Among all newly discovered chemical entities about 40% drugs are lipophillic and fail to reach market due to their poor water solubility. Drug with poor water solubility cause slow dissolution rates, generally show erratic and incomplete absorption leading to low bioavailability when administered orally. Aqueous solubility of any therapeutically active substance is a key property, as it governs...

glucosyl-ƒ¿-CD (G-ƒ¿-CD), 6-O-ƒ¿-D-glucosyl-ƒÀ-CD (G-ƒÀ-CD), and 6A,6D-di-O-ƒ¿-D-glucosyl-ƒÀ-CD (2G-ƒÀ-CD) with slightly soluble or insoluble drugs in aqueous solution and in the solid state was studied by the solubility method, ultraviolet spectroscopy, and differential scanning calorimetry. These glucosyl-CDs were capable of forming inclusion complexes with compounds which can form complexes ...

The drug candidates coming from combinatorial chemistry research and/or the drugs selected from biologically based high-throughput screening are quite often very lipophilic, as these drug candidates exert their pharmacological action at or in biological membranes or membrane-associated proteins. This challenges drug delivery institutions in industry or academia to develop carrier systems for th...

Introduction Although the capability of ingested lipids to enhance the bioavailability of poorly water-soluble drugs has been experimentally observed and established 1 , the phenomenon is not well understood and is unpredictable. Commercially, lipids could offer valuable opportunities for enabling oral drug delivery, as approximately 4070% of all new drug candidates have been estimated to have ...

The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to both the pharmaceutical industry and the agencies that regulate them. These challenges include developing and validating the test methods, ensuring that methods are appropriately discriminatory, and addressing the potential for an in vivo–in vitro correlation (IVIVC). Di...

To prepare immunomicelles, new targeted carriers for poorly soluble pharmaceuticals, a procedure has been developed to chemically attach mAbs to reactive groups incorporated into the corona of polymeric micelles made of polyethylene glycol-phosphatidylethanolamine conjugates. Micelle-attached antibodies retained their ability to specifically interact with their antigens. Immunomicelles with att...

The objective of this study was to develop nanoemulsion formulations for enhancement of oral bioavailability of paclitaxel, a model hydrophobic drug and P-glycoprotein substrate. The oil-in-water (o/w) nanoemulsions were made with pine nut oil as the internal oil phase, egg lecithin as the primary emulsifier, and water as the external phase. Stearylamine and deoxycholic acid were used to impart...

At present about 40% of the drugs being in the development pipelines are poorly soluble, even up to 60% of compounds coming directly from synthesis are poorly soluble [1]. Poor solubility is in most cases associated with poor bioavailability. According to the Noyes-Whitney law the dissolution velocity dc/dt depends on the saturation solubility cs. There are two basic approaches to overcome the ...

Nanotechnology has been improving and has a variety of application fields. One of the major application areas of nanotechnology in pharmacy is nanoparticular drug delivery systems. Preparation of drug nanocrystals to improve the solubility of poorly water-soluble drugs for oral delivery is also one of the important applications. Nanocrystal dispersions comprise water, active drug substance and ...