Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs

TLDR

Nanocrystals are a carrier‑free colloidal delivery system in the nanometer range that enhance saturation solubility, dissolution rate, and membrane adhesiveness, making them attractive for poorly soluble drugs. Production of nanocrystals employs precipitation, milling, high‑pressure homogenization, and hybrid techniques such as NanoEdge, SmartCrystal, and PLH, with additional discussion of formulation conversion and future trends. Oral administration of nanocrystals improves pharmacokinetics, pharmacodynamics, safety, and targeted delivery, as highlighted in this review.

Abstract

Nanocrystals, a carrier-free colloidal delivery system in nano-sized range, is an interesting approach for poorly soluble drugs. Nanocrystals provide special features including enhancement of saturation solubility, dissolution velocity and adhesiveness to surface/cell membranes. Several strategies are applied for nanocrystals production including precipitation, milling, high pressure homogenization and combination methods such as NanoEdge™, SmartCrystal and Precipitation-lyophilization-homogenization (PLH) technology. For oral administration, many publications reported useful advantages of nanocrystals to improve in vivo performances i.e. pharmacokinetics, pharmacodynamics, safety and targeted delivery which were discussed in this review. Additionally, transformation of nanocrystals to final formulations and future trends of nanocrystals were also described.