Improve oral bioavailability of poorly soluble APIs
Overcoming solubility challenges in oral drug development
For a growing share of new drug candidates, poor aqueous solubility remains one of the key barriers to translating promising active pharmaceutical ingredients into successful oral dosage forms. Specialty silica excipients help overcome this bottleneck: AEROPERL® 300 Pharma helps formulators improve the solubility and bioavailability of poorly water-soluble APIs, enabling more effective oral dosage forms and robust pharmaceutical manufacturing.
Good aqueous solubility of active pharmaceutical ingredients (APIs) is a key prerequisite for many drugs to achieve the intended effect in the body. APIs in oral dosage forms need to dissolve before they can permeate the intestinal membrane, enter the systemic circulation, and reach the blood concentration required for efficacy.
Yet a large and growing share of drugs are poorly water-soluble – making dissolution the limiting factor between a potential API and an effective medicine. That is why drug solubility and bioavailability are major formulation challenges in pharmaceutical development. AEROPERL® 300 Pharma offers a smart solution.
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AEROPERL® 300 Pharma boosts API bioavailability via solubility enhancement
For formulators working at the intersection of API selection and excipient design, AEROPERL® 300 Pharma is a versatile excipient that increases the dissolution of poorly water-soluble molecules, leading to high drug bioavailability.
The Biopharmaceutics Classification System (BCS) groups APIs into four different classes according to their permeability and solubility in aqueous media. Drugs categorized in class II and class IV of the BCS system have poor aqueous solubility, which is the limitation to achieve therapeutically necessary blood concentrations.
In several case studies, AEROPERL® 300 Pharma has demonstrated the ability to improve the apparent solubility of BCS class II and class IV APIs, potentially shifting their biopharmaceutical performance toward higher BCS classes3, 4.
Smart Effects of AEROPERL® 300 Pharma
Improves dissolution performance and supports higher bioavailability of poorly water-soluble APIs (e.g. BCS class II and IV)
Converts liquid APIs and lipid formulations into free-flowing powders suitable for manufacturing andeasy tableting
Enhances mechanical tablet strength and protects APIs from moisture-induced degradation, ensuring long-term physical and chemical stability
Acts as an effective desiccant during wet granulation and moisture-activated dry granulation of oral solid dosage forms (OSDs)
Enhanced solubility for liquid, lipid and solid API preparations
Formulators benefit from flexibility in choosing oral solid dosage forms for drugs – e.g. tablet, powder sachet, or capsule – because the high surface area and mesoporous structure of AEROPERL® 300 Pharma enhance API presentation and dissolution regardless of formulation approach. AEROPERL® 300 Pharma converts liquid and solid APIs as well as lipid-based drug delivery systems into highly concentrated, free-flowing powders with improved solubility.
Lipid-based drug delivery systems (incl. self-nanoemulsified drug delivery technologies, SNEDDS): Loading fat-soluble active ingredients onto AEROPERL® 300 Pharma converts them into dry powders, enabling mechanically stable tablets with superior solubility and therefore increased bioavailability.4,5 Compared to inserting liquid lipid formulations into capsules, formulating with AEROPERL® 300 Pharma enables the more cost-efficient manufacturing of mechanically stable tablets with a longer shelf life.
Solid dispersion: AEROPERL® 300 Pharma is a mesoporous carrier for solvent or melt systems, stabilizing APIs in an amorphous state6,7 or smaller crystalline forms8 – enabling the production of mechanically stable tablets with superior solubility.
Micronized APIs: AEROPERL® 300 Pharma improves dissolution performance and promotes higher bioavailability by preventing particle agglomeration and maintaining a high effective surface area.
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Why formulators choose AEROPERL® 300 Pharma
AEROPERL® 300 Pharma monograph compliance
AEROPERL® 300 Pharma is qualified following Ph. Eur, USP/NF & ChP and it is globally available.
Ready to evaluate AEROPERL® 300 Pharma?
Whether you are developing a BCS Class II formulation, optimizing a lipid delivery system, or seeking to improve oral bioavailability, our experts can help.
