Release performance and sustained-release efficacy of emamectin benzoate-loaded polylactic acid microspheres
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摘要
High-performance liquid chromatography(HPLC) was employed to determine drug release rates based on emamectin benzoate concentrations in the medium. Release kinetics equations were used to fit the drug release behavior. The effects of particle size and release medium p H on the release rate were also investigated. The indoor toxicity of emamectin benzoate-loaded polylactic acid microspheres on the diamondback moth larva(Plutella xylostella) was studied to explore drug sustained-release performance. In acidic and neutral media, the drug release behavior of the microspheres was in accord with the first-order kinetics equation. Increasing the spray dosage of emamectin benzoate-loaded polylactic acid microspheres initially resulted in an equivalent insecticidal efficacy with the conventional emamectin benzoate microemulsion. However, the drug persistence period was four-fold longer than that observed using the conventional formulation. The developed emamectin benzoate-loaded polylactic acid microspheres showed dramatic sustained-release performance. A treatment threshold of greater than 35 mg m L–1 was established for an efficient accumulated release concentration of emamectin benzoate-loaded microspheres.
High-performance liquid chromatography(HPLC) was employed to determine drug release rates based on emamectin benzoate concentrations in the medium. Release kinetics equations were used to fit the drug release behavior. The effects of particle size and release medium p H on the release rate were also investigated. The indoor toxicity of emamectin benzoate-loaded polylactic acid microspheres on the diamondback moth larva(Plutella xylostella) was studied to explore drug sustained-release performance. In acidic and neutral media, the drug release behavior of the microspheres was in accord with the first-order kinetics equation. Increasing the spray dosage of emamectin benzoate-loaded polylactic acid microspheres initially resulted in an equivalent insecticidal efficacy with the conventional emamectin benzoate microemulsion. However, the drug persistence period was four-fold longer than that observed using the conventional formulation. The developed emamectin benzoate-loaded polylactic acid microspheres showed dramatic sustained-release performance. A treatment threshold of greater than 35 mg m L–1 was established for an efficient accumulated release concentration of emamectin benzoate-loaded microspheres.
High-performance liquid chromatography(HPLC) was employed to determine drug release rates based on emamectin benzoate concentrations in the medium. Release kinetics equations were used to fit the drug release behavior. The effects of particle size and release medium p H on the release rate were also investigated. The indoor toxicity of emamectin benzoate-loaded polylactic acid microspheres on the diamondback moth larva(Plutella xylostella) was studied to explore drug sustained-release performance. In acidic and neutral media, the drug release behavior of the microspheres was in accord with the first-order kinetics equation. Increasing the spray dosage of emamectin benzoate-loaded polylactic acid microspheres initially resulted in an equivalent insecticidal efficacy with the conventional emamectin benzoate microemulsion. However, the drug persistence period was four-fold longer than that observed using the conventional formulation. The developed emamectin benzoate-loaded polylactic acid microspheres showed dramatic sustained-release performance. A treatment threshold of greater than 35 mg m L–1 was established for an efficient accumulated release concentration of emamectin benzoate-loaded microspheres.
引文
Barakat N S,Elbagory I M,Almurshedi A S.2008.Controlledrelease carbamazepine granules and tablets comprising lipophilic and hydrophilic matrix components.The American Association of Pharmaceutical Scientists,9,1054-1062.
Bodmeier R,Mcginity J M.1987.The preparation and evaluation of drug-containing poly(dl-lactide)microspheres formed by solvent evaporation method.Pharmaceutical Research,4,465-471.
