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作为牙周药物递送载体的来自无花果树和芫荽的粘膜粘附凝胶的设计、配方及评价

Design, formulation and evaluation of a mucoadhesive gel from Quercus brantii L. and coriandrum sativum L. as periodontal drug delivery.

作者信息

Aslani Abolfazl, Ghannadi Alireza, Najafi Hajar

机构信息

Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

Adv Biomed Res. 2013 Mar 6;2:21. doi: 10.4103/2277-9175.108007. eCollection 2013.

Abstract

BACKGROUND

Periodontitis is inflammation of the supporting tissues of the teeth caused by specific microorganisms. Intra-periodontal pocket, mucoadhesive drug delivery systems have been shown to be clinically effective in the treatment of periodontitis. The aim of this study was to formulate a mucoadhesive gel from the seed hull of Quercus brantii and fruits of Coriandrum sativum for the treatment of periodontitis.

MATERIALS AND METHODS

The semisolid concentrated extracts were incorporated in gel base. Mucoadhesive gels were prepared using carbopol 940, sodium carboxymethylcellulose (sodium CMC) and hydroxypropyl methylcellulose K4M (HPMC) as bioadhesive polymers. Physicochemical tests, mucoadhesive strength measurement and in vitro drug release study were carried out on two formulations containing carbopol 940 and sodium CMC polymers (Formulations F4 and F5). We investigated the antibacterial activity of formulation F5 against Porphyromonas gingivalis using the disk diffusion method on supplemented Brucella agar.

RESULTS

Eight gel formulations were prepared. Physical appearance, homogeneity and consistency of F4 and F5 were good. Mucoadhesion and viscosity of F5 (1% carbopol 940 and 3% sodium CMC) was more than F4 (0.5% carbopol 940 and 3% sodium CMC). Drug release from F5 was slower. Both of formulations were syringeable through 21 G needle. In the disk diffusion method, F5 produced significant growth inhibition zones against P. gingivalis.

CONCLUSION

The ideal formulation for the treatment of periodontitis should exhibit high value of mucoadhesion, show controlled release of drug and be easily delivered into the periodontal pocket preferably using a syringe. Based on in vitro release and mucoadhesion studies, F5 was selected as the best formulation.

摘要

背景

牙周炎是由特定微生物引起的牙齿支持组织的炎症。牙周袋内给药的粘膜粘附药物递送系统已被证明在牙周炎治疗中具有临床疗效。本研究的目的是用无梗花栎种子壳和芫荽果实制备一种粘膜粘附凝胶用于治疗牙周炎。

材料与方法

将半固体浓缩提取物加入凝胶基质中。使用卡波姆940、羧甲基纤维素钠(CMC钠)和羟丙基甲基纤维素K4M(HPMC)作为生物粘附聚合物制备粘膜粘附凝胶。对含有卡波姆940和CMC钠聚合物的两种制剂(制剂F4和F5)进行了理化测试、粘膜粘附强度测量和体外药物释放研究。我们在补充了布鲁氏菌琼脂的培养基上,采用纸片扩散法研究了制剂F5对牙龈卟啉单胞菌的抗菌活性。

结果

制备了八种凝胶制剂。F4和F5的外观、均匀性和稠度良好。F5(1%卡波姆940和3%CMC钠)的粘膜粘附性和粘度高于F4(0.5%卡波姆940和3%CMC钠)。F5的药物释放较慢。两种制剂都可以通过21G针头注射。在纸片扩散法中,F5对牙龈卟啉单胞菌产生了明显的生长抑制圈。

结论

治疗牙周炎的理想制剂应具有高粘膜粘附性,显示药物控释,并且最好使用注射器易于递送至牙周袋。基于体外释放和粘膜粘附研究,F5被选为最佳制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/93de/3748668/f72f76278e6f/ABR-2-21-g005.jpg

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