Leber Attila, Budai-Szucs Maria, Urban Edit, Valyi Peter, Kovacs Anita, Berko Szilvia, Csanyi Erzsebet
Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Szeged, Hungary.
Institute of Clinical Microbiology, Faculty of Medicine, University of Szeged, Szeged, Hungary.
Curr Drug Deliv. 2018;15(6):887-897. doi: 10.2174/1567201815666180116092354.
Periodontitis is a chronic inflammatory disease, which affects the supporting tissues of the teeth, and without proper treatment it may lead to tooth loss. Antibiotics - administered orally - have been widely used in the treatment of periodontitis. With the conventional administration routes, adequate drug levels cannot be reached in the periodontal pockets and oral application of antimicrobials could lead to side effects. Drug delivery systems containing antibiotics, administered at the site of infection, could possibly help eliminate pathogen bacteria and treat periodontitis.
The aim of the recent study was to create a locally swellable, biodegradable, biocompatible, mucoadhesive, lipophilic drug delivery system containing antimicrobial drugs which softens at body temperature, accommodate to the shape of the periodontal pocket and can provide extended drug release for at least one week.
During the formulation, thermoanalytical, consistency, wettability, swelling, degradation and drug release studies were applied to determine the ideal ratios of lipid bases, structure-building components and surface active agent concentrations.
The structure-building component cetostearyl alcohol appeared to be the most convenient, thanks to its wettability and mechanical properties, which led to controlled drug release. With the use of ideal concentrations of components (10% surfactant, 40% structure-building component, 32 % lipid base, 15% antimicrobial agent and 3% polymer), sustained drug release can be provided up to nearly 3 weeks.
牙周炎是一种慢性炎症性疾病，会影响牙齿的支持组织，若不进行适当治疗可能导致牙齿脱落。口服抗生素已被广泛用于治疗牙周炎。采用传统给药途径时，牙周袋内无法达到足够的药物浓度，且口服抗菌药物可能会产生副作用。在感染部位给药的含抗生素药物递送系统可能有助于消除病原菌并治疗牙周炎。
近期研究的目的是创建一种局部可膨胀、可生物降解、生物相容、具有粘膜粘附性、亲脂性的药物递送系统，该系统含有抗菌药物，在体温下会软化，能贴合牙周袋的形状，并可提供至少一周的延长药物释放。
在制剂过程中，应用热分析、稠度、润湿性、膨胀、降解和药物释放研究来确定脂质基质、结构构建成分和表面活性剂浓度的理想比例。
结构构建成分鲸蜡硬脂醇似乎是最方便的，这得益于其润湿性和机械性能，从而实现了药物的控释。使用理想浓度的成分（10%表面活性剂、40%结构构建成分、32%脂质基质、15%抗菌剂和3%聚合物），可持续药物释放近3周。