Dong D W.2012.Preparation and characterization of melamineformaldehyde microcapsules filled with acetamiprid.MSc thesis,Beijing University of Chemical Technology,China.(in Chinese)
Fu L Y.2008.Research of the synthesis and the release rate of pesticide slowrelease substrate.MSc thesis,Heilongjiang University,China.(in Chinese)
Fu X D,Gao Y L.2003.Test for in vitro release rate of microspheres and correlation of its in vivo-in vitro.Chinese Journal of New Drugs,12,608-611.(in Chinese)
Han W Q.2010.Study on preparation of polylactic acid and poly lactic acid microspheres.MSc thesis,Beijing University of Chemical Technology,China.(in Chinese)
Huang B B,Zhong J B,Zhang X X,Yang F J,Wu Z J,Wu G.2011.Effect of ratio of core material to wall material on quality of microsphere of spinosad.Agrochenicals,50,714-717.(in Chinese)
Ioriatti C,Anfora G,Angeli G,Civolani S,Schmidt S,Pasqualini E.2009.Toxicity of emamectin benzoate to Cydia pomonella(L.)and Cydia molesta(Busck)(Lepidoptera:Tortricidae):Laboratory and field tests.Pest Management Science,65,306-312.
Kong L E.2012.The microencapsulation of three different pesticides and research of their controlled release properties.MSc thesis,Chinese Academy of Agricultural Sciences.(in Chinese)
Li W,Lu F S,Guo W T.2010.Preparation and characterization of emamectin benzoate microcapsules.Chinese Journal of Applied Chemistry,27,1381-1385.(in Chinese)
Lu Y.2006.Study proceedings of gelatin microsphere.The Science and Technology of Gelatin,26,57-68.(in Chinese)
Ma X Y,Shi S X,Xia Y Z.2004.Preparation and degradation of polylactide and its copolymer.Journal of Beijing University of Chemical Technology(Natural Science Edition),31,51-56.(in Chinese)
Nie Q,Chen P,Wu C.2004.Study on controlled release of the mixture of polylactide and drug.Chemical World,45,20-21,16.(in Chinese)
Reeve M S,Mccarthy S P,Gross R A.1993.Preparation and characterization of(R)-poly(β-hydroxybutyrate)-poly(ε-caprolactone)and(R)-poly(β-hydroxybutyrate)-poly(ε-lactide)degradable diblock copolymers.Macromolecules,26,888-894.
Sinclair R G.1973.Slow-release pesticide system.Polymers of lactic and glycolic acids as ecologically beneficial,costeffective encapsulating materials.Environmental Science&Technology,7,955-956.
Sun R X,Shi J J,Guo Y C.2008.Study of factors influencing diameter of gelatin microsphere.The Science and Technology of Gelatin,28,119-124,128.(in Chinese)
Tsuji H,Ikarashi K.2004.In vitro hydrolysis of polylactide crystalline residues as extended-chain crystallites III.Effects of p H and enzyme.Polymer Degradation and Stability,85,647-656.
Wu C,Zhang Y,Xu L.2007.Study on the release kinetics of OPC’s microcapsule.Chemistry and Adhesion,29,172-175.(in Chinese)
Wu Y K.2011.Preparation and evaluation of emamectin benzoate microcystis controlled release formulation.MSc thesis,Shanghai Normal University,China.(in Chinese)
Xing C C,Chen S H,Sun M.2011.Study on the release-kinetics of microcapsule of synthetic capsaicin.Chemical World,52,228-231,243.(in Chinese)
Zhang M,Cui C N,Song J.2008.Analysis of the factors influencing degradability and degradation mechanism of polylactic acid.Packaging Engineering,29,16-18,46.(in Chinese)
Zhang Y.2004.The review of microspheres for slowrelease pesticides.Herald of Medicine,23,843-844.(in Chinese)
Zhou X H,Liao L W,Zhang Z X.2010.Progress on preparation and its modification of microspheres for slowrelease pesticides.Agrochenicals,49,862-867,873.(in Chinese)
Zhu J,He Y,Gao M,Zhou W,Hu J,Shen J,Zhu Y C.2011.Photodegradation of emamectin benzoate and its influence on efficacy against the rice stem borer,Chilo suppressalis.Crop Protection,30,1356-1362.
Bodmeier R,Mcginity J M.1987.The preparation and evaluation of drug-containing poly(dl-lactide)microspheres formed by solvent evaporation method.Pharmaceutical Research,4,465-471.
