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一种用于牙周病的新型盐酸利多卡因粘膜粘附膜。

A novel lidocaine hydrochloride mucoadhesive films for periodontal diseases.

机构信息

Department of Pharmacy, Pharmaceutical Technology and Parasitology, Faculty of Pharmacy, University of Valencia, Av. Vicent Andrés Estellés s/n, 46100, Burjassot, Valencia, Spain.

Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, Universitat deValència, Av. Vicent Andrés Estellés s/n, 46100, Burjassot, Valencia, Spain.

出版信息

J Mater Sci Mater Med. 2019 Jan 11;30(1):14. doi: 10.1007/s10856-018-6213-7.

DOI:10.1007/s10856-018-6213-7
PMID:30635738
Abstract

Periodontal diseases are inflammatory disorders caused primarily by dental plaque microorganisms that even may need surgery to remove damaged tissue. Adhesive biocompatible films may be an adequate form in order to improve drug retention or prevent microbial infections by covering the surgical site. In recent years, much attention has been focused on biocompatible inexpensive polymers, for biomedical and pharmaceutical potential applications. The objective of this research is the development of a film for mucosal application containing lidocaine hydrochloride (5%, w/w) as anesthetic drug. Lidocaine films were prepared with three biopolymers: hydroxypropylmethylcellulose (HPMC), chitosan (CH), or xanthan gum (XG). Their thickness and uniformity content were characterized. Rheological behavior of the hydrated films was studied using flow curves, creep and recovery tests and dynamic oscillatory measurements with a rheometer. The mucoadhesive assays were carried out with cheeks of Wistar rat using a universal tensile tester to know their adhesiveness. Finally, lidocaine delivery through the films was investigated in Franz cells. All films (n = 3 for each polymer) showed flexibility, a drug content of 0.015 ± 0.001 g/cm and a thickness of 0.25 ± 0.01 mm. The results of the maximum detachment force in tensile tests and work adhesion indicated that XG is the polymer that showed greater power of mucoadhesion (p < 0.05). These properties show a good correlation with the rheological characteristics. In all cases, the lidocaine amount released at 30 min is around 4 mg/cm. This amount could be considered sufficient to guarantee the anesthetic effect.

摘要

牙周病是一种炎症性疾病,主要由牙菌斑微生物引起,甚至可能需要手术切除受损组织。为了提高药物保留率或防止微生物感染,覆盖手术部位的粘性生物相容性膜可能是一种合适的形式。近年来,人们对生物相容性廉价聚合物越来越关注,因为它们具有生物医学和制药方面的潜在应用。本研究的目的是开发一种含有盐酸利多卡因(5%,w/w)作为麻醉药物的粘膜应用薄膜。使用三种生物聚合物:羟丙基甲基纤维素(HPMC)、壳聚糖(CH)或黄原胶(XG)制备利多卡因薄膜。对其厚度和均匀性含量进行了表征。使用流变仪通过流动曲线、蠕变和恢复测试以及动态振荡测量研究了水合薄膜的流变行为。使用万能拉伸试验机对 Wistar 大鼠的脸颊进行粘膜粘附试验,以了解其粘附性。最后,通过 Franz 细胞研究了通过薄膜的利多卡因释放。所有薄膜(每种聚合物 n = 3)均表现出柔韧性、药物含量为 0.015 ± 0.001 g/cm 和厚度为 0.25 ± 0.01 mm。拉伸试验和工作粘附的最大分离力结果表明,XG 是表现出更强粘膜粘附力的聚合物(p < 0.05)。这些特性与流变特性显示出良好的相关性。在所有情况下,30 分钟时释放的利多卡因量约为 4 mg/cm。这个量可以被认为足以保证麻醉效果。

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