Application of polyhydroxyalkanoates nanoparticles as intracellular sustained drug-release vectors.
Polyhydroxybutyrate (PHB), co-polyesters of 3-hydroxybutyrate and 3-hydroxyhexanoate (PHBHHx), and polylactic acid (PLA) were used to prepare nanoparticles with average sizes of 160, 250 and 150 nm, respectively. A lipid-soluble colorant, rhodamine B isothiocyanate (RBITC), was employed to study drug-release behaviors from these nanoparticles. A high RBITC drug-loading efficiency of over 75% was achieved with all PHA nanoparticles prepared. Macrophage endocytosis led to an intracellular RBITC drug sustained release over a period of at least 20 days for PHB and PHBHHx nanoparticles, while PLA nanoparticles and free drug lasted only 15 days and a week, respectively. Polymer properties and particle sizes showed little effect on drug-release behavior. This study showed for the first time that PHB and PHBHHx can be used effectively to achieve intracellular controlled drug releases.
Xiong
Yu-Cui
YC
Multidisciplinary Research Center, Shantou University, Shantou 515063, Guangdong, P. R. China.
Yao
Yong-Chao
YC
Zhan
Xiao-Yong
XY
Chen
Guo-Qiang
GQ
D000818:Animals; D002478:Cells, Cultured; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004705:Endocytosis; D006885:Hydroxybutyrates / Q000737:chemistry; D019344:Lactic Acid / Q000737:chemistry; D008264:Macrophages / Q000166:cytology; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry; D054813:Polyhydroxyalkanoates / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D012235:Rhodamines / Q000008:administration & dosage*; D000094122:Polyhydroxybutyrates
D003692:Delayed-Action Preparations; D006885:Hydroxybutyrates; D019344:Lactic Acid; D011091:Polyesters; D054813:Polyhydroxyalkanoates; D011108:Polymers; D012235:Rhodamines; C488798:poly(3-hydroxycaproate); C003182:poly-beta-hydroxybutyrate; D000094122:Polyhydroxybutyrates; C033616:poly(lactide); C027755:rhodamine isothiocyanate