Lipid-Polymer Hybrid Nanocarriers to Overcome Intestinal Permeability Barriers in Oral Delivery of Risedronate for Osteoporosis Therapy – A Review

Osteoporosis is a serious global health problem. It makes bones lose density and become weak over time, making fractures more common and imposing a huge economic burden on society. Risedronate sodium - is a common drug that is prescribed as a bisphosphonate for osteoporosis. However, it has extremely low oral bioavailability (<1%) due to not crossing the intestine very well, being eliminated quickly from the body, and binding strongly to dietary divalent cations. As a result, regular oral tablets fail to deliver the drug in an efficient and consistent way. Nanotechnology has provided new avenues for overcoming such barriers for poorly permeable medicines. Lipid-polymer hybrid nanoparticles (LPHNPs) are a contemporary nanocarrier platform that combines the predictable release and stability of polymeric nanoparticles with the friendliness and membrane touching properties of lipids. The polymer core contains the drug safely and prevents early interactions and the lipid layer around it enhances the adhesion to the intestinal wall and facilitates passage of the drug through cells. Recent studies demonstrate that LPHNPs can significantly improve a drug's stability, permeability and oral bioavailability.

Despite these merits, risedronate is yet to be widely tried in LPHNPs. Developing risedronate loaded LPHNPs could thus be a valuable strategy for enhancing the oral absorption of this drug, thereby improving the drug's therapeutic effect, and propel the forward the nanotechnology-based osteoporosis treatments.