Puyathorn Napaphol, Lertsuphotvanit Nutdanai, Chantadee Takron, Pichayakorn Wiwat, Phaechamud Thawatchai
Programme of Pharmaceutical Engineering, Department of Industrial Pharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Program of Pharmaceutical Technology, Department of Industrial Pharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Gels. 2023 Jun 19;9(6):495. doi: 10.3390/gels9060495.
Solvent exchange-induced in situ forming gel (ISG) has emerged as a versatile drug delivery system, particularly for periodontal pocket applications. In this study, we developed lincomycin HCl-loaded ISGs using a 40% borneol-based matrix and N-methyl pyrrolidone (NMP) as a solvent. The physicochemical properties and antimicrobial activities of the ISGs were evaluated. The prepared ISGs exhibited low viscosity and reduced surface tension, allowing for easy injection and spreadability. Gel formation increased the contact angle on agarose gel, while higher lincomycin HCl content decreased water tolerance and facilitated phase separation. The drug-loading influenced solvent exchange and matrix formation, resulting in thinner and inhomogeneous borneol matrices with slower gel formation and lower gel hardness. The lincomycin HCl-loaded borneol-based ISGs demonstrated sustained drug release above the minimum inhibitory concentration (MIC) for 8 days, following Fickian diffusion and fitting well with Higuchi's equation. These formulations exhibited dose-dependent inhibition of ATCC 25923, ATCC 8739, and ATCC 33277, and the release of NMP effectively inhibited ATCC 10231. Overall, the 7.5% lincomycin HCl-loaded 40% borneol-based ISGs hold promise as localized drug delivery systems for periodontitis treatment.
溶剂交换诱导原位形成凝胶（ISG）已成为一种多功能药物递送系统，尤其适用于牙周袋应用。在本研究中，我们使用40%的冰片基基质和N-甲基吡咯烷酮（NMP）作为溶剂开发了载有盐酸林可霉素的ISG。对ISG的物理化学性质和抗菌活性进行了评估。制备的ISG表现出低粘度和降低的表面张力，便于注射和铺展。凝胶形成增加了在琼脂糖凝胶上的接触角，而较高的盐酸林可霉素含量降低了耐水性并促进了相分离。药物负载影响溶剂交换和基质形成，导致冰片基质更薄且不均匀，凝胶形成较慢且凝胶硬度较低。载有盐酸林可霉素的冰片基ISG在最低抑菌浓度（MIC）以上持续释放药物8天，遵循菲克扩散并与 Higuchi 方程拟合良好。这些制剂对 ATCC 25923、ATCC 8739 和 ATCC 33277 表现出剂量依赖性抑制，并且 NMP 的释放有效抑制了 ATCC 10231。总体而言，载有7.5%盐酸林可霉素的40%冰片基ISG有望作为治疗牙周炎的局部药物递送系统。
