Preparation and characterization of sodium ferulate entrapped bovine serum albumin nanoparticles for liver targeting.
Sodium ferulate (SF) loaded nanoparticles were prepared by desolvation procedure and subsequent cross-linking of the wall material of bovine serum albumin (BSA). Several factors in the nanoencapsulation process, such as the addition rate of the desolvation agent, composition of BSA and SF solution, amount of the cross-linker glutaraldehyde, were investigated to elucidate their influences on the particle size, zeta potential, drug loading and encapsulation efficiency of the resulted nanoparticles. The obtained spherical nanoparticles were negative charged with zeta potential from -20 to -40 mV, and characterized between 100 and 200 nm with a narrow size distribution. In the condition of introducing 1.0 mL 8% glutareldehyde per mg of BSA, the drug entrapment efficiency (EE) of 80% (w/w) and loading capacity of about 16% (w/w) could be achieved for the cross-linked BSA nanoparticles with SF encapsulated (SF-BSA-NP). And the drug EE was decreased along with the increasing amount of glutareldehyde used for cross-linking. The in vitro drug release properties of SF-BSA-NP behaved with an initial burst effect and then sustained-release stage. To some extent, the drug release rate could be adjusted by cross-linking with different amount of glutaraldehyde. Compared with SF solution, SF-BSA-NP showed a much higher drug distribution into liver and a lower drug concentration in other tissues, after intravenously injected to mice. So, BSA based nanoparticles might be a suitable controlled released carrier for the freely water-soluble drug SF and further hepatic targeted drug delivery.
Li
Feng-Qian
FQ
Department of Pharmaceutical Sciences, Changhai Hospital, Second Military Medical University, Shanghai 200433, China. fqlijr@gmail.com
Su
Hua
H
Wang
Jing
J
Liu
Ji-Yong
JY
Zhu
Quan-Gang
QG
Fei
Yi-Bo
YB
Pan
Yong-Hua
YH
Hu
Jin-Hong
JH
D000818:Animals; D003373:Coumaric Acids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D003432:Cross-Linking Reagents; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004563:Electrochemistry; D000431:Ethanol / Q000737:chemistry; D005343:Fibrinolytic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D007202:Indicators and Reagents; D008099:Liver / Q000187:drug effects*; D051379:Mice; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D010316:Particle Size; D012710:Serum Albumin, Bovine / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D014018:Tissue Distribution
D003373:Coumaric Acids; D003432:Cross-Linking Reagents; D005343:Fibrinolytic Agents; D007202:Indicators and Reagents; D012997:Solvents; D012710:Serum Albumin, Bovine; D000431:Ethanol; C004999:ferulic acid