Solubilized Technologies (oral & parenteral administration)

Solubilized

Survey, Speed and Icebreaker services use specific technologies to improve the solubility and dissolution of poorly soluble compounds. Classification of these technologies is based on the physical form of the compound and sub-categorized on how the desired form is obtained. In the Solubilized form, the molecules of the compound are arranged in an unstructured way where no ordered crystalline structure exists. Such a high energy form usually has faster dissolution and (transiently) higher aqueous solubility in vivo than the Crystalline form.

Micelle
Surfactant or mixture of surfactants that dissolves the compound. A compound that can be solubilized in this way should also not crystallize and precipitate out upon dilution. To find out more about this technology click here.
Mixed Micelle
Carefully selected mixtures of surfactant (such as bile and lecithin). These colloidal carriers are useful for a compound that is lipophilic and fits snugly into mixed micelles. To find out more about this technology click here.
Co-Solvent
Mixture of acceptable solvents that dissolve the drug. Not a true solubilized form because upon dilution the drug can crash out as there is no excipient to capture the compound in solution. To find out more about this technology click here.
pH
pH adjustment to increase the solubility of an ionizable compound. Not a true solubilized form but can increase solubility without excipients. To find out more about this technology click here.
Liposome
Phospholipids that can solubilize a poorly soluble compound within a bilayered membrane-like structure. These biocompatible carriers are ideal for a compound that can move rapidly between water and membranes. To find out more about this technology click here.
Cyclodextrin
Water soluble, donut-shaped structures that capture a part of an insoluble molecule to increase the compound solubility. A relatively high drug concentration may be reached if the compound has a high affinity to cyclodextrins. To find out more about this technology click here.
Emulsion
Milk-like liquids where oil droplets are homogeneously emulsified in water. Mainly useful for intravenous administration of a highly oil soluble lipophilic drug. To find out more about this technology click here.

(oral administration only)

Oily Solution
Digestible oil that dissolves the compound, usually only suited for a highly lipophilic/fatty compound. Though the compound does not require dissolution inside the body, it may need digestion of the oil to release the drug. To find out more about this technology click here.
Macroemulsion
Self emulsifying system that forms cloudy microscopically visible droplets after contact with water. The system may need some digestion in the intestines to release the drug completely. To find out more about this technology click here.
Microemulsion
Self (micro)emulsifying system that readily forms ultra fine droplets which look almost clear upon contact with water. Absorption is normally independent of digestion and circumvents positive food effects. To find out more about this technology click here.
Phospholipid Mixed Micelle
Phospholipid carrier that package a lipophilic molecule in the zone where one fatty acid tail has been removed from some of the phospholipids which usually have two tails. Normally independent of digestion and can avoid positive food effects. To find out more about this technology click here.

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