Influence of histidine on the release of all-trans retinoic acid from self-assembled glycol chitosan nanoparticles

Abstract

Objective: In this study, the influence of N-acetyl histidine (NAHis) on the all-trans retinoic acid (ATRA) release from the NAHis-conjugated self-assembled glycol chitosan (GC) nanoparticles was investigated. Methods: NAHis was conjugated to GC as a hydrophobic moiety to prepare the self-assembled nanoparticles, and ATRA was incorporated into the inner core of the NAHis–GC nanoparticles. The ATRA release from NAHis–GC nanoparticles was performed at 37°C in a phosphate-buffered saline buffer (pH 5.5 or 7.4) for 48 hours. Results: At a pH of 5.5, less than 20% (w/w) of total loading amount of ATRA was released from the nanoparticles after 48 hours. In contrast, two times greater amount of ATRA was released at a pH of 7.4. The ATRA release rate from the NAHis–GC nanoparticles was significantly slower at a pH of 5.5 than at a pH of 7.4. Conclusion: The release profiles of ATRA that was incorporated into the NAHis–GC nanoparticles were controlled by the NAHis content in the GC nanoparticles.

Keywords:

• All-trans retinoic acid
• controlled release
• glycol chitosan
• histidine
• self-assembled nanoparticles

Acknowledgments

This research was financially supported by the Ministry of Education, Science Technology (MEST) and Korea Institute for Advancement of Technology (KIAT) through the Human Resource Training Project for Regional Innovation. This study was also supported by a grant from the National R&D Program for Cancer Control, Ministry for Health, Welfare and Family affairs, Republic of Korea (0620220 and 0720420).

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this paper.