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Preparation, Characterization and in vitro/in vivo Evaluation of Lovastatin-Loaded PLGA Microspheres by Local Administration for Femoral Head Necrosis
Drug Design, Development and Therapy ( IF 4.8 ) Pub Date : 2021-02-16 , DOI: 10.2147/dddt.s286306 Yang Sun 1 , Di Long 1
Drug Design, Development and Therapy ( IF 4.8 ) Pub Date : 2021-02-16 , DOI: 10.2147/dddt.s286306 Yang Sun 1 , Di Long 1
Affiliation
Background: The present work is an effort to develop a novel locally injection LVTT-loaded PLGA microspheres (LVTT-PLGA-MS) on the treatment of rabbits with femoral head necrosis (FHN).
Methods: LVTT-loaded PLGA microspheres (LVTT-PLGA MS) were prepared by an emulsion-solvent evaporation method. The physicochemical properties of LVTT-PLGA-MS were investigated to ensure that they have good qualities and are suitable for local delivery. In vitro drug release behavior of MS was also studied compared with free LVTT. In vivo, we also studied the pharmacokinetics and pharmacodynamics of MS in rabbits with the optimized formulation.
Results: In this study, we used the emulsion-solvent evaporation method to prepare LVTT-PLGA MS. Scanning electron microscopy demonstrated that the LVTT-PLGA MS were regular, round in shape and relatively unified size distributions were selected. The mean PS was 12.3± 2.1 μm. The drug-loading rate (27.6% ± 2.9%) was calculated for three batches of MS. The thermogram of LVTT-PLGA MS showed an endothermic peak at 98.3°C, revealing that LVTT existed in MS in an uncrystallized rather than a crystallized form. In the release study, LVTT-PLGA MS is observed linear prolonging drug release rates for more than 21 days without initial burst release. The pharmacodynamic results confirmed that the LVTT-PLGA MS had a good and lasting improvement effect against femoral head necrosis.
Conclusion: Our results demonstrated that LVTT-PLGA MS has the potential for being a local delivery system.
中文翻译：
洛伐他汀负载 PLGA 微球的制备、表征和体外/体内评价由当地政府用于治疗股骨头坏死
背景：目前的工作是开发一种新型局部注射 LVTT 负载 PLGA 微球 (LVTT-PLGA-MS)，用于治疗兔股骨头坏死 (FHN)。
方法：采用乳液-溶剂蒸发法制备负载LVTT的PLGA微球（LVTT-PLGA MS）。对 LVTT-PLGA-MS 的理化性质进行了研究，以确保它们具有良好的品质并适合本地交付。还研究了 MS 与游离 LVTT 相比的体外药物释放行为。在体内，我们还用优化的配方研究了 MS 在兔体内的药代动力学和药效学。
结果：在本研究中，我们使用乳液-溶剂蒸发法制备 LVTT-PLGA MS。扫描电镜表明，LVTT-PLGA MS 呈规则、圆形，选择了相对统一的尺寸分布。平均 PS 为 12.3± 2.1 μm。计算了三批 MS 的载药率 (27.6% ± 2.9%)。LVTT-PLGA MS 的热谱图在 98.3°C 处有一个吸热峰，表明 LVTT 在 MS 中以非结晶形式而不是结晶形式存在。在释放研究中，观察到 LVTT-PLGA MS 线性延长药物释放速率超过 21 天，而没有初始突释。药效学结果证实，LVTT-PLGA MS对股骨头坏死具有良好且持久的改善作用。
结论：我们的结果表明，LVTT-PLGA MS 具有成为本地交付系统的潜力。
更新日期：2021-04-20
Methods: LVTT-loaded PLGA microspheres (LVTT-PLGA MS) were prepared by an emulsion-solvent evaporation method. The physicochemical properties of LVTT-PLGA-MS were investigated to ensure that they have good qualities and are suitable for local delivery. In vitro drug release behavior of MS was also studied compared with free LVTT. In vivo, we also studied the pharmacokinetics and pharmacodynamics of MS in rabbits with the optimized formulation.
Results: In this study, we used the emulsion-solvent evaporation method to prepare LVTT-PLGA MS. Scanning electron microscopy demonstrated that the LVTT-PLGA MS were regular, round in shape and relatively unified size distributions were selected. The mean PS was 12.3± 2.1 μm. The drug-loading rate (27.6% ± 2.9%) was calculated for three batches of MS. The thermogram of LVTT-PLGA MS showed an endothermic peak at 98.3°C, revealing that LVTT existed in MS in an uncrystallized rather than a crystallized form. In the release study, LVTT-PLGA MS is observed linear prolonging drug release rates for more than 21 days without initial burst release. The pharmacodynamic results confirmed that the LVTT-PLGA MS had a good and lasting improvement effect against femoral head necrosis.
Conclusion: Our results demonstrated that LVTT-PLGA MS has the potential for being a local delivery system.
中文翻译：
洛伐他汀负载 PLGA 微球的制备、表征和体外/体内评价由当地政府用于治疗股骨头坏死
背景：目前的工作是开发一种新型局部注射 LVTT 负载 PLGA 微球 (LVTT-PLGA-MS)，用于治疗兔股骨头坏死 (FHN)。
方法：采用乳液-溶剂蒸发法制备负载LVTT的PLGA微球（LVTT-PLGA MS）。对 LVTT-PLGA-MS 的理化性质进行了研究，以确保它们具有良好的品质并适合本地交付。还研究了 MS 与游离 LVTT 相比的体外药物释放行为。在体内，我们还用优化的配方研究了 MS 在兔体内的药代动力学和药效学。
结果：在本研究中，我们使用乳液-溶剂蒸发法制备 LVTT-PLGA MS。扫描电镜表明，LVTT-PLGA MS 呈规则、圆形，选择了相对统一的尺寸分布。平均 PS 为 12.3± 2.1 μm。计算了三批 MS 的载药率 (27.6% ± 2.9%)。LVTT-PLGA MS 的热谱图在 98.3°C 处有一个吸热峰，表明 LVTT 在 MS 中以非结晶形式而不是结晶形式存在。在释放研究中，观察到 LVTT-PLGA MS 线性延长药物释放速率超过 21 天，而没有初始突释。药效学结果证实，LVTT-PLGA MS对股骨头坏死具有良好且持久的改善作用。
结论：我们的结果表明，LVTT-PLGA MS 具有成为本地交付系统的潜力。
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