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Nano‐in‐Micro Sildenafil Dry Powder Formulations for the Treatment of Pulmonary Arterial Hypertension Disorders: The Synergic Effect of POxylated Polyurea Dendrimers, PLGA, and Cholesterol
Particle & Particle Systems Characterization ( IF 2.7 ) Pub Date : 2020-05-06 , DOI: 10.1002/ppsc.201900447 Rita B. Restani 1 , Rita F. Pires 2 , Pedro V. Baptista 3 , Alexandra R. Fernandes 3 , Teresa Casimiro 1 , Vasco D. B. Bonifácio 2 , Ana Aguiar‐Ricardo 1
Particle & Particle Systems Characterization ( IF 2.7 ) Pub Date : 2020-05-06 , DOI: 10.1002/ppsc.201900447 Rita B. Restani 1 , Rita F. Pires 2 , Pedro V. Baptista 3 , Alexandra R. Fernandes 3 , Teresa Casimiro 1 , Vasco D. B. Bonifácio 2 , Ana Aguiar‐Ricardo 1
Affiliation
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POXylated polyurea dendrimer nanoparticles (PUREG4OOx48) are loaded with sildenafil (SDF) by a supercritical carbon dioxide–assisted (scCO2) impregnation. Further supercritical CO2‐assisted spray drying (SASD) leads to hybrid nano‐in‐micro dry powder formulations that are investigated aiming at efficient pulmonary delivery of SDF in pulmonary arterial hypertension treatment. This is the first report of the production of poly(D,L‐lactide‐co‐glycolide)‐cholesterol (PLGA‐Chol) microparticles processed by SASD. The optimized formulation of nano‐in‐microparticles is composed of PLGA, Chol, and PUREG4OOx48, loaded with SDF solutions in a 77:23 ratio (PLGA‐Chol:dendrimer, w/w). The dry powders are fully characterized and found to be highly biodegradable and biocompatible, and the SDF release profile evaluates under different pH values. The median mass average diameter (MMAD) of the nano‐in‐micro systems varies between 2.57 and 5 µm and the fine particle fraction (FPF) between 36% and 29% for PUREG4OMeOx48[PLGA‐Chol] and PUREG4OEtOx48[PLGA‐Chol], respectively. The data validate the potential use of these new formulations in inhalation therapy. In vitro studies are also carried out in order to evaluate the effect of the free drug in cell viability and formulations cytotoxicity.
中文翻译：
纳米微西地那非干粉制剂用于治疗肺动脉高压疾病：氧化聚脲树状大分子，PLGA和胆固醇的协同作用
通过超临界二氧化碳辅助（scCO 2）浸渍，将聚氧乙烯化的聚脲树状聚合物纳米颗粒（PURE G4 OOx 48）装载西地那非（SDF）。进一步的超临界CO 2辅助喷雾干燥（SASD）导致了混合纳米级微细干粉制剂的研究，旨在有效地在肺动脉高压治疗中通过SDF进行肺部递送。这是由SASD处理的聚（D，L-丙交酯-共-乙交酯）-胆固醇（PLGA-Chol）微粒生产的第一份报告。纳米微粒的优化配方由PLGA，Chol和PURE G4 OOx 48组成，以77:23的比例（PLGA-Chol：dendrimer，w / w）加载SDF解决方案。干粉具有充分的特性，并具有很高的生物降解性和生物相容性，并且SDF释放曲线在不同的pH值下进行评估。对于PURE G4 OMeOx 48 [PLGA-Chol]和PURE G4 OEtOx ，纳米微系统的平均质量平均直径（MMAD）在2.57和5 µm之间变化，细颗粒分数（FPF）在36％和29％之间变化48 [PLGA-Chol]。数据证实了这些新制剂在吸入疗法中的潜在用途。为了评估游离药物对细胞活力和制剂细胞毒性的影响，还进行了体外研究。
更新日期：2020-05-06
中文翻译：
纳米微西地那非干粉制剂用于治疗肺动脉高压疾病：氧化聚脲树状大分子，PLGA和胆固醇的协同作用
通过超临界二氧化碳辅助（scCO 2）浸渍，将聚氧乙烯化的聚脲树状聚合物纳米颗粒（PURE G4 OOx 48）装载西地那非（SDF）。进一步的超临界CO 2辅助喷雾干燥（SASD）导致了混合纳米级微细干粉制剂的研究，旨在有效地在肺动脉高压治疗中通过SDF进行肺部递送。这是由SASD处理的聚（D，L-丙交酯-共-乙交酯）-胆固醇（PLGA-Chol）微粒生产的第一份报告。纳米微粒的优化配方由PLGA，Chol和PURE G4 OOx 48组成，以77:23的比例（PLGA-Chol：dendrimer，w / w）加载SDF解决方案。干粉具有充分的特性，并具有很高的生物降解性和生物相容性，并且SDF释放曲线在不同的pH值下进行评估。对于PURE G4 OMeOx 48 [PLGA-Chol]和PURE G4 OEtOx ，纳米微系统的平均质量平均直径（MMAD）在2.57和5 µm之间变化，细颗粒分数（FPF）在36％和29％之间变化48 [PLGA-Chol]。数据证实了这些新制剂在吸入疗法中的潜在用途。为了评估游离药物对细胞活力和制剂细胞毒性的影响，还进行了体外研究。
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