Tan Jeremy P K, Goh Chew H, Tam Kam C
School of Mechanical and Aerospace Engineering, Nanyang Technological University, 50 Nanyang Avenue, Singapore 639798, Singapore.
Eur J Pharm Sci. 2007 Dec;32(4-5):340-8. doi: 10.1016/j.ejps.2007.08.010. Epub 2007 Sep 7.
pH-responsive nanogels consisting of methacrylic acid-ethyl acrylate (MAA-EA) cross-linked with di-allyl phthalate (DAP) were synthesized via the emulsion polymerization process. Delivery systems based on pH-responsive nanoparticles can control the release of rapidly metabolized drugs and/or have the ability to protect sensitive drugs, thereby making them ideal candidates for drug delivery applications. In this study, a drug selective electrode (DSE) was used to directly measure the concentration of procaine hydrochloride (PrHy) and imipramine hydrochloride (IMI) released from MAA-EA nanogels. With a single drug delivery system, drug release for two different drugs loaded via two distinctly different interaction forces was demonstrated. Drug release was conducted using the DSE under different pHs, MAA-EA molar ratio and DAP content. The release rate increased with pH for PrHy loaded nanogels and MAA-EA molar ratio but decreased with pH for IMI loaded nanogels and DAP content. PrHy was found to be hydrophobically bounded, while IMI was found to be electrostatically bounded onto the MAA-EA nanogels, which was further enhanced by hydrogen bonding.
通过乳液聚合过程合成了由甲基丙烯酸 - 丙烯酸乙酯(MAA - EA)与邻苯二甲酸二烯丙酯(DAP)交联而成的pH响应性纳米凝胶。基于pH响应性纳米颗粒的给药系统可以控制快速代谢药物的释放和/或具有保护敏感药物的能力,因此使其成为药物递送应用的理想候选者。在本研究中,使用药物选择性电极(DSE)直接测量从MAA - EA纳米凝胶中释放的盐酸普鲁卡因(PrHy)和盐酸丙咪嗪(IMI)的浓度。通过单一药物递送系统,展示了通过两种截然不同的相互作用力负载的两种不同药物的药物释放情况。在不同的pH值、MAA - EA摩尔比和DAP含量下使用DSE进行药物释放实验。对于负载PrHy的纳米凝胶,释放速率随pH值和MAA - EA摩尔比增加;而对于负载IMI的纳米凝胶,释放速率随pH值和DAP含量降低。发现PrHy通过疏水作用结合,而IMI通过静电作用结合到MAA - EA纳米凝胶上,氢键作用进一步增强了这种结合作用。