Park Ji Hoon, Kwon Doo Yeon, Heo Ji Yeon, Park Seung Hun, Park Joon Yeong, Lee Bong, Kim Jae Ho, Kim Moon Suk
1Department of Molecular Science and Technology, Ajou University, 206 Worldcup-ro, Yeongtong-gu, Suwon, 16499 Korea.
2Department of Polymer Engineering, Pukyong National University, 365 Sinseon-ro, Nam-gu, Busan, 48547 Korea.
Tissue Eng Regen Med. 2017 Aug 31;14(6):743-753. doi: 10.1007/s13770-017-0077-7. eCollection 2017 Dec.
Here, we examined the effect of melting point of drug carriers on drug release of dexamethasone (Dex)-loaded microspheres. We prepared poly(L-lactide-ran-ε-caprolactone) (PLC) copolymers with varying compositions of poly(ε-caprolactone) (PCL) and poly(L-lactide) (PLLA). As the PLLA content increased, the melting points of PLC copolymers decreased from 61 to 43 °C. PLC copolymers in vials solubilized at 40-50 °C according to the incorporation of PLLA into the PCL segment. Dexamethasone (Dex)-loaded PLC (MCL) microspheres were prepared by the oil-in-water (O/W) solvent evaporation/extraction method. The preparation yields were above 70%, and the mean particle size ranged from 30 to 90 μm. The MCL microspheres also showed controllable melting points in the range of 40-60 °C. Dex-loaded MCL microspheres showed similar and sustained release patterns after the initial burst of Dex. The and order of the Dex release was MCL > MCL > MCL, which agreed well with the melting point order of the drug carrier. Using fluorescence imaging of fluorescein (FI)-loaded microspheres implanted in animals, we confirmed the sustained release of FI over an extended period. inflammation associated with the PLC microsphere implants was less pronounced than that associated with Poly(lactide-co-glycolide) (PLGA). In conclusion, we successfully demonstrated that it is possible to control Dex release using Dex-loaded MCL microspheres with different melting points.
在此,我们研究了药物载体熔点对载地塞米松(Dex)微球药物释放的影响。我们制备了具有不同聚(ε-己内酯)(PCL)和聚(L-丙交酯)(PLLA)组成的聚(L-丙交酯-ran-ε-己内酯)(PLC)共聚物。随着PLLA含量的增加,PLC共聚物的熔点从61℃降至43℃。根据PLLA掺入PCL链段的情况,小瓶中的PLC共聚物在40 - 50℃溶解。通过水包油(O/W)溶剂蒸发/萃取法制备了载地塞米松(Dex)的PLC(MCL)微球。制备产率高于70%,平均粒径范围为30至90μm。MCL微球的熔点也在40 - 60℃范围内可控。载Dex的MCL微球在Dex的初始突释后呈现出相似且持续的释放模式。Dex释放的顺序为MCL>MCL>MCL,这与药物载体的熔点顺序非常吻合。通过对植入动物体内的载荧光素(FI)微球进行荧光成像,我们证实了FI在较长时间内的持续释放。与PLC微球植入相关的炎症比与聚(丙交酯-共-乙交酯)(PLGA)相关的炎症不那么明显。总之,我们成功证明了使用具有不同熔点的载Dex的MCL微球来控制Dex释放是可行的。