PLA对贝美前列素植入剂体外释放行为影响的考察

Investigation on Effect of PLA on in vitro Release Behavior of Bimatoprost Implants

高眼压是不可逆性眼病的重要原因,但传统滴眼液存在诸多缺点,为了开发长效缓释的眼用植入剂,考察了聚丙交酯(PLA)对贝美前列素植入剂体外释放行为的影响。采用溶剂挥发-热熔挤出的方法制备了长5 mm、直径0.5 mm、载药量20%的贝美前列素-聚乙交酯丙交酯(PLGA)植入剂。通过考察加入不同量PLA的植入剂的体外释放度、扫描电镜下的微观形态和释放过程中的质量损失,探究PLA对释药行为的影响。体外释放试验表明,添加PLA能减缓释药速率,延长释药周期,其中含30% PLA的植入剂较不添加PLA的植入剂释药时间延长20 d。并且,加入PLA能降低突释量,随着PLA添加量的增多,突释量减少。

Ocular hypertension is an important cause of irreversible eye disease.But traditional eye drops have many shortcomings.In order to develop long-acting sustained-release ocular implants,the effect of polylactide(PLA)on in vitro release behavior of bimatoprost implants was investigated.The solvent-evaporation method combined with hot-melt extrusion was adopted to prepare bimatoprost poly(lactide-co-glycolide)(PLGA)implants with a length of 5 mm,a diameter of 0.5 mm and a drug loading of 20%.Then,the implants containing different amounts of PLA were characterized by in vitro release,scanning electron microscopy(SEM)and mass loss after exposure to the release medium.The in vitro release showed that adding PLA could slow down the drug release rate and prolong the drug release time.The release time of the implants containing 30%PLA was 20 days longer than that of the implants without PLA.Besides,adding PLA could reduce the burst release amount.The burst release amount decreased with the increasing of adding amount of PLA.