Nanoforming enabling long acting injectables

Oral delivery remains the most common route of administration for small molecules. However, there is a growing use of long acting injectable (LAI) formulations where they offer advantages over daily or more frequent capsules and tablets, especially in psychiatry settings and for chronic indications. LAIs can offer several benefits over standard oral therapies:

• Improved adherence to therapy by eliminating the need for frequent dosing, especially beneficial for patients with schizophrenia, HIV, or opioid use disorder (OUD)
• Consistent drug levels with optimal payload delivery within the desired timeframe, eliminating the maximum and minimum serum concentration (c_max and c_min / c_trough) of orally administered drugs
• Enhanced patient convenience with reduced side effects
• Lower risk of abuse, relevant for opioids, sedatives and stimulants

Absorption from a subcutaneously administered suspension is governed by dissolution rate. Crystalline APIs with poor solubility have long absorption windows. For subcutaneous or intramuscular delivery of LAIs, an appropriate formulation needs to be developed. The nanocrystalline particles of pure drug produced by Nanoforming can lead to best-in-class performance, which enables optimal drug release and absorption because:

• the pure API particles produced permit greater flexibility in formulation development and selection of vehicles and excipients
• the narrow particle-size distribution achieved minimizes potential physical instabilities in suspension form; leading to consistent performance of the drug product
• Nanoformed injectable formulations have already been proven to outperform compositions based on nanomilled API, <link to TargTex case> and are proven to be beneficial when designing extended release implants.

Nanoform and Celanese Use Drug Nanoparticles to Modify the Release Kinetics of Ethylene Vinyl Acetate Long-acting Implants