Dong D W.2012.Preparation and characterization of melamineformaldehyde microcapsules filled with acetamiprid.MSc thesis,Beijing University of Chemical Technology,China.(in Chinese)
Fu L Y.2008.Research of the synthesis and the release rate of pesticide slowrelease substrate.MSc thesis,Heilongjiang University,China.(in Chinese)
Fu X D,Gao Y L.2003.Test for in vitro release rate of microspheres and correlation of its in vivo-in vitro.Chinese Journal of New Drugs,12,608-611.(in Chinese)
Han W Q.2010.Study on preparation of polylactic acid and poly lactic acid microspheres.MSc thesis,Beijing University of Chemical Technology,China.(in Chinese)
Huang B B,Zhong J B,Zhang X X,Yang F J,Wu Z J,Wu G.2011.Effect of ratio of core material to wall material on quality of microsphere of spinosad.Agrochenicals,50,714-717.(in Chinese)
Ioriatti C,Anfora G,Angeli G,Civolani S,Schmidt S,Pasqualini E.2009.Toxicity of emamectin benzoate to Cydia pomonella(L.)and Cydia molesta(Busck)(Lepidoptera:Tortricidae):Laboratory and field tests.Pest Management Science,65,306-312.
Kong L E.2012.The microencapsulation of three different pesticides and research of their controlled release properties.MSc thesis,Chinese Academy of Agricultural Sciences.(in Chinese)
Li W,Lu F S,Guo W T.2010.Preparation and characterization of emamectin benzoate microcapsules.Chinese Journal of Applied Chemistry,27,1381-1385.(in Chinese)
Lu Y.2006.Study proceedings of gelatin microsphere.The Science and Technology of Gelatin,26,57-68.(in Chinese)
Ma X Y,Shi S X,Xia Y Z.2004.Preparation and degradation of polylactide and its copolymer.Journal of Beijing University of Chemical Technology(Natural Science Edition),31,51-56.(in Chinese)
Nie Q,Chen P,Wu C.2004.Study on controlled release of the mixture of polylactide and drug.Chemical World,45,20-21,16.(in Chinese)
Reeve M S,Mccarthy S P,Gross R A.1993.Preparation and characterization of(R)-poly(β-hydroxybutyrate)-poly(ε-caprolactone)and(R)-poly(β-hydroxybutyrate)-poly(ε-lactide)degradable diblock copolymers.Macromolecules,26,888-894.
Sinclair R G.1973.Slow-release pesticide system.Polymers of lactic and glycolic acids as ecologically beneficial,costeffective encapsulating materials.Environmental Science&Technology,7,955-956.
Sun R X,Shi J J,Guo Y C.2008.Study of factors influencing diameter of gelatin microsphere.The Science and Technology of Gelatin,28,119-124,128.(in Chinese)
Tsuji H,Ikarashi K.2004.In vitro hydrolysis of polylactide crystalline residues as extended-chain crystallites III.Effects of p H and enzyme.Polymer Degradation and Stability,85,647-656.
Wu C,Zhang Y,Xu L.2007.Study on the release kinetics of OPC’s microcapsule.Chemistry and Adhesion,29,172-175.(in Chinese)
Wu Y K.2011.Preparation and evaluation of emamectin benzoate microcystis controlled release formulation.MSc thesis,Shanghai Normal University,China.(in Chinese)
Xing C C,Chen S H,Sun M.2011.Study on the release-kinetics of microcapsule of synthetic capsaicin.Chemical World,52,228-231,243.(in Chinese)
Zhang M,Cui C N,Song J.2008.Analysis of the factors influencing degradability and degradation mechanism of polylactic acid.Packaging Engineering,29,16-18,46.(in Chinese)
Zhang Y.2004.The review of microspheres for slowrelease pesticides.Herald of Medicine,23,843-844.(in Chinese)
Zhou X H,Liao L W,Zhang Z X.2010.Progress on preparation and its modification of microspheres for slowrelease pesticides.Agrochenicals,49,862-867,873.(in Chinese)
Zhu J,He Y,Gao M,Zhou W,Hu J,Shen J,Zhu Y C.2011.Photodegradation of emamectin benzoate and its influence on efficacy against the rice stem borer,Chilo suppressalis.Crop Protection,30,1356-1362.