| Objective Establishment of the preparation process of icarrin nanoparticles by using the latest nanoparticle materials, followed by checking the icarrin release performance from the nanoparticles in vitro and in vivo.Methods The ICA was separately loaded into the Ca CO3 nanoparticles, solid lipid nanoparticles(SLN), and magnetic nano-liposomes(MNL). ICA was loaded into Ca CO3 nanoparticles by simply shaking the Ca CO3 powder in ICA solution. For ICA-SLN preparation, the ultrasonic emulsification was used coupled with materials melting at high temperature and solidification at low temperature. The membrane-sonic method was used to prepare ICA-MNL. To optimize the process, the encapsulation rate and the ICA loading rate were checked at various parameters. The ICA release performance was tested in vitro, in which ICA was detected by UV spectrometer; while it was tested in vivo, in which ICA concentration in rat serum was detected by HPLC coupled with mass spectrometry.Results The Ca CO3 nano-structured porous hollow microspheres to ICA had a high drug loading capacity of 34.18mg/g by UV-Vis spectrophotometer at 270 nm.Rats were intragastric administered by oral ICA and ICA/Ca CO3, The results demonstrate that the half-life of ICA and maximum absorption concentration were 1.51±0.42 h and 82.9±12.37(ng/m L), and the half-life of the ICA/Ca CO3 and maximum absorption concentration were 4.12±1.01 h and 51.1±31.35(ng/m L) by the LC-MS/MS determination of blood drug concentration, computational and statistics. Optimum formulation was as follows: Soybean Phosphatidylcholine of 500 mg, cholesterol of 150 mg,ICA of 60 mg,F-68 of 200 mg,PEG-2000 of 80 mg, The entrapment efficiency and the ratio of loading drug of ICA-SLN were(98.07±0.15)% and(6.47±0.14)% respectively.The cumulative release rate of ICA from PBS solution containing 30% methanol was near 99.97% in 9h and over 89.75% in 72 h. Rats were intragastric administered by oral ICA and ICA-SLN, The results demonstrate that the half-life of ICA and maximum absorption concentration were1.51±0.42 h and 82.9±12.37(ng/m L), and the half-life of the ICA-SLN and maximum absorption concentration were2.15±0.39 h and 165±25.16(ng/m L) by the LC-MS/MS determination of blood drug concentration, computational and statistics.Optimum ICA-MNLformulation was as follows:icariin-magnetic powder(2 : 1),F-68 of 200 mg, PEG-2000 of 60 mg,lecithin of 500 mg,cholesterol of 150 mg,PBS(p H7.4) as hydration medium.Entrapment efficiency of ICA-MNL was(96.57 ±0. 42) %; cumulative release rate of icariin solution was near 99. 68% in 16 h,but it was over 96. 51% in 72 h for ICA-MNL.Conclusion Preparation of ICA nanoparticles by nano-modified compared with the ICA, It is the absorption rate has being further improved in vivo. In contrast with ICA,the ICA/Ca CO3 has better to delay the release time in vivo,the ICA/Ca CO3 thus is a great choice as an oral sustained-release nano carrier materials.But,From promoting the oral drug absorption rate that the ICA-SLN is better. Because of ICA-MNL is Driving under magnetic field,For targeting medicine is selected about ICA is targeted therapy provide a possible in the future. Thus, loading of ICA into nanoparticles was a suggested way to develop ICA to clinic. Aim to the preparation of nanoparticles, this study gave more than one choice regarding the materials. |
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