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Benzoyl Peroxide In Situ Forming Antimicrobial Gel for Periodontitis Treatment

机译:过氧化苯甲酰原位形成抗菌凝胶治疗牙周炎

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Periodontitis is an inflammatory disease of the supporting structures of the tooth caused by bacterial infection which can result in tooth loss. The local intra-pocket drug delivery system was interesting and highly effective for periodontitis treatment. In situ forming gel system is the polymeric solution which could transform into gel for localizing and sustaining the drug release at desired site. This system has been recommended as one of suitable delivery system for this purpose. Benzoyl peroxide (BPO) in situ forming gels were developed using Eudragit RS as polymer dispersed in N-methyl-pyrrolidone (NMP). Peppermint oil and polyethylene glycol 1500 were also incorporated as the excipients. The prepared systems were evaluated for rheology, syringeability (using texture analyzers), in situ gel formation (after injection into PBS pH 6.8), antimicrobial activity (against Streptococcus mutans with agar diffusion) and drug release (with dialysis method in PBS pH 6.8 at 50 rpm, 37 ℃). The viscosity and syringeability of the prepared systems was increased as the amount of BPO, peppermint oil or PEG 1500 was increased. All prepared gels showed the Newtonian flow which the viscosity was decreased as the temperature was increased. All prepared gels comprising peppermint oil and PEG 1500 could form in situ gel in used medium which the pH was close to the environment pH of periodontal pocket. The inhibition zone against Streptococcus mutans of the prepared system was significantly decreased when the peppermint oil and PEG 1500 was incorporated owing to the higher viscous environment and thereafter retardation of drug diffusion was evident. This effect could prolong the drug release. From drug release test, all prepared gels could sustain the BPO release for at least 96 hrs. Release kinetic obtained from curve fitting with various release equations using least square fit technique indicated that the release patterns were as Higuchi's model therefore the release of BPO was performed with diffusion control. This developed BPO in situ forming gel presented its ability as the controlled drug delivery system for localized antimicrobial activity at periodontal pocket.
机译:牙周炎是细菌感染引起的牙齿支撑结构的炎性疾病,可导致牙齿脱落。局部口袋内药物递送系统对于牙周炎的治疗很有趣并且非常有效。原位形成凝胶系统是聚合物溶液,其可以转变成凝胶以定位和维持药物在所需部位的释放。为此,该系统被推荐为合适的传送系统之一。使用Eudragit RS作为分散在N-甲基-吡咯烷酮(NMP)中的聚合物开发了过氧化苯甲酰(BPO)原位形成凝胶。还掺入了薄荷油和聚乙二醇1500作为赋形剂。对制得的系统进行流变学,可注射性(使用质构分析仪),原位凝胶形成(注入PBS pH 6.8后),抗菌活性(抗变形链球菌和琼脂扩散)和药物释放(在PBS pH 6.8下采用透析方法)进行评估。 50 rpm,37℃)。随着BPO,薄荷油或PEG 1500含量的增加,所制备体系的粘度和可注射性也随之提高。所有制备的凝胶均显示牛顿流,其粘度随温度升高而降低。所有制备的包含薄荷油和PEG 1500的凝胶都可以在pH值接近牙周袋环境pH值的使用过的培养基中原位形成凝胶。当掺入薄荷油和PEG 1500时,由于较高的粘性环境,制得的系统对变形链球菌的抑制区明显减少,此后药物扩散的抑制作用明显。这种作用可以延长药物释放。从药物释放测试来看,所有制备的凝胶均可以维持BPO释放至少96小时。使用最小二乘拟合技术通过各种释放方程的曲线拟合获得的释放动力学表明,释放模式为Higuchi模型,因此BPO的释放通过扩散控制进行。这种开发的BPO原位形成凝胶展示了其作为牙周袋局部抗菌活性的受控药物递送系统的能力。

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