Preparation and characterization of modified lipid nanoparticles for doxorubicin controlled release.
Low drug encapsulation efficiency and burst release are the main drawbacks of lipid nanoparticles. To solve these problems, lipid nanoparticles containing a cross-linked lipid network were prepared in this study. Monostearin (MS) and octadecylamine (ODA) were used as the solid lipids, and oleic acid (OA) was used as liquid lipid. The use of a small amount of ODA was to form cross-linked network by glutaraldehyde in the presence of OA. Using doxorubicin (DOX) as a model drug, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and glutaraldehyde cross-linked NLC were prepared. The physicochemical properties of these lipid nanoparticles such as average diameter, drug loading, drug encapsulation efficiency and in vitro drug release were investigated. The drug loading capacities and encapsulation efficiency were improved by mixing OA with the solid lipids to produce the nanoparticle matrix, and were further increased by the cross-linking of glutaraldehyde. The faster drug release was obtained when the NLC with higher OA content. After cross-linking by glutaraldehyde, the burst release of DOX from NLC could be reduced, in comparison to both SLN and non cross-linked NLC. The results indicated the NLC with cross-linked network are a potential drug delivery system with improved drug encapsulation and controlled drug release.
Ying
Xiao-Ying
XY
College of Pharmaceutical Science, Zhejiang University, Hangzhou, PR China.
Du
Yong-Zhong
YZ
Chen
Wan-Wei
WW
Yuan
Hong
H
Hu
Fu-Qiang
FQ
D000465:Algorithms; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry; D003432:Cross-Linking Reagents; D004058:Diffusion; D004317:Doxorubicin / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D004563:Electrochemistry; D005976:Glutaral / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles; D010316:Particle Size; D012995:Solubility
D000903:Antibiotics, Antineoplastic; D003432:Cross-Linking Reagents; D004337:Drug Carriers; D008055:Lipids; D004317:Doxorubicin; D005976:Glutaral