Crystals sustained drug release

Sustained release from disperse systems such as emulsions and suspensions can be achieved by the adsorption of appropriate mesogenic molecules at the interface. The drug substance, which forms the inner phase or is included in the dispersed phase, cannot pass the liquid ciystals at the interface easily and thus diffuses slowly into the continuous phase and from there into the organism via the site of application. This sustained drug release is especially pronounced in the case of multilamellar liquid crystals at the interface. 

Solid formulations for sustained drug release may contain mesogenic polymers as excipients. The mesogenic polymers form a matrix, which is usually compressed into tablets. Some of the most frequently used excipients for sustained release matrices include cellulose derivatives, which behave like lyotropic liquid crystals when they are gradually dissolved in aqueous media. Cellulose derivatives such as hydroxy-propyl cellulose or hydroxy-propylmethyl cellulose form gel-like lyotropic mesophases in contact with water, through which diffusion takes place relatively slowly. Increasing dilution of the mesophase with water transforms the mesophase to a highly viscous slime and then to a colloidal polymer solution. 

Wu EC, Andrew JS, Cheng L, Freeman WR, Pearson L, Sailor MJ (2011b) Real-time monitoring of sustained drug release using the optical properties of porous silicon photonic crystal particles. Biomaterials 32 1957-1966... 

Wu EC, Andrew JS, Cheng LY, Freeman WR, Pearson L, Sailor MJ (2011) Real-time monitoring of sustained drug release using the optical properties of porous silicon photonic crystal particles. Biomaterials 32(7) 1957-1966. doi 10.1016/j.biomaterials.2010.11.013 Yu L (2001) Amorphous pharmaceutical solids preparation, characterization and stabilization. Adv Drug Deliv Rev 48(l) 27-42. doi 10.1016/s0169-409x(01)00098-9... 

Apart from the already established formulations, researchers are trying to develop novel oil-based formulations to combat the poor solubility and bioavailablity of NCE. Shevachman et al. developed novel U-type microemulsions to improve the percutaneous permeability of diclofenac. Shah et al.2 2 used microwave heating for the preparation of solid lipid nanoparticles by microemulsion techniques, which resulted in improved particle characteristics. Ki et al. reported sustained-release liquid crystal of injectable leuprolide using sorbitan monooleate. Recently, various novel oil-based drug delivery technologies are reported, which includes tocol emulsions, solid lipid nanopar-ticles, nanosuspensions, Upid microbubbles, sterically stabilized phospholipid micelles, and environmentally responsive drug delivery systems for parenteral administration.25 259... 

Exceptional structural properties allow the lyotropic mesophases to entrap water-soluble compounds within the aqueous domains, and hydrophobic molecules via direct interactions within their lipid hydrophobic compartments. LLCs have been shown to provide sustained release of drug molecules with a range of physicochemical properties [18, 53, 55]. In addition to its biological significance, inverse lipid phases could be useful as host systems for the crystallization of membrane proteins [8] and for inorganic synthesis [70]. 

The solid — and normally crystalline — state of the matrix lipid has, however, some drawbacks. Due to the high order of the crystal lattice, the capacity of drug incorporation is comparatively low. ° To improve the drug loading capacity and — potentially — to obtain a sustained release of incorporated drugs, lipid nanoparticles with a modified lipid matrix were developed in recent years. As the methods for preparation and characterization... 

---