New Prospects for Therapeutic Organic Nanocrystals

Nanocrystals have emerged as an interesting class of delivery systems to solubilize pharmaceuticals belonging to classes II and IV of the Biopharmaceutics Classification System (BCS). This can be attributed to their small size and high drug content. More than 20 nanocrystal formulations have already been approved by the Food and Drug Administration (FDA) for oral and parenteral administration, with additional clinical trials in progress. This review provides an update on FDA-approved nanocrystals and current literature findings on their production using bottom-up techniques. Controlling drug supersaturation is a key step in this context. The beneficial surface-to-volume ratio enhances the dissolution rate of drugs compared to their solid form. Most monocrystal studies focus on diseases related to cancer and inflammation. We have concentrated on these areas, as well as new strategies aimed at combining drugs, including co-crystallization of drugs in nano-forms. Finally, we reviewed targeting approaches proposed for nanocrystals, which are primarily based on two main strategies: either grafting a ligand onto their surface or incorporating them into natural or modified membranes to facilitate homing to specific cells or tissues.