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


CONCLUSIONS
The release profiles of ATRA that was incorporated into the NAHis-GC nanoparticles were controlled by the NAHis content in the GC nanoparticles.
Department of Nuclear Medicine, Chonbuk National University Medical School, Jeonju, South Korea.
Chang-Moon
CM
Lee
Ji-Won
JW
Park
Jin
J
Kim
Dong-Woon
DW
Kim
Hwan-Jeong
HJ
Jeong
Ki-Young
KY
Lee
D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D006639:Histidine / Q000031:analogs & derivatives* / Q000737:chemistry; D008823:Micelles; D053758:Nanoparticles; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D013678:Technology, Pharmaceutical; D014212:Tretinoin / Q000008:administration & dosage* / Q000737:chemistry
D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008823:Micelles; C118638:glycol-chitosan; D011092:Polyethylene Glycols; D006639:Histidine; D014212:Tretinoin; D048271:Chitosan; C023495:N-acetylhistidine