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用于局部牙周治疗的聚乙二醇化壳聚糖干凝胶:设计、表征及药物释放

PEGylated chitosan xerogels for localized periodontal therapy: design, characterization, and drug release.

作者信息

Zafar Farjad, Sheraz Muhammad Ali, Ali Syed Abid, Riaz Maryam, Ahmed Sofia, Kazi Sadia Hafeez, Tariq Safoora, Anwar Zubair

机构信息

Baqai Dental College, Baqai Medical University, Karachi, 75340, Pakistan.

Baqai Institute of Pharmaceutical Sciences, Baqai Medical University, Karachi, 75340, Pakistan.

出版信息

Sci Rep. 2025 Jul 1;15(1):20519. doi: 10.1038/s41598-025-05894-1.

DOI:10.1038/s41598-025-05894-1
PMID:40596023
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12216814/
Abstract

It is essential to adopt effective therapy strategies for periodontal diseases to achieve optimal results while avoiding adverse effects on the system. This study has developed various PEGylated chitosan-based biodegradable xerogels for localized release of doxycycline hyclate (DH) to treat periodontal infectious diseases. The xerogels were formulated using the solvent casting method, and the solvent (0.25 M HCl) was slowly evaporated at ambient conditions. Two different molecular weights were employed for chitosan and polyethylene glycol, and twelve combinations, including the placebos and controls, were prepared for the formulation of xerogels. Different physical and chemical characteristics of the prepared DH xerogels were studied, such as drying time and rate, thickness, moisture content, swelling index, organoleptic characteristics, scanning electron microscopy, FTIR spectrometry, differential scanning calorimetry, drug release and kinetics, and antibacterial activity. The results revealed that the drug transforms from a crystalline to an amorphous state, thus rapidly releasing the drug (> 60% in 30 min. in all xerogels), followed by a sustained release up to 10 h. The release kinetics results revealed that the drug followed the Korsmeyer-Peppas model. It is concluded that the formulated DH-loaded xerogels showed promising results for use in the periodontal pockets to treat various infectious diseases.

摘要

为了在避免对全身产生不良反应的同时获得最佳疗效,采用有效的牙周疾病治疗策略至关重要。本研究开发了多种基于聚乙二醇化壳聚糖的可生物降解干凝胶,用于局部释放盐酸多西环素(DH)以治疗牙周感染性疾病。干凝胶采用溶剂浇铸法制备,溶剂(0.25M盐酸)在环境条件下缓慢蒸发。壳聚糖和聚乙二醇采用两种不同的分子量,制备了包括安慰剂和对照在内的十二种组合用于干凝胶的配方。研究了制备的DH干凝胶的不同物理和化学特性,如干燥时间和速率、厚度、水分含量、溶胀指数、感官特性、扫描电子显微镜、傅里叶变换红外光谱、差示扫描量热法、药物释放和动力学以及抗菌活性。结果表明,药物从结晶态转变为非晶态,从而迅速释放药物(所有干凝胶在30分钟内释放>60%),随后持续释放长达10小时。释放动力学结果表明,药物遵循Korsmeyer-Peppas模型。得出的结论是,所制备的载有DH的干凝胶在用于牙周袋治疗各种感染性疾病方面显示出有前景的结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/c503d0500c6a/41598_2025_5894_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/ce9859a9b236/41598_2025_5894_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/076ec296472f/41598_2025_5894_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/8eb526405800/41598_2025_5894_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/c185f309293b/41598_2025_5894_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/c503d0500c6a/41598_2025_5894_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/ce9859a9b236/41598_2025_5894_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/076ec296472f/41598_2025_5894_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/8eb526405800/41598_2025_5894_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/c185f309293b/41598_2025_5894_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5c0d/12216814/c503d0500c6a/41598_2025_5894_Fig5_HTML.jpg

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本文引用的文献

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Curr Drug Deliv. 2025 Mar 26. doi: 10.2174/0115672018377472250326061736.
2
Reducing the effective dose of doxycycline using chitosan silver nanocomposite as a carriers on gram positive and gram-negative bacteria.利用壳聚糖银纳米复合材料作为载体减少四环素的有效剂量对革兰氏阳性菌和革兰氏阴性菌的影响。
Sci Rep. 2024 Nov 13;14(1):27819. doi: 10.1038/s41598-024-78326-1.
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Effect of N-Acetyl-L-cysteine on Activity of Doxycycline against Biofilm-Forming Bacterial Strains.
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Antibiotics (Basel). 2023 Jul 14;12(7):1187. doi: 10.3390/antibiotics12071187.
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Oral Tetracycline-Class Drugs in Dermatology: Impact of Food Intake on Absorption and Efficacy.皮肤科口服四环素类药物:食物摄入对吸收及疗效的影响
Antibiotics (Basel). 2023 Jul 5;12(7):1152. doi: 10.3390/antibiotics12071152.
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