05. September 2018
This study aimed to enhance the dissolution rate of isradipine and to avoid the problem of first-pass metabolism using oral fast dissolving films (OFDFs). Isradipine was complexed with hydroxypropyl-beta-cyclodextrin (HP-β-CD) using the solvent co-evaporation technique to produce an isradipine inclusion complex with increased solubility. This complex was evaluated for its solubility and dissolution behavior compared with the free drug. Then, the inclusion complex was formulated in OFDFs. The...
07. May 2018
The aim of this research was to design and evaluate a hydrophilic matrix system for sustained release of glipizide, a weakly acidic poor soluble drug. A combination of inclusion complexation and microenvironmental pH modification techniques was utilized to improve the dissolution and pH-independent release of glipizide. Hydroxypropyl-β-cyclodextrin (HP-β-CD) was used as the complexation agent while sodium citrate and magnesium oxide (MgO) were used as model pH modifiers. The hydrophilic...
04. November 2016
γ-Cyclodextrin (γCD) is a cyclic oligosaccharide formed by bacterial digestion of starch and used as solubilizing agent and stabilizer in a variety of pharmaceutical and food products. γCD is a large (molecular weight 1297 Da) hydrophilic molecule that does not readily permeate biological membranes and is rapidly digested by bacteria in the gastrointestinal tract. In humans γCD is metabolized by α-amylase that is found in, for example, saliva, bile fluid and tears. Thus, bioavailability of...
01. October 2016
Abstract The aim of this study was to evaluate hot-melt extrusion (HME) as a continuous process to form cyclodextrin (CD) inclusion complexes in order to increase the solubility and dissolution rate of itraconazole (ITZ), a class II model drug molecule of the Biopharmaceutics Classification System. Different CD derivatives were tested in a 1:1 (CD:ITZ) molar ratio to obtain CD ternary inclusion complexes in the presence of a polymer, namely Soluplus® (SOL). The CD used in this series of...
20. June 2016
Abstract Since the discovery about 30 years ago (2-hydroxypropyl) beta-cyclodextrin, a highly soluble derivative of beta-cyclodextrin, has become an approved excipient of drug formulations included both in the United States and European Pharmacopoeias. It is recommended to use as solubilizer and stabilizer for oral and parenteral formulations. Recently, its pharmacological activity has been recognized in various diseases. The increasing applications require a closer look to the...
06. July 2015
Highlights •Synthesis and characterization of cysteamine conjugated β-cyclodextrin (β-CD-Cys). •Conjugates showed no toxic effects on Caco-2 cells at concentrations of 0.5% (m/v). •Maximum 34.51-fold improved mucoadhesion on the porcine buccal mucosa. •Inclusion complexes resulted in 150-fold increased water solubility of miconazole nitrate. More