Mucoadhesive microparticles as potential carriers in inhalation delivery of doxycycline hyclate:a comparative study  

作　　者：Madhusmita Mishra Brahmeshwar Mishra 

机构地区：[1]Department of Pharmaceutics,Institute of Technology,Banaras Hindu University,Varanasi 221005,India

出　　处：《Acta Pharmaceutica Sinica B》2012年第5期518-526,共9页药学学报（英文版）

摘　　要：The present work compares and evaluates the suitability of different polymer-based microparticles for inhalation delivery of doxycycline hyclate.Mucoadhesive polymers,such as sodium carboxymethyl cellulose,sodium alginate,polyvinyl alcohol,polyvinylpyrolidone,starch,and carbopol were selected as carriers for inhalation delivery.Microparticles were prepared by spray drying and evaluated in terms of yield,moisture content,morphology,tapped density,encapsulation efficiency,in vitro mucoadhesion,thermal properties and in vitro aerosolization performance.Additionally,the cytotoxicity of the microparticles on H1299 human alveolar cell line was examined.Smooth spherical to collapsed doughnut shaped particles were formed.They exhibited tap densities of 0.202-0.502 g/cm^(3) and mass median aerodynamic diameter of 3.746.54 um.Mucoadhesion was highest in case of carbopol-based microparticles.Drug release from these microparticles exhibited biphasic Fickian type of diffusion.Only at the highest concentration of microparticles(1 mg/mL)less than 90% cell viability was seen in DX loaded sodium alginate microparticles(DXSA,87.2%),starch microparticles(DXST,85.1%)and carbopol microparticles(DXCP,82.7%)preparations after 48 h of exposure to alveolar cells.The results clearly indicate that sodium carboxymethyl cellulose-based microparticles may serve as an ideal carrier for inhalation delivery of doxycycline hyclate.

关 键 词：Mucoadhesive polymers Sodium carboxymethyl cellulose Sodium alginate Polyvinyl alcohol Polyvinylpyrrolidone Starch CARBOPOL Doxycycline hyclate Spray drying Aerosolization performance Inhalation microparticles 

分 类 号：R94[医药卫生—药剂学]