醋酸甲孕酮
微粒
电喷雾
同轴
车辆段
材料科学
PLGA公司
化学
剂型
控制释放
生物医学工程
色谱法
医学
纳米技术
化学工程
纳米颗粒
内科学
质谱法
雌激素
考古
工程类
电气工程
历史
作者
Jie Tang,Richard Schutzman,Carlos E. Alfaro Rodríguez,Joerg Lahann,Naír Rodríguez-Hornedo,Mark R. Prausnitz,Steven P. Schwendeman
标识
DOI:10.1016/j.jconrel.2021.12.017
摘要
Despite its high efficacy and good patient compliance, the only long-acting injectable (LAI) contraceptive currently available in the US, depot medroxyprogesterone acetate (DMPA), is limited by significant side effects and a delayed return to fertility for up to 10 months after its intended duration of action. To overcome these limitations, we sought to develop an injectable poly(D,l-lactide) (PLA) microparticle for sustained release of contraceptive hormone, etonogestrel (ENG). A one-step technique, coaxial electrospray method was applied to prepare uniform ENG loaded core-shell structured and slow-degrading PLA microparticles (ENG-cs-MPs) to provide release control while minimizing polymer content. By adjusting voltage, polymer concentration and flow rate of the coaxial jetting solution, the prepared ENG-cs-MPs exhibited uniformly small particle size with volume mean diameter of 14.7 ± 0.5 μm and a shell thickness of 2.5 ± 0.1 μm, high drug loading of ~54%, high encapsulation efficiency of ~99%, and initial 1-day burst release of just ~10%. Long-term in vitro release of ENG was continuous for more than 3 months without change of the shell structure in 6 months. In PK studies, ENG-cs-MPs achieved a steady and continuous drug release for approximately 3 months and then quickly tapered off within 3 weeks. Hence, ENG-cs-MPs prepared by the coaxial electrospray method may be useful as a LAI contraceptive with an improved PK profile relative to DMPA.
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