Studies on the oridonin-loaded poly(D,L-lactic acid) nanoparticles in vitro and in vivo.
The purpose of this paper was to investigate the possibility of developing a polymeric nanoparticle delivery system for ORI to increase its solubility, blood circulation time and tissue targeting. Oridonin-loaded poly(D,L-lactic acid) nanoparticles (ORI-PLA-NP) were prepared by the further modified spontaneous emulsion solvent diffusion (MSESD) method. Studies were carried out to characterize and evaluate the produced ORI-PLA-NP both in vitro and in vivo. The experimental results showed that the mean size of the nanoparticles were 137.3 nm, with 87.2% of the nanoparticles distributed between the range of 107 and 195 nm. The entrapment efficiency and actual drug loading of the nanoparticles were 91.88+/-1.83 and 2.32+/-0.05%, respectively. It was demonstrated by differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) that ORI existed in the form of amorphous in the nanoparticles. The in vitro release profile of ORI-PLA-NP could be expressed well by the Higuchi equation: Q=8.944t(1/2)+11.246. The results of pharmacokinetics demonstrated that being encapsulated in PLA nanoparticles was remarkably effective for ORI to prolong its blood circulation time. After the i.v. administration of ORI-PLA-NP, we could observe a stable and high concentration of ORI in liver, lung and spleen, while its distribution in heart and kidney decreased.
Xing
Jie
J
Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan, PR China.
Zhang
Dianrui
D
Tan
Tianwei
T
D000818:Animals; D004224:Diterpenes / Q000008:administration & dosage* / Q000493:pharmacokinetics; D045786:Diterpenes, Kaurane / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D019344:Lactic Acid / Q000737:chemistry*; D051379:Mice; D008815:Mice, Inbred Strains; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry* / Q000648:ultrastructure; D011091:Polyesters; D011108:Polymers / Q000737:chemistry*
D004224:Diterpenes; D045786:Diterpenes, Kaurane; D011091:Polyesters; D011108:Polymers; C011959:oridonin; D019344:Lactic Acid; C033616:poly(lactide)