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Studies on preparation of albendazole and its chitosan microspheres for hepatic artery embolization

Liang Zhang

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Abstract

Objective This article chooses chistosan with excellent formability as a carrier,albendazole as model drug to study the preparation technique of albendazole solid dispersions.And albendazole-loaded chitosan microspheres(ABZ-LSD-CS)were futher prepared.The encapsulation efficiency,drug-loading amount,average diameter,superficial shape,and physical and chemical properties were also investigated.Methods Albendazole-loaded chitosan microspheres for embolization were achieved by emulsification cross-linking process with liquid paraffin as oil phase,Span-80 as emulsifier,and glutaraldehyde as cross linking agent.The surface characterization of the microspheres was identified with scanning electronic microscope(SEM),and the particle size and distribution of microspheres were analyzed by optical microscope.(FT-IR) and XRD and DSC were used to characterize microspheres.In vitro dynamic dialysis method was used to determine the drug release property of microspheres in different media conditions.Results A novel microspheres with a global shape and narrow distribution were prepared.The average diameter was about(153±7)μm,drug-loading amount was(20.92±0.15)%,and encapsulation efficiency was(25.37±0.22)%.The drug release behavior in 0.1mol/L HCl,phosphate buffered saline(pH =3.5),phosphate buffered saline(pH =7.4) and physiological saline was slow.The release in pH =3.5 was best of all,which conformed to weibull distribution model.Conclusion The prepared ABZ-LSD-CS have a good property of high drug loading amount and entrapment efficiency,whose surfaces were smooth and round.The in vitro release time of drug was increased obviously,so that sustained drug release was achieved.The preparation technique is very feasible.

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Objective This article chooses chistosan with excellent formability as a carrier,albendazole as model drug to study the preparation technique of albendazole solid dispersions.And albendazole-loaded chitosan microspheres(ABZ-LSD-CS)were futher prepared.The encapsulation efficiency,drug-loading amount,average diameter,superficial shape,and physical and chemical properties were also investigated.Methods Albendazole-loaded chitosan microspheres for embolization were achieved by emulsification cross-linking process with liquid paraffin as oil phase,Span-80 as emulsifier,and glutaraldehyde as cross linking agent.The surface characterization of the microspheres was identified with scanning electronic microscope(SEM),and the particle size and distribution of microspheres were analyzed by optical microscope.(FT-IR) and XRD and DSC were used to characterize microspheres.In vitro dynamic dialysis method was used to determine the drug release property of microspheres in different media conditions.Results A novel microspheres with a global shape and narrow distribution were prepared.The average diameter was about(153±7)μm,drug-loading amount was(20.92±0.15)%,and encapsulation efficiency was(25.37±0.22)%.The drug release behavior in 0.1mol/L HCl,phosphate buffered saline(pH =3.5),phosphate buffered saline(pH =7.4) and physiological saline was slow.The release in pH =3.5 was best of all,which conformed to weibull distribution model.Conclusion The prepared ABZ-LSD-CS have a good property of high drug loading amount and entrapment efficiency,whose surfaces were smooth and round.The in vitro release time of drug was increased obviously,so that sustained drug release was achieved.The preparation technique is very feasible.

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Available abstract

Objective This article chooses chistosan with excellent formability as a carrier,albendazole as model drug to study the preparation technique of albendazole solid dispersions.And albendazole-loaded chitosan microspheres(ABZ-LSD-CS)were futher prepared.The encapsulation efficiency,drug-loading amount,average diameter,superficial shape,and physical and chemical properties were also investigated.Methods Albendazole-loaded chitosan microspheres for embolization were achieved by emulsification cross-linking process with liquid paraffin as oil phase,Span-80 as emulsifier,and glutaraldehyde as cross linking agent.The surface characterization of the microspheres was identified with scanning electronic microscope(SEM),and the particle size and distribution of microspheres were analyzed by optical microscope.(FT-IR) and XRD and DSC were used to characterize microspheres.In vitro dynamic dialysis method was used to determine the drug release property of microspheres in different media conditions.Results A novel microspheres with a global shape and narrow distribution were prepared.The average diameter was about(153±7)μm,drug-loading amount was(20.92±0.15)%,and encapsulation efficiency was(25.37±0.22)%.The drug release behavior in 0.1mol/L HCl,phosphate buffered saline(pH =3.5),phosphate buffered saline(pH =7.4) and physiological saline was slow.The release in pH =3.5 was best of all,which conformed to weibull distribution model.Conclusion The prepared ABZ-LSD-CS have a good property of high drug loading amount and entrapment efficiency,whose surfaces were smooth and round.The in vitro release time of drug was increased obviously,so that sustained drug release was achieved.The preparation technique is very feasible.

Key concepts: Glutaraldehyde, Hepatic artery embolization, Albendazole, Materials science, Chitosan, Particle size, Chromatography, Microsphere

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