Solubility Enhancers for Oral Drug Delivery

Hydrogen Bonding: Between Strengthening the Crystal Packing and Improving Solubility of Three Haloperidol Derivatives

“…Formulation scientists employ various approaches to address this issue. In addition to the classical approaches like particle size reduction, salt formation, co-solvency, and complexation, modern technologies are also used, such as: nanotechnology, micro emulsions and solid dispersions [3].…”

“…Amorphous drug forms may have multiple-fold higher solubility compared to their crystalline counterparts [3,4]. This approach is challenging, however, because the amorphous drug form is thermodynamically unstable, which results in frequent recrystallization upon storage.…”

Prediction of the solubility in lipidic solvent mixture: Investigation of the modeling approach and thermodynamic analysis of solubility

“…There are various well known techniques are used for enhancement of solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like Solid dispersions (Alam et al, 2012;Leuner and Dressman, 2000;Murtaza et al, 2014), co-crystallization (Kim and Park, 2004;Miroshnyk et al, 2009;Shan and Zaworotko, 2008), particle size reduction like micronization and nanosuspension (Charoen chaitrakool et al, 2000;Chen et al, 2011;Liversidge and Cundy, 1995), cryogenic techniques (Charoenchaitrakool et al, 2000), complexation (Brewster and Loftsson, 2007;Loftsson and Brewster, 1996), salt formation (Blagden et al, 2007;Serajuddin, 2007), use of adjuvants like surfactants, solubilizers, co-solvents, and novel lipidic excipients (Blagden et al, 2007;Savjani et al, 2012). Of all, one of the contemporary approaches is Lipid based drug delivery systems (LBDDS) like self-microemulsifying DDS (SMEDDS) which usually present the drug to the stomach in a solubilized state, unlike tablets (Constantinides, 1995;Gao and Morozowich, 2006;Kommuru et al, 2001;Pouton and Porter, 2008).…”

Improved Supersaturation and Oral Absorption of Dutasteride by Amorphous Solid Dispersions

“…Many technological methods have been reported with regard to enhancing the dissolution and absorption properties of drugs with low water solubility, such as self-emulsifying formulations, solid dispersions, ionic inclusion complexation, lipid-based complexation, formation of salts, polymorphs, cocrystals, and prodrugs, and particle size reduction techniques, such as micronization or nanomilling. 5) Among these, solid dispersions with hydrophilic carriers are particularly promising methods for improving the solubility and dissolution rate of poorly water-soluble drugs.…”