Folate-targeted drug-delivery systems prepared by nano-comminution

Abstract

Background: The size reduction ability of conventional wet comminution has been improved by proper polymeric stabilizer systems, and the resulting nano-comminution methods have led to the commercialization of many poorly water-soluble drugs after improving their bioavailability. During nano-comminution, polymer steric stabilizers physically adsorb onto the surface of drug particles. Method: In this study, the cross-linking and subsequent functionalization methods of the physically adsorbed polymers were used to widen the applicability of the nano-comminution. Chitosan was used as a steric stabilizer for two hydrophobic drugs, naproxen and paclitaxel. Results: Chitosan was successfully cross-linked (immobilized) by tripolyphosphate. The cross-linked stable polymer layer on drug nanoparticles was conjugated with folic acid, a model targeting moiety. The chemical reactions were performed without destroying the stabilities of drug nanosuspensions. The cross-linking and conjugation reactions significantly modified the release profiles of drug nanoparticles. Conclusion: This simple preparation method can be utilized to prepare novel drug encapsulations and folate-targeted delivery systems.

• Drug release
• milling
• nanoparticles
• particle size
• suspensions

Acknowledgments

SK would like to thank Human Resource Development BK21 (KRF) and the Human Resource Training Project for strategic technology (MKE & KOTEF).

Declaration of interest

This research was supported by the Ministry of Health and Welfare in South Korea (A090996). The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this paper.