ABSTRACT
Objective:To use polylactic-co-glycolic acid(PLGA) as vector material to prepare the compound total flavonoids of Rhizoma Drynariae(TFRD) and total flavonoids of Chrysanthemum(TFC) sustained release microcapsule TF-PLGA microcapsules,and to investigate the the best preparation technique of TF-PLGA microcapsules and their sustained release characteristics in vitro.Methods:The TF-PLGA microcapsules were prepared with TFRD,TFC,and PLGA by emulsifying-solvent evaporation technique under certain conditions.With the encapsulation efficiency(EE) as the evaluation indicator,the optimal formulation was verified by single factor experiment and orthogonal design;the general morphology,the particle size and distribution of the microcapsules were observed by light microscope(LM) and scanning electron microscope(SEM);the cumulative drug release rate of TF-PLGA microcapsules was detected by constant temperature commotion method in vitro and the release curves of the TF-PLGA were drawn.Results:The optimal prescription was as follows:the concentration of PLGA was 140 g·L-1,oil phase volume was 1.4 mL,emulsifying speed was 900 r·min-1,emulsifying time was 5 min,the average EE was(83.89±2.30)%,and the average drug loading rate(DL) was(5.90±0.07)%.The LM and SEM resluts showed that the TF-PLGA microcapsules presented as round ball,the average particle size was(44.34±14.68)μm,and the distribution was relatively narrow.The drug release in vitro results showed that the initial drug release rate(24 h)was about 40%,and the cumulative drug release rate was over 90% after 50 d.Conclusion:The TF-PLGA sustained release microcapslue has better drug-loaded and sustained-release effects with simple preparation technique and better repeatability.
ABSTRACT
Aim To investigate the effect of total flavonoids of Chrysanthemum indicum on proliferation of synoviocytes and TRAIL/TNF-? expression of synovial tissue with adjuvant arthritis rats.Methods SD rats were divided randomly into six groups including normol,model,TFC(84,168,336 mg?kg-1)and control drug Tripterygium glycosides(30 mg?kg-1)groups.Adjuvant arthritis rat model was induced by a single intradermal injection of 0.1 ml of the complete Freund's adjuvant into the the right hind feet pads of the SD rats.The proliferation of synoviocyte was measured by MTT;The expression of TRAIL and TNF-? on synovial tissue were detected by means of immunofluorescence.Results TFC was shown to suppress the excessive synoviocyte proliferation;The expression of TRAIL was lower in model group than that of the normal group.TFC can increase the expression of TRAIL protein;The contrary to TNF-? protein.Conclusions TRAIL play a role in the development of AA.TFC can increase the lower expression of TRAIL protein,that maybe one of the mechanisms of TFC improvement AA.
ABSTRACT
Objective To study the effect of the extract of total flavonoids of Chrysanthemum indicum(TFC) on adjuvant arthritis(AA) synoviocytes.Methods Totally 0.1ml of the complete Freund's adjuvant was subcutaneously injected into the right hind feet pads of 20 SD rats.24 days after immunity synoviocytes in the knee joint were treated with TFC.Cell morphology was examined with electron microscopy.Protein level of caspase-3 cleaved fragments was analyzed by Western blotting.The annexin V stain assay was applied to explore the effect of caspase-3 inhibitor on the amelioration in synovial cells apoptosis of AA rats.Results Typical morphology and biochemical feature of apoptosis in synovial cells of AA rats were observed with TFC.The protein level of caspase-3 cleaved fragments increased obviously and was related with the concentration of TFC in synovial cells of AA rats.The apoptotic cells positively stained with annexin V were markedly reduced by caspase-3 inhibitor.Conclusion TFC can induce apoptosis in AA rats synoviocytes,which may achieve therapeutical effects in AA.The activation of caspase-3 may be one of the main causations.
ABSTRACT
Objective To study the effect of the extract of total flavonoids of chrysanthemum indicum(TFC) on adjuvant arthritis synovial cells. Methods 0.1ml of the complete Freund's adjuvant was subcutaneously injected into the right hind feet pads of the SD rats.24 days after immunity synovial cells in knee joint were treated with TFC and inhibition of proliferation was measured with MTT assay.DNA fragmentations were analyzed with DNA gel electrophoresis.Fluorescence staining of Hoechst 33258 to observe apoptotic body.Results The IC_50 of TFC on synovial cells was 112mg/L.DNA gel electrophoresis showed ladder-like strap.Apoptotic bodies were observed by Hoechst 33258.Conclusion TFC can inhibit proliferation and induce apoptosis in synovial cells,and exerts therapeutical effect on rheumstoid arthritis.