Improving the effectiveness of Active Pharmaceutical Ingredients (APIs) is one of the most pressing formulation challenges facing today’s pharmaceutical industry. While innovation in drug discovery continues to accelerate, formulation scientists are increasingly constrained by one major issue: poor API solubility.
In fact, nearly 80% of APIs are poorly water-soluble, significantly limiting their bioavailability and therapeutic performance. Overcoming this challenge requires not only innovative molecules, but also advanced excipients capable of enhancing solubilisation, absorption and controlled release.
The Solubility Challenge in Modern Drug Formulation
Despite major investments in new APIs and biotechnologies, the pharmaceutical industry still faces a shortage of truly innovative excipients. Many formulations struggle to deliver consistent efficacy, especially when dealing with BCS Class II and IV APIs, which are hydrophobic and often highly crystalline.
To address this gap, Safic-Alcan works closely with leading excipient manufacturers to bring next-generation formulation solutions to the market.
An Innovative Excipient: BioSustane® SAIB NF
In partnership with Eastman, Safic-Alcan introduces BioSustane® SAIB NF, an innovative pharmaceutical excipient designed to improve API solubility, absorption and release control.
BioSustane® SAIB NF is a fully substituted sucrose molecule, containing acetate and isobutyrate esters in a 2:6 ratio. It belongs to the family of sucrose long-chain fatty acid esters, materials already well known in the food and cosmetic industries for their emulsifying and solubilising properties.
These excipients are biodegradable, non-crystalline and highly hydrophobic, making them particularly suitable for complex pharmaceutical formulations.
How BioSustane® SAIB NF Improves API Performance
BioSustane® SAIB NF offers multiple formulation benefits across a wide range of APIs:
Enhanced Solubilisation and Absorption
Its viscous, hydrophobic nature makes BioSustane® SAIB NF an excellent solvent for poorly water-soluble APIs, particularly BCS Class II and IV compounds, which represent the majority of marketed APIs.
When combined with suitable surfactants, APIs dissolved in BioSustane® SAIB NF can be efficiently released and absorbed in the gastrointestinal tract. Studies have demonstrated up to 80–90% drug release within one hour for Class IV APIs such as aprepitant.
Controlled and Sustained Release
BioSustane® SAIB NF provides remarkable sustained-release functionality for all BCS classes:
- BCS Class II & IV APIs: The API is dissolved within the matrix and diffuses out over time.
- BCS Class I & III APIs: The API is encapsulated within the matrix, allowing gradual diffusion and controlled release.
This dual functionality makes BioSustane® SAIB NF a versatile excipient for a wide range of therapeutic applications.
Formulating with BioSustane® SAIB NF
Formulation with BioSustane® SAIB NF is straightforward and adaptable:
- The excipient is typically heated to 70–80°C, allowing the API to dissolve under agitation.
- Higher temperatures may be used depending on API stability.
- Alternatively, 5–10% ethanol (by weight of BioSustane® SAIB NF) can be added to facilitate dissolution.
- The resulting solution is then processed via wet granulation, followed by tableting or capsule filling.
Controlled-release performance has been demonstrated with relatively low excipient concentrations:
- Diclofenac Sodium: sustained release achieved with 8–16% BioSustane® SAIB NF
- Ephedrine formulations: effective release profiles with 16–30% BioSustane® SAIB NF
Final concentrations remain formulation-dependent, and Safic-Alcan supports customers in optimising formulations based on their specific constraints.
Why Consider BioSustane® SAIB NF?
BioSustane® SAIB NF offers several unique advantages:
- Suitable for oral, parenteral and topical dosage forms
- Remains amorphous at room temperature, enabling consistent drug delivery
- Non-polymeric: does not coagulate or precipitate in body fluids
- Exhibits mucoadhesive properties, opening opportunities for specialised drug delivery systems
These properties make BioSustane® SAIB NF a powerful tool for formulators seeking to enhance drug performance while maintaining formulation stability.
Advancing Pharmaceutical Innovation Together
Safic-Alcan actively supports pharmaceutical innovation through technical expertise, formulation guidance and access to cutting-edge excipients. A dedicated technical webinar presented by the Eastman team has already been successfully delivered, with multiple European projects underway. The webinar recording is available upon request.
Want to know more?
Contact our teams to discuss your formulation challenges or request access to our technical webinar and formulation data.
