Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Department of Pharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Int J Pharm. 2022 Apr 5;617:121603. doi: 10.1016/j.ijpharm.2022.121603. Epub 2022 Feb 19.
Given its safety and apparent low aqueous solubility, borneol may serve as a matrix forming component of anti-solvent based in situ forming matrixes (ISMs) for crevicular pocket targeting. Drug-free and vancomycin hydrochloride-loaded borneol ISMs were evaluated for pH, density, viscosity, contact angle, surface tension, matrix formation, drug release behavior, in vitro degradability and antimicrobial activities. Density and pH values of borneol-based ISMs decreased with increasing borneol concentration. Given their markedly low viscosity could facilitate better injectability. The contact angles of the drug-free and vancomycin HCl-loaded borneol ISMs increased after being in contact with the agarose gel or the bulge tissue of porcine due to phase inversion. A dense borneol crystal matrix formed after using the highly concentrated ISM corresponded to fast matrix formation. The borneol-based ISM exhibited a sustainable drug release longer than 14 days with a diffusion-controlled release mechanism. Moreover, the developed ISM exhibited strong antimicrobial activities against various microbes. Thus, the vancomycin HCl-loaded borneol-based ISM is a potentially effective local anti-solvent-based ISM for periodontitis treatment via crevicular pocket injection.
鉴于其安全性和明显的低水溶解度，龙脑可能作为抗溶剂原位形成基质（ISMs）的基质形成成分，用于龈沟靶向。评估了无药物和盐酸万古霉素负载龙脑 ISMs 的 pH 值、密度、粘度、接触角、表面张力、基质形成、药物释放行为、体外降解性和抗菌活性。随着龙脑浓度的增加，基于龙脑的 ISMs 的密度和 pH 值降低。鉴于其明显的低粘度，可以更容易地进行注射。由于相转变，无药物和盐酸万古霉素负载龙脑 ISMs 的接触角在与琼脂糖凝胶或猪的隆起组织接触后增加。使用高浓度 ISM 后形成致密的龙脑晶体基质，对应快速的基质形成。基于龙脑的 ISM 表现出可持续的药物释放超过 14 天，具有扩散控制释放机制。此外，所开发的 ISM 对各种微生物表现出强烈的抗菌活性。因此，载盐酸万古霉素的龙脑基 ISM 是一种潜在有效的局部抗溶剂基于 ISM，可通过龈沟注射用于牙周炎治疗。
