Phaechamud Thawatchai, Thurein Sai Myo, Chantadee Takron
Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Department Pharmaceutical Engineering, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Asian J Pharm Sci. 2018 Mar;13(2):131-142. doi: 10.1016/j.ajps.2017.09.004. Epub 2017 Sep 28.
Solvent exchange induced forming gel (ISG) is the promising drug delivery system for periodontitis treatment owing to the prospect of maintaining an effective high drug level in the gingival crevicular fluid. In the present study, the influence of clove oil (CO) on the characteristics of doxycycline hyclate (DH)-loaded ISG comprising Eudragit RS (ERS) was investigated including viscosity/rheology, syringeability, gel formation/drug release, matrix formation/solvent diffusion and antimicrobial activities. CO could dissolve ERS and increase the viscosity of ISG and its hydrophobicity could also retard the diffusion of solvent and hinder the drug diffusion; thus, the minimization of burst effect and sustained drug release were achieved effectively. All the prepared ISGs comprising CO could expel through the 27-gauge needle for administration by injection and transform into matrix depot after exposure to the simulated gingival crevicular fluid. The antimicrobial activities against , , were increased when the ratio of CO and -methyl pyrrolidone (NMP) was decreased from 1:1 to 1:10 owing to higher diffusion of DH except that for was increased as CO amount was higher. Therefore, CO could minimize the burst while prolonging the drug release of DH-loaded ERS ISG for use as a local drug delivery system for periodontitis treatment.
溶剂交换诱导形成凝胶(ISG)因其有望在龈沟液中维持有效的高药物水平,成为治疗牙周炎的一种很有前景的药物递送系统。在本研究中,考察了丁香酚(CO)对含盐酸多西环素(DH)的、由Eudragit RS(ERS)组成的ISG特性的影响,包括粘度/流变学、可注射性、凝胶形成/药物释放、基质形成/溶剂扩散以及抗菌活性。CO可溶解ERS并增加ISG的粘度,其疏水性还可延缓溶剂扩散并阻碍药物扩散;因此,有效地实现了突释效应的最小化和药物的持续释放。所有含CO制备的ISG均可通过27号针头挤出用于注射给药,并在暴露于模拟龈沟液后转变为基质贮库。当CO与N-甲基吡咯烷酮(NMP)的比例从1:1降至1:10时,对牙龈卟啉单胞菌、伴放线聚集杆菌、具核梭杆菌的抗菌活性增加,这是由于DH的扩散性更高,不过对牙龈卟啉单胞菌的抗菌活性随着CO含量的增加而增强。因此,CO可使含DH的ERS ISG的突释最小化,同时延长药物释放,用作牙周炎治疗的局部药物递送系统。