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

摘要

Abstract > POXylated polyurea dendrimer nanoparticles (PURE <sub>G4</sub> OOx <sub>48</sub> ) are loaded with sildenafil (SDF) by a supercritical carbon dioxide–assisted (scCO <sub>2</sub> ) impregnation. Further supercritical CO <sub>2</sub> ‐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 PURE <sub>G4</sub> OOx <sub>48</sub> , 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 PURE <sub>G4</sub> OMeOx <sub>48</sub> [PLGA‐Chol] and PURE <sub>G4</sub> OEtOx <sub>48</sub> [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. </abstract> </span> <span class="z_kbtn z_kbtnclass hoverxs" style="display: none;">展开▼</span> </div> <div class="translation abstracttxt"> <span class="zhankaihshouqi fivelineshidden" id="abstract"> <span>机译：</span><Abstract Type =“Main”XML：Lang =“en”> <标题类型=“main”>抽象</ title> > Poxylated Polyurea树枝状聚合物纳米粒子（纯净 <sub> g4 </ sub> oox. <sub> 48 </ sub> ）通过超临界二氧化碳辅助（SCCO）与Sildenafil（SDF）一起装载 <sub> 2 </ sub> ）浸渍。进一步超临界CO. <sub> 2 </ sub> -Assisted喷雾干燥（SASD）导致杂交纳米型微型干粉配方，其研究旨在在肺动脉高压处理中的高效肺部递送。这是Poly（D，L-丙交酯 - ）生产的第一个报告 co </ i> -Glycolide） - 通过SASD加工的硫醇（PLGA-CHOL）微粒。纳米微粒的优化制剂由PLGA，CHOL和纯净组成 <sub> g4 </ sub> oox. <sub> 48 </ sub> ，以77:23的比率（PLGA-CHOL：树枝状大分子，W / W）负载。干粉完全表征并发现是高度可生物降解和生物相容性的，并且SDF释放曲线在不同的pH值下评估。纳米微系统的中值平均直径（MMAD）在2.57和5μm之间变化，细颗粒馏分（FPF）在36％和29％之间为纯度 <sub> g4 </ sub> OMEOX. <sub> 48 </ sub> [PLGA-CHOL]和纯净 <sub> g4 </ sub> oetox. <sub> 48 </ sub> [PLGA-CHOL]分别。数据验证了吸入治疗中这些新配方的潜在使用。还进行体外研究，以评估游离药物在细胞活力和制剂细胞毒性中的作用。 </ p> </摘要> </span> <span class="z_kbtn z_kbtnclass hoverxs" style="display: none;">展开▼</span> </div> </div> <div class="record"> <h2 class="all_title" id="enpatent33" >著录项</h2> <ul> <li> <span class="lefttit">来源</span> <div style="width: 86%;vertical-align: text-top;display: inline-block;"> <a href='/journal-foreign-28901/'>《Particle & Particle Systems Characterization: Measurement and Description of Particle Properties and Behavior in Powders and Other Disperse Systems》</a> <b style="margin: 0 2px;">|</b><span>2020年第6期</span><b style="margin: 0 2px;">|</b><span>共9页</span> </div> </li> <li> <div class="author"> <span class="lefttit">作者</span> <p id="fAuthorthree" class="threelineshidden zhankaihshouqi"> </p> <span class="z_kbtnclass z_kbtnclassall hoverxs" id="zkzz" style="display: none;">展开▼</span> </div> </li> <li> <div style="display: flex;"> <span class="lefttit">作者单位</span> <div style="position: relative;margin-left: 3px;max-width: 639px;"> <div class="threelineshidden zhankaihshouqi" id="fOrgthree"> </div> <span class="z_kbtnclass z_kbtnclassall hoverxs" id="zhdw" style="display: none;">展开▼</span> </div> </div> </li> <li > <span class="lefttit">收录信息</span> <span style="width: 86%;vertical-align: text-top;display: inline-block;"></span> </li> <li> <span class="lefttit">原文格式</span> <span>PDF</span> </li> <li> <span class="lefttit">正文语种</span> <span>eng</span> </li> <li> <span class="lefttit">中图分类</span> <span><a href="https://www.zhangqiaokeyan.com/clc/6960.html" title="特种结构材料">特种结构材料;</a></span> </li> <li class="antistop"> <span class="lefttit">关键词</span> <p style="width: 86%;vertical-align: text-top;"> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=cholesterol&option=203" rel="nofollow">cholesterol;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=nano‐in‐microparticles&option=203" rel="nofollow">nano‐in‐microparticles;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=PLGA&option=203" rel="nofollow">PLGA;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=pulmonary drug delivery&option=203" rel="nofollow">pulmonary drug delivery;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=sildenafil citrate&option=203" rel="nofollow">sildenafil citrate;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=supercritical‐assisted spray drying&option=203" rel="nofollow">supercritical‐assisted spray drying;</a> </p> <div class="translation"> 机译：胆固醇;纳米甲基微粒;PLGA;肺药递送;西地那非柠檬酸盐;超临界辅助喷雾干燥; </div> </li> </ul> </div> </div> <div class="literature cardcommon"> <div class="similarity "> <h3 class="all_title" id="enpatent66">相似文献</h3> <div class="similaritytab clearfix"> <ul> <li class="active" >外文文献</li> <li >专利</li> </ul> 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