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开发负载糠酸莫米松的可生物降解纳米颗粒用于潜在的鼻腔给药。

Developing Biodegradable Nanoparticles Loaded with Mometasone Furoate for Potential Nasal Drug Delivery.

作者信息

Far Jumana, Abdel-Haq Muhammad, Gruber Maayan, Abu Ammar Aiman

机构信息

Department of Pharmaceutical Engineering, Azrieli College of Engineering Jerusalem, Jerusalem 9103501, Israel.

Department of Otolaryngology-Head and Neck Surgery, Galilee Medical Center, Nahariya 2210001, Israel.

出版信息

ACS Omega. 2020 Mar 25;5(13):7432-7439. doi: 10.1021/acsomega.0c00111. eCollection 2020 Apr 7.

Abstract

Intranasal drug administration is considered a routine in the treatment of many nasal conditions including chronic rhinosinusitis (CRS), which is a common disease involving long-term inflammation of the nasal mucosa. Topical nasal steroid treatment is safe and easy to use and plays a basic role in both nonsurgical and surgical treatments for CRS. Intranasal steroid therapy for various time intervals is commonly used before and after endoscopic CRS nasal surgeries to reduce inflammation and edema and to improve mucosal healing. The medication is currently administered via conventional nasal sprays; therefore, there is an incentive to develop more efficient drug delivery systems for the controlled release of topical steroids into the sinonasal cavities over a prolonged period of time. In this study, poly(lactic--glycolic acid) (PLGA) nanoparticles (NPs) loaded with mometasone furoate (MF) were generated using the nanoprecipitation method and characterized physicochemically and morphologically. MF NPs exhibited adequate physicochemical properties and high drug encapsulation efficiency and loading content. MF exhibited sustained release from NPs over 7 days in vitro with an initial burst release; various mathematical models were applied to determine the kinetics of drug release. Having demonstrated the ability to load MF in PLGA-NPs using the nanoprecipitation method for the first time, these NPs urge the need for additional investigations to demonstrate their therapeutic potential in nasal delivery applications.

摘要

鼻内给药被认为是治疗包括慢性鼻-鼻窦炎(CRS)在内的许多鼻腔疾病的常规方法,CRS是一种涉及鼻黏膜长期炎症的常见疾病。局部鼻用类固醇治疗安全且易于使用,在CRS的非手术和手术治疗中均发挥着基础作用。在鼻内镜CRS鼻腔手术前后,通常会在不同时间段使用鼻内类固醇疗法,以减轻炎症和水肿,并促进黏膜愈合。目前该药物通过传统鼻喷雾剂给药;因此,有动力开发更有效的药物递送系统,以便在较长时间内将局部类固醇药物控释到鼻窦腔中。在本研究中,采用纳米沉淀法制备了负载糠酸莫米松(MF)的聚乳酸-乙醇酸共聚物(PLGA)纳米颗粒(NPs),并对其进行了物理化学和形态学表征。MF NPs表现出良好的物理化学性质、高药物包封率和载药量。MF在体外7天内从NPs中持续释放,初期有突释现象;应用各种数学模型来确定药物释放动力学。首次证明了使用纳米沉淀法将MF负载到PLGA-NPs中的能力,这些NPs促使需要进行更多研究以证明其在鼻腔给药应用中的治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9729/7144157/9f894ba0279a/ao0c00111_0009.jpg

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