α-MANGOSTIN/CLOVE OIL-INCORPORATED LAURIC ACID-BASED SOLVENT REMOVAL-INDUCED IN SITU FORMING MATRICES

J. Mahadlek, T. Phaechamud, P. Toungsuwan
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Abstract

Typically, the bacteria in periodontal pocket of periodontitis disease are capable of producing a number of virulence factors, which are directly toxic to host tissues or immune cells, or indirectly damage host tissues via induction of inflammatory cytokines. The eradication of these microbes from periodontal pocket is one of crucial processes of periodontitis treatment.  The α-mangostin from Garcinia mangostana Linn has the most potent antibacterial activity with less tendency to acquire resistance; therefore, it is interesting for using as active compound for periodontitis treatment. This study focuses on the development of in situ forming matrices (ISM) involving 50% w/w lauric acid, 5% w/w clove oil and different α-mangostin amount in NMP for periodontal drug delivery. Physicochemical properties of ISM were investigated including pH, density, viscosity, surface tension, in vitro matrix formation, and injectability. Antimicrobial activities of formulated ISM against three standard microbes were evaluated using agar cup diffusion methods. The pH and density of all α-mangostin and clove oil-loaded 50% w/w lauric acid matrices was 4.40 ± 0.04 to 4.78 ± 0.20 and 0.960 ± 0.000 to 0.963 ± 0.001 g/cm3, respectively. The increasing α-mangostin amounts significantly increased the viscosity of prepared formulation and injection force. All formulations had low viscosity that it was easy to injection and spreadable in the periodontal pockets. After contact PBS pH 6.8, they transformed as matrix and the hydrophobic manner of clove oil retarded a solvent exchange. These prepared formulations showed the antimicrobial activities against Staphylococcus aureus ATCC 6538, Escherichia coli ATCC 25922, and Candida albicans ATCC 17011. Hence, they are the potential systems for periodontal drug delivery.
α-芒果苷/椰子油包含的月桂酸类溶剂在原位形成材料中的去除诱导作用
通常情况下,牙周炎疾病牙周袋中的细菌能够产生多种毒力因子,直接对宿主组织或免疫细胞产生毒性,或通过诱导炎症细胞因子间接损害宿主组织。根除牙周袋中的这些微生物是牙周炎治疗的关键过程之一。 来自藤黄属植物芒果中的α-芒果苷具有最强的抗菌活性,且不易产生抗药性;因此,将其用作治疗牙周炎的活性化合物很有意义。本研究的重点是开发原位成型基质(ISM),将 50%月桂酸(重量比)、5%丁香油(重量比)和不同剂量的α-芒果苷(重量比)加入 NMP 中,用于牙周病的给药。研究了 ISM 的物理化学特性,包括 pH 值、密度、粘度、表面张力、体外基质形成和可注射性。使用琼脂杯扩散法评估了配制的 ISM 对三种标准微生物的抗菌活性。所有α-芒果苷和丁香油负载 50%重量月桂酸基质的 pH 值和密度分别为 4.40 ± 0.04 至 4.78 ± 0.20,0.960 ± 0.000 至 0.963 ± 0.001 g/cm3。α-曼戈斯汀含量的增加会显著提高制剂的粘度和注射力。所有制剂的粘度都很低,易于在牙周袋中注射和涂抹。与 pH 值为 6.8 的 PBS 接触后,它们转化为基质,而丁香油的疏水性阻碍了溶剂交换。这些制备的制剂对金黄色葡萄球菌(ATCC 6538)、大肠杆菌(ATCC 25922)和白色念珠菌(ATCC 17011)具有抗菌活性。因此,它们是牙周给药的潜在系统。
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