Introduction

In formulations, solubilizer play a pivotal role in improving the solubility and bioavailability of poorly soluble drugs. These excipients enhance the dissolution rate of active pharmaceutical ingredients (APIs), allowing for better absorption and maximizing therapeutic efficacy.

Subtypes of Solubilizer

Surfactants

Surfactants have surfactant properties, meaning they can reduce the surface tension between two immiscible substances, such as water and oil. They enhance solubility by forming micelles or emulsions that encapsulate the hydrophobic drug molecules. Examples of surfactants commonly used as solubilizers include polysorbates (e.g., Polysorbate 80), Tweens (e.g., Tween 80), and sodium lauryl sulfate.

Co-solvents

Co-solvents, such as alcohols, glycols, and polyethylene glycols (PEGs), are commonly utilized as solubilizers. They increase the solubility of hydrophobic drugs by forming molecular interactions with the API, facilitating its dispersion in the solvent. Common examples include ethanol, propylene glycol, and PEG 400.

Cyclodextrins

Cyclodextrins are cyclic oligosaccharides that can form inclusion complexes with hydrophobic drugs. They have a hydrophobic core and a hydrophilic outer surface, enabling the solubilization of poorly soluble compounds. Common cyclodextrins used as solubilizers include α-cyclodextrin, β-cyclodextrin, and hydroxypropyl-β-cyclodextrin.

Examples of Solubilizer

Polysorbate 80

Polysorbate 80 is a surfactant frequently employed as a solubilizer in oral and parenteral formulations. It improves the solubility of lipophilic drugs, facilitating their absorption in the gastrointestinal tract or enhancing their miscibility in intravenous solutions.

Ethanol

Ethanol is a commonly used co-solvent that enhances solubility in various drug formulations. It is utilized in oral solutions, suspensions, and topical preparations to solubilize lipophilic drugs and enhance their bioavailability.

Hydroxypropyl-β-cyclodextrin

Hydroxypropyl-β-cyclodextrin is a cyclodextrin derivative known for its solubilizing properties. It can form inclusion complexes with poorly soluble drugs, improving their solubility in aqueous systems. It is commonly used in oral and injectable formulations.

Conclusion

Enhancing the solubility of poorly soluble drugs is vital for optimizing their therapeutic efficacy. Solubilizers assist in increasing solubility, aiding drug absorption, and enhancing bioavailability. They enable the formulation of various dosage forms, including liquids, suspensions, and injectables, expanding treatment options and improving patient compliance. Partnering with Protheragen-ING, a reputable supplier, ensures the availability of high-quality excipients and supports the development of stable and efficacious pharmaceutical products. If you have any excipient requirements, please contact us by phone or email, and we will respond within 2-4 working days.