Phaechamud Thawatchai, Setthajindalert Orn
Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Eur J Pharm Sci. 2017 Mar 1;99:258-265. doi: 10.1016/j.ejps.2016.12.023. Epub 2016 Dec 24.
Cholesterol has been widely used in drug delivery systems including implant. Doxycycline hyclate (DH)-loaded cholesterol in situ forming gels using N-methyl pyrrolidone as a solvent were prepared and investigated for their properties including viscosity, rheology, syringeability, gel formation, drug release, degradation and antimicrobial activities. The burst drug release of a DH-loaded in situ forming gel using cholesterol as the gelling agent was minimized when the amount of benzyl benzoate was increased. The viscosity of the system was increased as the amount of benzyl benzoate was increased with Newtonian flow. The systems were easy to inject into the target site because of their minimal force of syringeability. They could transform from solution into matrix-like structures, but formulations with higher concentrations of benzyl benzoate took a longer time. However, the degradability was decreased when the amount of benzyl benzoate was increased. These systems inhibited P. gingivalis, S. mutans and S. aureus effectively. DH-loaded cholesterol in situ forming gel system comprising 10% benzyl benzoate was the most suitable owing to its sustainable release manner for 10days and therefore was the proper formulation for periodontitis treatment.
胆固醇已广泛应用于包括植入物在内的药物递送系统。制备了以N-甲基吡咯烷酮为溶剂的载有盐酸多西环素(DH)的胆固醇原位形成凝胶,并对其性质进行了研究,包括粘度、流变学、可注射性、凝胶形成、药物释放、降解和抗菌活性。当苯甲酸苄酯的用量增加时,以胆固醇为胶凝剂的载DH原位形成凝胶的药物突释现象最小化。随着苯甲酸苄酯用量的增加,体系粘度呈牛顿流体流动规律增加。由于其最小的可注射力,这些体系易于注射到靶部位。它们可以从溶液转变为基质状结构,但苯甲酸苄酯浓度较高的制剂转变所需时间更长。然而,当苯甲酸苄酯用量增加时,降解性降低。这些体系能有效抑制牙龈卟啉单胞菌、变形链球菌和金黄色葡萄球菌。含有10%苯甲酸苄酯的载DH胆固醇原位形成凝胶体系因其可持续释放10天而最为合适,因此是治疗牙周炎的合适制剂。