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Poly(lactic acid)-hyperbranched polyglycerol nanoparticles enhance bioadhesive treatment of esophageal disease and reduce systemic drug exposure
Nanoscale ( IF 5.8 ) Pub Date : 2022-05-31 , DOI: 10.1039/d2nr01846b Yang Mai 1 , Yaqi Ouyang 1 , Yujia Qin 1 , Changchang Jia 2 , Laura E McCoubrey 3 , Abdul W Basit 3 , Yichu Nie 4 , Yizhen Jia 1 , Liu Yu 1 , Liu Dou 1 , Wenbin Deng 1 , Yang Deng 1 , Yang Liu 1
Nanoscale ( IF 5.8 ) Pub Date : 2022-05-31 , DOI: 10.1039/d2nr01846b Yang Mai 1 , Yaqi Ouyang 1 , Yujia Qin 1 , Changchang Jia 2 , Laura E McCoubrey 3 , Abdul W Basit 3 , Yichu Nie 4 , Yizhen Jia 1 , Liu Yu 1 , Liu Dou 1 , Wenbin Deng 1 , Yang Deng 1 , Yang Liu 1
Affiliation
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The effective treatment of esophageal disease represents a significant unmet clinical need, as existing treatments often lead to unnecessary systemic drug exposure and suboptimal concentrations at the disease site. Here, surface-modified bioadhesive poly(lactic acid)-hyperbranched polyglycerol nanoparticles (BNPs), with an average 100–200 nm diameter, were developed for local and sustained esophageal drug delivery. BNPs showed significantly higher adhesion and permeation into ex vivo human and rat esophageal tissue than non-adhesive nanoparticles (NNPs) and had longer residence times within the rat esophagus in vivo. Incubation with human esophagus (Het-1A) cells confirmed BNPs’ biocompatibility at clinically relevant concentrations. In a rat model of achalasia, nifedipine-loaded BNPs significantly enhanced esophageal drug exposure, increased therapeutic efficacy, and reduced systemic drug exposure compared to NNPs and free drug. The safety of BNPs was demonstrated by an absence of intestinal, hepatic, and splenic toxicity following administration. This study is the first to demonstrate the efficacy of BNPs for esophageal drug delivery and highlight their potential for improving the lives of patients suffering with esophageal conditions.
中文翻译：
聚（乳酸）-超支化聚甘油纳米颗粒增强食管疾病的生物粘附治疗并减少全身药物暴露
食管疾病的有效治疗代表了一个重要的未满足的临床需求，因为现有的治疗通常会导致不必要的全身药物暴露和疾病部位的次优浓度。在这里，开发了平均直径为 100-200 nm 的表面改性生物粘附性聚（乳酸）超支化聚甘油纳米颗粒（BNP），用于局部和持续的食管药物输送。与非粘附性纳米颗粒 (NNP) 相比，BNP 对离体人和大鼠食管组织的粘附性和渗透性显着更高，并且在体内大鼠食管内的停留时间更长. 与人食道 (Het-1A) 细胞一起孵育证实了 BNP 在临床相关浓度下的生物相容性。在大鼠贲门失弛缓症模型中，与 NNP 和游离药物相比，负载硝苯地平的 BNP 显着增强了食管药物暴露，提高了治疗效果，并减少了全身药物暴露。BNPs 的安全性通过给药后没有肠、肝和脾毒性得到证实。这项研究首次证明了 BNP 对食管给药的功效，并强调了它们在改善食管疾病患者生活方面的潜力。
更新日期：2022-05-31
中文翻译：
聚（乳酸）-超支化聚甘油纳米颗粒增强食管疾病的生物粘附治疗并减少全身药物暴露
食管疾病的有效治疗代表了一个重要的未满足的临床需求，因为现有的治疗通常会导致不必要的全身药物暴露和疾病部位的次优浓度。在这里，开发了平均直径为 100-200 nm 的表面改性生物粘附性聚（乳酸）超支化聚甘油纳米颗粒（BNP），用于局部和持续的食管药物输送。与非粘附性纳米颗粒 (NNP) 相比，BNP 对离体人和大鼠食管组织的粘附性和渗透性显着更高，并且在体内大鼠食管内的停留时间更长. 与人食道 (Het-1A) 细胞一起孵育证实了 BNP 在临床相关浓度下的生物相容性。在大鼠贲门失弛缓症模型中，与 NNP 和游离药物相比，负载硝苯地平的 BNP 显着增强了食管药物暴露，提高了治疗效果，并减少了全身药物暴露。BNPs 的安全性通过给药后没有肠、肝和脾毒性得到证实。这项研究首次证明了 BNP 对食管给药的功效，并强调了它们在改善食管疾病患者生活方面的潜力。
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