用于新型局部给药的表面活性剂修饰壳聚糖纳米颗粒的制备和优化:通过增强抗菌特性提高伤口愈合效果

IF 5.3 2区 医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics Pub Date : 2024-09-25 DOI:10.1016/j.ijpharm.2024.124763
Merna A Badie, Mahmoud H Teaima, Mohamed A El-Nabarawi, Noha M Badawi
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引用次数: 0

摘要

烧伤伤口仍然是全球关注的一个重大健康问题,细菌感染经常会加剧伤口愈合并提高发病率。头孢地尼是第三代头孢菌素类抗生素,可用于治疗各种疾病,但它存在水溶性低、生物利用度有限和生物半衰期短等局限性。本研究旨在制备和优化新型表面活性剂基头孢地尼壳聚糖纳米颗粒(CFD-CSNPs),以增强头孢地尼的局部给药能力和在烧伤愈合中的疗效。利用 Design Expert® 软件,采用方框-贝肯设计(BBD)来开发优化的 CFD-CSNPs,其中独立因素包括壳聚糖浓度、壳聚糖:三聚磷酸钠比率、pH 值和表面活性剂类型。粒度 PS、Zeta 电位 ZP、多分散指数 PDI 和夹带效率 EE% 作为因变量进行评估。CFD-CSNPs 采用离子凝胶法生产。确定了优化配方后,对其进行了进一步的体外和体内评估。优化后的 CFD-CSNPs 具有可接受的 PS、PDI 和 ZP 值。CSNPs 中 CFD 的 EE% 达到 57.89 % ± 1.66。TEM 分析显示其形态为球形。体外释放研究表明,48 小时内的双相释放曲线可达(75.5 % ± 3.8)。优化后的 CFD-CSNPs 对测试微生物的抗菌效果有所提高,在预防和消除生物膜方面都表现出色。在体外和体内研究中,经优化的 CFD-CSNPs 增强了伤口愈合活性,这一点已在划痕伤口试验和皮肤烧伤小鼠模型中得到证实。本研究证明了 CFD-CSNPs 在伤口愈合和治疗伤口感染方面的创新性局部应用功效。
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Formulation and optimization of surfactant-modified chitosan nanoparticles loaded with cefdinir for novel topical drug delivery: Elevating wound healing efficacy with enhanced antibacterial properties.

Burn wounds remain a significant global health concern, frequently exacerbated by bacterial infections that hinder healing and raise morbidity rates. Cefdinir, a third-generation cephalosporin antibiotic, is used to treat various conditions, but it has limitations such as low water solubility, limited bioavailability, and a short biological half-life. This study aimed to fabricate and optimize novel surfactant-based Cefdinir-loaded chitosan nanoparticles (CFD-CSNPs) for enhancing topical CFD delivery and efficacy in burn healing. Box-Behnken Design (BBD) was employed to develop optimized CFD-CSNPs using Design Expert® software, where the independent factors were chitosan concentration, chitosan: sodium tripolyphosphate ratio, pH, and surfactant type. Particle size PS, zeta potential ZP, Polydispersity index PDI, and entrapment efficiency EE% were evaluated as dependent factors. CFD-CSNPs were produced using the ionic gelation method. The optimized formula was determined and then examined for further in vitro and in vivo assessments. The optimized CFD-CSNPs exhibited acceptable PS, PDI, and ZP values. The EE% of CFD from CSNPs reached 57.89 % ± 1.66. TEM analysis revealed spherical morphology. In vitro release studies demonstrated a biphasic release profile up to (75.5 % ± 3.8) over 48 hrs. The optimized CFD-CSNPs showed improved antimicrobial efficacy against the tested microorganisms, exhibiting superior performance for both biofilm prevention and eradication. Enhanced wound healing activity was achieved by the optimized CFD-CSNPs in both in vitro and in vivo studies as confirmed by scratch wound assay and skin burn mice model. The current study advocates the efficacy of the innovative topical application of CFD-CSNPs for wound healing purposes and treatment of wound infections.

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来源期刊
CiteScore
10.70
自引率
8.60%
发文量
951
审稿时长
72 days
期刊介绍: The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.
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