Drug Delivery and Device Development, MedImmune, One MedImmune Way, Gaithersburg, MD, 20878, USA.
DelSiTech Ltd., PharmaCity, Itäinen Pitkäkatu 4 B, 20520, Turku, Finland.
Drug Deliv Transl Res. 2018 Apr;8(2):368-374. doi: 10.1007/s13346-017-0408-1.
Silica microparticle hydrogel depot (HG) formulation was prepared using spray drying of silica-based sol-gels for the sustained delivery of MR1 antibody which binds to CD40 ligand (CD40L). The formulation was tested in vitro for antibody release, surface morphology, particle size, rheology, and injectability. In vivo pharmacokinetic evaluation was performed for the microparticle formulation and free MR1 antibody in BALB/c female mice. Serum samples up to day 62 were assessed using an enzyme-linked immunosorbent assay. In vitro release indicated that the MR1 antibody was uniformly encapsulated in silica microparticles, and less than 5% burst release of the antibody was observed. In vivo pharmacokinetics showed a zero-order release up to 62 days from the MR1 silica microparticle HG-controlled release composition.
采用喷雾干燥法制备基于硅溶胶的硅胶微球水凝胶储库（HG），用于持续输送结合 CD40 配体（CD40L）的 MR1 抗体。对制剂进行了体外抗体释放、表面形态、粒径、流变学和可注射性测试。对 BALB/c 雌性小鼠进行了微球制剂和游离 MR1 抗体的体内药代动力学评价。使用酶联免疫吸附试验评估了长达 62 天的血清样本。体外释放表明 MR1 抗体均匀包裹在硅胶微球中，观察到不到 5%的抗体突释。体内药代动力学显示，MR1 硅胶微球 HG 控释组合物可在 62 天内实现零级释放。
