The Study On Atropine/Cyclodextrin Eye Drops For Inhibiting The Development Of Myopia

Myopia is a very common eye disease,and is characterized by scleral thinning,localized ectasia of the posterior sclera and sclera remodeling.Studies have shown that atropine can inhibit scleral remodeling,thereby reducing the progression of myopia.The commercially available atropine eye drops have disadvantages of rapid elimination and low bioavailability and inaccessibility to sclera.In order to improve the sclera targeting effect and reduce the side effects like mydriasis and photophobia,this project provides a 1.0% atropine ? cyclodextrin eye drop(in the form of suspension)that combines with the inclusion effect of ? cyclodextrin,which is prepared by stirring.The eye drop was made in the form of freeze-dried powder with a dedicated solution to enhance its stability.The inclusion rate,osmotic pressure and sedimentation ratio were the indexes for prescription screening.The particle size of inclusion complex,PDI,moisture and redispersibility were the indexes for process screening.The inclusion complex was characterized by differential canning calorimetry and infrared spectroscopy.The atropine ? cyclodextrin eye drop was evaluated for release in vitro and quality,and the inclusion complex and eye drop were explored for stability.The sclera targeting effect was assessed based on the pharmacokinetic parameters of eye tissue in rabbits.The atropine ? cyclodextrin eye drop contains 1.0% atropine,18% ? cyclodextrin,0.05 mol/L of phosphate buffer,and 1.0% polyvinyl alcohol.The main process parameters include: stirring time 16 h,stirring rate 500 r/min,and preparation of inclusion complex powder using freeze drying method.The formation of inclusion complex was evidenced by the disappearance of atropine endothermic peak in the differential scanning calorimetry and the changes of characteristic peak in the infrared spectrum.The results of quality evaluation proved that the content of eye drop was in the range of 99.8%~100.3%,and the particle size,PDI,osmotic pressure,p H and sedimentation ratio all met the requirements for eye drop in the form of suspension.The in vitro release results also showed a certain sustained release effect of the eye drop.The stability study indicated that the inclusion complex was stable at a low temperature of-4?,and the stability of eye drop within 6 h met relevant requirements.By comparing the atropine ? cyclodextrin eye drop and atropine sulphate solution in terms of targeting index,targeting efficiency,peak concentration ratio and other indexes,it is concluded that the atropine ? cyclodextrin eye drop changes distribution of atropine in eye tissue and has a certain sclera targeting effect.