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壳聚糖基软水凝胶包裹的阿奇霉素纳米粒：一种新型牙科药物递送方法

Azithromycin-Loaded Nanoparticles Incorporated in Chitosan-Based Soft Hydrogels: A Novel Approach for Dental Drug Delivery.

作者信息

Kwiatek Jakub, Paczkowska-Walendowska Magdalena, Rył Anna, Karpiński Tomasz M, Miklaszewski Andrzej, Swora-Cwynar Ewelina, Leśna Marta, Cielecka-Piontek Judyta

机构信息

Kwiatek Dental Clinic Sp. z o.o., Kordeckiego 22, 60-144 Poznan, Poland.

Department of Pharmacognosy and Biomaterials, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznan, Poland.

出版信息

Pharmaceutics. 2025 Feb 26;17(3):304. doi: 10.3390/pharmaceutics17030304.

DOI:10.3390/pharmaceutics17030304
PMID:40142968
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11945840/
Abstract

Azithromycin (AZC), a BCS class II/IV antibiotic with broad-spectrum antimicrobial activity, has poor water solubility, limiting its formulation potential. This study aimed to develop and optimize AZC-based soft hydrogels for the first time for improved solubility, local controlled drug release, and local dental applications. AZC nanoparticles (based on polyvinylpyrrolidone) were synthesized via electrospinning enhanced solubility 40-fold. These were incorporated into chitosan (CS) hydrogels with varying concentrations and degrees of deacetylation (DDA), optimized using a factorial design. Hydrogels were characterized for drug release, mucoadhesion, antioxidant, anti-inflammatory, and antimicrobial properties, with Principal Component Analysis (PCA) assessing correlations. Soft hydrogels with 3% CS and 80% DDA achieved sustained drug release (62.9-94.7% over 48 h), strong mucoadhesion, and enhanced biological activity. Higher CS and DDA improved antioxidant and anti-inflammatory effects due to increased free amino groups. Antimicrobial tests showed efficacy against and . PCA revealed an inverse correlation between AZC release and mucoadhesion and positive correlations between release and anti-inflammatory activity. AZC-based soft hydrogels significantly improved solubility, controlled release, and biological activity, showing strong potential for dental drug delivery. Further clinical validation and optimization are recommended.

摘要

阿奇霉素（AZC）是一种具有广谱抗菌活性的BCS II/IV类抗生素，水溶性差，限制了其制剂应用潜力。本研究旨在首次开发并优化基于阿奇霉素的软质水凝胶，以提高其溶解度、实现局部控释并用于局部牙科应用。通过静电纺丝合成了阿奇霉素纳米颗粒（基于聚乙烯吡咯烷酮），溶解度提高了40倍。将这些纳米颗粒以不同浓度和脱乙酰度（DDA）掺入壳聚糖（CS）水凝胶中，并采用析因设计进行优化。对水凝胶的药物释放、粘膜粘附性、抗氧化、抗炎和抗菌性能进行了表征，并通过主成分分析（PCA）评估相关性。含3% CS和80% DDA的软质水凝胶实现了药物的持续释放（48小时内释放62.9 - 94.7%）、较强的粘膜粘附性和增强的生物活性。较高的CS和DDA由于游离氨基增加而改善了抗氧化和抗炎作用。抗菌试验表明对……和……有效。PCA显示阿奇霉素释放与粘膜粘附性呈负相关以及释放与抗炎活性呈正相关。基于阿奇霉素的软质水凝胶显著提高了溶解度、控释性能和生物活性，在牙科药物递送方面显示出强大潜力。建议进一步进行临床验证和优化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/e44fa9f6b6f5/pharmaceutics-17-00304-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/c4ee212ae626/pharmaceutics-17-00304-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/5054fd23f341/pharmaceutics-17-00304-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/a2cad21fbcc0/pharmaceutics-17-00304-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/72c6c5c85ab1/pharmaceutics-17-00304-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/48199300f9e0/pharmaceutics-17-00304-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/9a61f6852422/pharmaceutics-17-00304-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/1c0d69ac3439/pharmaceutics-17-00304-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/463bbf4b2b67/pharmaceutics-17-00304-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/e44fa9f6b6f5/pharmaceutics-17-00304-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/c4ee212ae626/pharmaceutics-17-00304-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/5054fd23f341/pharmaceutics-17-00304-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/a2cad21fbcc0/pharmaceutics-17-00304-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/72c6c5c85ab1/pharmaceutics-17-00304-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/48199300f9e0/pharmaceutics-17-00304-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/9a61f6852422/pharmaceutics-17-00304-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/1c0d69ac3439/pharmaceutics-17-00304-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/463bbf4b2b67/pharmaceutics-17-00304-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1475/11945840/e44fa9f6b6f5/pharmaceutics-17-00304-g009.jpg

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