Khaing Ei Mon, Puyathorn Napaphol, Yodsin Nuttapon, Phonarwut Nakharin, Thammasut Warakon, Rojviriya Catleya, Pichayakorn Wiwat, Phattarateera Supanut, Phaechamud Thawatchai
Program of Pharmaceutical Engineering, Department of Industrial Pharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Polymers (Basel). 2025 Jun 2;17(11):1551. doi: 10.3390/polym17111551.
Cellulose acetate butyrate (CAB) and cellulose acetate propionate (CAP) are biobased materials that are insoluble in water and present a potential alternative to fossil-based plastics. Solvent removal-induced in situ matrices are gaining attention as an innovative dosage form for localized drug delivery for periodontitis therapy. This study aims to develop levofloxacin hemihydrate (Lh)-loaded in situ matrices formed through solvent removal, incorporating various molecular weights (MWs) and concentrations of CAB and CAP. Increased MWs and higher concentrations of these cellulosic esters significantly improved formulation viscosity and injection force, contributing to enhanced phase inversion and greater matrix toughness. Microscopic analysis of interfacial phase changes revealed progressive thickening of the matrix over time, which was influenced by polymer concentration and limited solvent movement. The transformed matrices with high MW CAP and elevated CAB content demonstrated prolonged drug release, predominantly following first-order kinetics, suggesting drug dissolution and diffusion through the scaffold structure. CAB-based in situ matrices containing 15% and 20% polymer exhibited low viscosities suitable for injection, along with optimal gel formation for maintaining their shape, and adhered effectively to periodontal pockets. These matrices provided extended Lh release for up to 120 h and inhibited the growth of periodontopathic bacteria for over 15 days. Therefore, the developed Lh-loaded in situ matrices show promise as an effective treatment for periodontitis, warranting further research to explore their therapeutic potential.
醋酸丁酸纤维素(CAB)和醋酸丙酸纤维素(CAP)是生物基材料,不溶于水,是化石基塑料的潜在替代品。溶剂去除诱导的原位基质作为一种用于牙周炎治疗的局部给药创新剂型正受到关注。本研究旨在开发通过溶剂去除形成的载有左氧氟沙星半水合物(Lh)的原位基质,其中包含不同分子量(MW)和浓度的CAB和CAP。这些纤维素酯分子量的增加和浓度的提高显著改善了制剂的粘度和注射力,有助于增强相转变和提高基质韧性。对界面相变的微观分析表明,基质随时间逐渐增厚,这受聚合物浓度和有限的溶剂移动影响。具有高分子量CAP和较高CAB含量的转化基质显示出药物的缓释,主要遵循一级动力学,表明药物通过支架结构溶解和扩散。含有15%和20%聚合物的基于CAB的原位基质表现出适合注射的低粘度,以及用于保持其形状的最佳凝胶形成,并能有效粘附于牙周袋。这些基质提供长达120小时的Lh缓释,并在超过15天的时间内抑制牙周病原菌的生长。因此,所开发的载有Lh的原位基质有望成为治疗牙周炎的有效方法,值得进一步研究以探索其治疗潜力。