Study Of Dry Powder Inhalation On Isoniazid Superparamagnetic Fe₃O₄Nanoparticle

Objective Tuberculosis is a long treating course chronic infectiousdiseases with lots of adverse reactions，Isoniazid (INH) is a first-line drugsto treat tuberculosis，but the side effects is huge.Most administration routesof INH is oral administration and intravenous injection. Due to pulmonaryadministration can enhance the clinical efficacy of INH significantly，thisarticle prepared to get Isoniazid superparamagnetic microspheres inhalation.guidanced by the magnetic field，inhalation target to lung，maybe it willimprove the local concentration and bioavailability of the drug，reduce thedrug Adverse reactions，the gastrointestinal tract，liver damage and thefrequency of administration. it will provide Tuberculosis treatment and thenew formulations of INH drug development.Methods Firstly Superparamagnetic iron oxide （SPIO） was madeby solvation-crosslinking method，then an external magnetic field wasprepared with Chongqing University.And1μm-5μm INH superparamagneticmicrospheres inhalation was made by spray drying method，and the natureof the microspheres and microspheres inhalation were detected.With thesame，the studies in vivo of rats and the effects of external magnetic field on the distribution of inhalation lung experiments were made.Results the average size of the SPIO is29.39nm，the PDI is0.185，the absolute value of zeta potential of the SPIO is approximately20，and thesaturation magnetization of8.223emu/g，the residual magnetization of0.0199emu/g，coercivity HC equal to1.7Oe.in line with the ultra-smallsuperparamagnetic iron oxide particle standard. Halbach magnet magneticstrength in depth from8-9cm greater than or equal20mT (200Gs)，in linewith the external magnetic field of magnetic nanoparticles in the bloodvessels of the basic requirements of bondage.The better prescription wasdiscovered，microspheres was small circular or elliptical particles in thesem，Dav=1.552μm，D90=2.351μm，the fitting coefficient=0.951， theparticle size and the dispersibility was good. Repose angle=38°,the tapdensity=0.298g/cm3，emptying rate was97.2%，the average depositionrate was42%in vitro. In pH=7.4PBS solution of the sustained release timewas8h in vitro experiments.Gained weight=12.4%，the microspheres shouldbe kept in a dry sealed jar，and at a temperature of4℃and25℃，the natureof the microspheres have no change within six months.The concentration ofmicrospheres in lung higher than other organs significantly.Themicrospheres of the group with quality unilateral Halbach magnetic fieldapplied magnetic field was more than the group without magnetic field.Conclusions The topic combine the advantages of the magneticfield， the magnetic targeting microspheres and DPI for the first time，The characteristics of the microspheres conformed with the regulations ofChinese pharmacopoeia.Not only avoiding the first pass effect，reducing thedosage，but also it can fix to the targeted areas by the influence of an externalmagnetic field，improve drug efficacy and reduce the damage to otherorgans.It improved patients’ compliance，and provided a way for new formsof treatment for tuberculosis with INH，it has greater economic and socialbenefits.