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用于牙周治疗药物递送的泡沫驱动纳米乳凝胶的设计:配方、表征及抗菌效果

Design of a Foam-Actuated Nano-Emulgel for Perioceutic Drug Delivery: Formulation, Characterization, and Antimicrobial Efficacy.

作者信息

Varughese Theresa P K, Ramburrun Poornima, Okafor Nnamdi I, Vuuren Sandy van, Choonara Yahya E

机构信息

Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown, Johannesburg 2193, South Africa.

Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown, Johannesburg 2193, South Africa.

出版信息

Gels. 2025 May 20;11(5):373. doi: 10.3390/gels11050373.

Abstract

Periodontitis is a prevalent oral condition worldwide. Azithromycin, a conventional lipophilic drug for periodontal treatment, often causes systemic side effects when administered orally. To address this, azithromycin-loaded nano-emulgels were developed using olive oil as a carrier within a xanthan gum aqueous gel phase. This oil-in-aqueous gel emulsion was actuated into a foam for localized drug delivery in gingival and periodontal disease. The solubility of azithromycin in various vehicles was tested, with olive oil showing the best solubility (0.347 mg/mL). Thermodynamic stability testing identified viable nano-formulations, with encapsulation efficiencies ranging from 98 to 100%. These formulations exhibited rapid drug release within 2-8 h. Muco-adhesion studies and ex vivo permeability tests on porcine buccal mucosa highlighted the beneficial properties of xanthan gum for local drug retention within the oral cavity. Antimicrobial efficiency was assessed using minimum inhibitory concentrations against various oral pathogens, where the formulation with equal surfactant and co-surfactant ratios showed the most potent antibacterial activity, ranging from 0.390 to 1.56 µg/mL. This was supported by the shear-thinning, muco-adhesive, and drug-retentive properties of the xanthan gel base. The study also examined the influence of the oil phase with xanthan gum gel on foam texture, rheology, and stability, demonstrating a promising prototype for periodontitis treatment.

摘要

牙周炎是一种在全球范围内普遍存在的口腔疾病。阿奇霉素是一种用于牙周治疗的传统亲脂性药物,口服时经常会引起全身副作用。为了解决这个问题,研究人员以橄榄油为载体,在黄原胶水凝胶相中制备了载阿奇霉素纳米乳剂。这种水凝胶包油乳液被制成泡沫,用于牙龈和牙周疾病的局部药物递送。测试了阿奇霉素在各种载体中的溶解度,结果显示橄榄油的溶解度最佳(0.347毫克/毫升)。热力学稳定性测试确定了可行的纳米制剂,其包封率在98%至100%之间。这些制剂在2至8小时内表现出快速的药物释放。对猪颊黏膜的黏膜粘附研究和体外渗透性测试突出了黄原胶在口腔内局部药物保留方面的有益特性。使用针对各种口腔病原体的最低抑菌浓度评估抗菌效率,其中表面活性剂和助表面活性剂比例相等的制剂显示出最有效的抗菌活性,范围为0.390至1.56微克/毫升。黄原胶基质的剪切变稀、粘膜粘附和药物保留特性也证实了这一点。该研究还考察了油相和黄原胶凝胶对泡沫质地、流变学和稳定性的影响,证明了一种有前景的牙周炎治疗原型。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4e6/12111423/abc1a2d94ff4/gels-11-00373-g001.jpg

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