Technology

Rilento is developing innovative drug delivery systems designed to manage pain after oral surgery. By using the FDA's 505(b)(2) regulatory pathway, Rilento can leverage existing knowledge of approved drugs to streamline the approval process. This approach allows them to efficiently demonstrate the effectiveness of their systems in treating not only oral surgery pain, but potentially other types of surgical and injury-related pain as well. Ultimately, Rilento aims to provide a preventative pain management strategy that reduces the need for opioid-based medications.

Rilento's drug delivery systems are designed to tackle pain after oral surgery by combining different medications for maximum effect. These systems can deliver an anesthetic alone, or pair it with anti-inflammatory painkillers that reduce swelling and pain by blocking COX1 and COX2 enzymes. This dual action helps prevent the initial pain from turning into a more sensitive, long-lasting pain state. By including a long-acting anesthetic, the system provides continuous pain relief for up to 72 hours after surgery. This extended release, combined with the anti-inflammatory action, aims to minimize pain and help patients regain normal function quickly after their procedure.

Cyclooxygenase-1 (Prostaglandin Synthase-1) in complex with a COX-1 selective inhibitor ⁽¹⁾

Cyclooxygenase-2 (Prostaglandin Synthase-2) in complex with a COX-2 selective inhibitor ⁽²⁾

(1) PDB: 1CQE; Picot D, Loll PJ, Garavito RM (January 1994). "The X-ray crystal structure of the membrane protein prostaglandin H2 synthase-1". Nature. 367 (6460): 243–9. doi:10.1038/367243a0. PMID 8121489.

(2) PDB: 6COX; Kurumbail RG, Stevens AM, Gierse JK, McDonald JJ, Stegeman RA, Pak JY, Gildehaus D, Miyashiro JM, Penning TD, Seibert K, Isakson PC, Stallings WC (1996). "Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents". Nature. 384 (6610): 644–8. doi:10.1038/384644a0. PMID 8967954.

Rilento uses a special micro-compounding process to create its drug delivery systems, carefully considering both the drug release profile and the practical aspects of manufacturing. This method allows them to fine-tune the system by adjusting the ingredients and their proportions.

For example, in their oral surgery products, Rilento optimizes both the drug release rate and the physical properties of the material. This ensures the system delivers the medication effectively while also being easy to manufacture and handle during surgery.

Formulation vehicles are being designed to co-disperse binder systems together with multi-modal particle size distributions of active-ingredients (anesthetics, analgesics, additives) into bioresorbable polymer-encapsulated particles within hydrophobic/hydrophilic and pH modulated phases. Although the state of dispersion can be regarded as an important factor that impacts the release profile, the key to release performance is in achieving reproducibility and consistency for any given state of dispersion (i.e., for a state of dispersion that simultaneously satisfies manufacturing constraints and end-use performance targets).