Based on in vivo fluorescence imaging technology, to extablish a fluorescence modification method for amphipathic block polymers / 药学学报

Rhodamine B (RhB) was used to decorate an amphipathic block polymers (β-CD-[P(AA-co-MMA)-b-PVP]4) in this study. First, after activated by 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, rhodamine B was marked with hydroxyethyl methacrylate (HEMA) through ester exchange reaction. Second, the labeled amphipathic block polymers (β-CD-[P(AA-(HEMA-RhB)-MMA)-b-PVP]4) were synthesized after polymerization reaction of double bones between RhB-HEMA and other reactants. Finally, the structure of product was measured by FT-IR spectra and fluorospectro photometer (FLUORO). The critical micelle concentration of RhB-labeled and unlabeled amphipathic block polymers were 4.96×10-3, 5.09×10-3 mg·L-1, respectively, indicating no change of their micellization behavior. In vivo tissue distribution and whole-body fluorescent imaging were studied by vinpocetine (VP)-loaded polymeric micelles which were prepared through a solvent evaporation method. Compared to the result of in vivo tissue distribution and whole-body fluorescence imaging, a similar bio-distribution behavior of VP-loaded polymeric micelles was found. Those proved the successful fluorescence modification with a labeling yield of 4.13%. With in vivo fluorescence imaging technology, we established a fluorescence method for modification of amphipathic block polymers.

Relation between drug release and the drug status within curcumin-loaded microsphere / 药学学报

To study the relation between drug release and the drug status within curcumin-loaded microsphere, SPG (shirasu porous glass) membrane emulsification was used to prepare the curcumin-PLGA (polylactic-co-glycolic acid) microspheres with three levels of drug loading respectively, and the in vitro release was studied with high-performance liquid chromatography (HPLC). The morphology of microspheres was observed with scanning electron microscopy (SEM), and the drug status was studied with X-ray diffraction (XRD), differential scanning calorimetry (DSC) and infrared analysis (IR). The drug loading of microspheres was (5.85 ± 0.21) %, (11.71 ± 0.39) %, (15.41 ± 0.40) %, respectively. No chemical connection was found between curcumin and PLGA. According to the results of XRD, curcumin dispersed in PLGA as amorphous form within the microspheres of the lowest drug loading, while (2.12 ± 0.64) % and (5.66 ± 0.07) % curcumin crystals was detected in the other two kinds of microspheres, respectively, indicating that the drug status was different within three kinds of microspheres. In the data analysis, we found that PLGA had a limited capacity of dissolving curcumin. When the drug loading exceeded the limit, the excess curcumin would exist in the form of crystals in microspheres independently. Meanwhile, this factor contributes to the difference in drug release behavior of the three groups of microspheres.

Relation between drug release and the drug status within curcumin-loaded microsphere / 药学学报

To study the relation between drug release and the drug status within curcumin-loaded microsphere, SPG (shirasu porous glass) membrane emulsification was used to prepare the curcumin-PLGA (polylactic-co-glycolic acid) microspheres with three levels of drug loading respectively, and the in vitro release was studied with high-performance liquid chromatography (HPLC). The morphology of microspheres was observed with scanning electron microscopy (SEM), and the drug status was studied with X-ray diffraction (XRD), differential scanning calorimetry (DSC) and infrared analysis (IR). The drug loading of microspheres was (5.85 ± 0.21)%, (11.71 ± 0.39)%, (15.41 ± 0.40)%, respectively. No chemical connection was found between curcumin and PLGA. According to the results of XRD, curcumin dispersed in PLGA as amorphous form within the microspheres of the lowest drug loading, while (2.12 ± 0.64)% and (5.66 ± 0.07)% curcumin crystals was detected in the other two kinds of microspheres, respectively, indicating that the drug status was different within three kinds of microspheres. In the data analysis, we found that PLGA had a limited capacity of dissolving curcumin. When the drug loading exceeded the limit, the excess curcumin would exist in the form of crystals in microspheres independently. Meanwhile, this factor contributes to the difference in drug release behavior of the three groups of microspheres.