nonpolar organic solvents and possessed quinonoid structure. The reverse micellar system induced the peroxidase-catalyzed copolymerization of p-hydroxythiophenol and />ethylphenol, yielding the thiol-containing polyphenol particles.32 The attachment of CdS to the particles gave the CdS—polymer nanocomposite showing fluorescence characteristics. 

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