Solid Dispersion as a Technical Solution to Boost the Dissolution Rate and Bioavailability of Poorly Water-Soluble Drugs

Abstract

Solid dispersion (SD) is one of the oldest and widely utilized techniques to improve the solubility of slowly dissolving drugs. A variety of pharmaceutically compatible additives using different emerging technology is used for preparing SDs. Multiple approaches were designed to prepare SDs by such as kneading, co-milling, fusion, solvent evaporation and various solvent-associated methods. The selection of appropriate preparation method and carrier is vital for producing a homogenous product affecting its stability and biological activity. Many attempts were recently carried out to improve the scalability of the applied approaches and the results were novel preparation methods such as KinetiSol, Electrospinning and Hot-melt extrusion. In the present review, drug carriers used to formulate SD were classified as small molecular weight carriers, large molecular weight named polymeric carriers and functionalized polymeric ones. Moreover, new attractive SD formulated using the newly emerged natural carriers recently joined the field of the pharmaceutical industry.

Ameliorating the Poor Dissolution Rate of Selexipag in Aqueous Acidic Conditions Following Confinement into Mesoporous Silica

“…24 Pure SXP (5 mg) and equivalent amounts of MSNs formulations were added to 500 mL of aqueous media containing 0.5 M phosphate buffer (pH = 5.8) and 0.1N HCl (pH = 1.2) in the dissolution vessel, and the paddle speed was set at 100 rpm while maintaining a temperature of 37 ± 0.5°C to simulate physiological conditions. Samples were collected at predetermined intervals (5,10,20,30,40,50, and 60 min) and centrifuged at 7000 rpm for 5 min to remove any suspended particles. The same withdrawn volume of fresh dissolution medium was added to retain sink conditions.…”

Current Trends on Solid Dispersions: Past, Present, and Future

“…Based on the carrier used, solid dispersions can be classified into the following four generations [ 18 ]: First generation: Solid dispersions were formed as the first carriers to be applied in solid dispersions [ 19 ]. In this generation, crystalline carriers are used such as sugars and urea.…”

“…First generation: Solid dispersions were formed as the first carriers to be applied in solid dispersions [ 19 ]. In this generation, crystalline carriers are used such as sugars and urea.…”

“…(i) freely water-soluble with intrinsic quick-dissolving capabilities (ii) nontoxic and pharmacologically inert (iii) e melting process must be heat stable and it should have a low melting point (iv) It must be soluble in a wide range of solvents (v) It should be able to preferably increase the aqueous solubility of the drug (vi) Ideally, it should be able to boost the medication's water solubility and be chemically compatible with the drug and should not form a firmly bound complex with it [17] Based on the carrier used, solid dispersions can be classified into the following four generations [18]: First generation: Solid dispersions were formed as the first carriers to be applied in solid dispersions [19]. In this generation, crystalline carriers are used such as sugars and urea.…”

Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance

“…Carvedilol acts by relaxing the blood vessels and slowing the heart rate, thereby reducing blood pressure and improving blood flow [ 4 ]. The oral administration of drugs is regarded as the most widely used and preferred route for patients because of its benefits, such as simplicity, convenience, painless administration, and self-application [ 5 ]. However, lipophilic drugs of low aqueous solubility can encounter poor pharmacokinetic profiles and low bioavailability while passing through the gastrointestinal tract (GIT).…”