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一种用于牙周袋内局部和持续释放抗菌剂的可注射系统。

An Injectable System for Local and Sustained Release of Antimicrobial Agents in the Periodontal Pocket.

作者信息

Morelli Laura, Cappelluti Martino Alfredo, Ricotti Leonardo, Lenardi Cristina, Gerges Irini

机构信息

Filarete Foundation, Viale Ortles 22/4, 20139, Milano, Italy.

SEMM-European School of Molecular Medicine, Campus IFOM-IEO, via Adamello 16, 20139, Milano, Italy.

出版信息

Macromol Biosci. 2017 Aug;17(8). doi: 10.1002/mabi.201700103. Epub 2017 May 2.

Abstract

Periodontitis treatments usually require local administration of antimicrobial drugs with the aim to reduce the bacterial load inside the periodontal pocket. Effective pharmaceutical treatments may require sustained local drug release for several days in the site of interest. Currently available solutions are still not able to fulfill the clinical need for high-quality treatments, mainly in terms of release profiles and patients' comfort. This work aims to fill this gap through the development of an in situ gelling system, capable to achieve controlled and sustained release of antimicrobial agents for medium-to-long-term treatments. The system is composed of micrometer-sized β-cyclodextrin-based hydrogel (bCD-Jef-MPs), featured by a strong hydrophilic character, suspended in a synthetic block-co-polymer solution (Poloxamer 407), which is capable to undergo rapid thermally induced sol-gel phase transition at body temperature. The chemical structure of bCD-Jef-MPs was confirmed by cross-correlating data from Fourier transform infrared (FTIR) spectroscopy, swelling test, and degradation kinetics. The thermally induced sol-gel phase transition is demonstrated by rheometric tests. The effectiveness of the described system to achieve sustained release of antimicrobial agents is demonstrated in vitro, using chlorhexidine digluconate as a drug model. The results achieved in this work disclose the potential of the mentioned system in effectively treating periodontitis lesions.

摘要

牙周炎治疗通常需要局部应用抗菌药物,目的是减少牙周袋内的细菌载量。有效的药物治疗可能需要在感兴趣的部位持续局部释放药物数天。目前可用的解决方案仍无法满足高质量治疗的临床需求,主要体现在释放曲线和患者舒适度方面。这项工作旨在通过开发一种原位凝胶系统来填补这一空白,该系统能够实现抗菌剂的可控和持续释放,用于中长期治疗。该系统由微米级的基于β-环糊精的水凝胶(bCD-Jef-MPs)组成,其具有很强的亲水性,悬浮在合成嵌段共聚物溶液(泊洛沙姆407)中,该溶液能够在体温下经历快速的热诱导溶胶-凝胶相变。通过傅里叶变换红外光谱(FTIR)、溶胀试验和降解动力学的数据相互关联,证实了bCD-Jef-MPs的化学结构。流变学测试证明了热诱导溶胶-凝胶相变。以葡萄糖酸氯己定为药物模型,在体外证明了所述系统实现抗菌剂持续释放的有效性。这项工作取得的结果揭示了上述系统在有效治疗牙周炎病变方面的潜力。

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