pH and temperature dual-sensitive liposome gel based on novel cleavable mPEG-Hz-CHEMS polymeric vaginal delivery system.
pH and temperature dual-sensitive liposome gel based on novel cleavable mPEG-Hz-CHEMS polymeric vaginal delivery system.
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DOI：
10.2147/ijn.s31757
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发表时间：
2012
影响因子：
8
通讯作者：
Liu W
中科院分区：
文献类型：
--
作者：
Chen D;Sun K;Mu H;Tang M;Liang R;Wang A;Zhou S;Sun H;Zhao F;Yao J;Liu W
在本研究中，基于新型可裂解腙的 pH 敏感的甲氧基聚乙二醇 2000-腙-胆固醇半琥珀酸酯 (mPEG-Hz-CHEMS) 聚合物的 pH 和温度双敏感脂质体凝胶用于阴道给药。 pH 敏感、可裂解的 mPEG-Hz-CHEMS 被设计为改良的 pH 敏感脂质体，可在局部酸性阴道条件下选择性降解。这种新型 pH 敏感脂质体经过精心设计，可在体温下形成热凝胶，并在酸性环境中降解。形成了牛蒡苷元高包封率的双敏感脂质体凝胶，通过傅里叶变换红外光谱和差示扫描量热法表征，提高了牛蒡苷元的溶解度。体温下具有溶胶-凝胶转变的双敏感脂质体凝胶以pH依赖性方式降解，并且在中性和碱性pH下长时间稳定，但在酸性条件（pH 5.0）下可裂解。封装在双敏感脂质体凝胶中的牛蒡甙元比负载到pH敏感脂质体中的牛蒡甙元更稳定且毒性更小。体外药物释放结果表明，双敏感脂质体凝胶在3天内显示出牛蒡子苷元的恒定释放，但在pH 7.4和pH 9.0的缓冲液中显示出牛蒡子苷元的持续释放。这项研究揭示了使用可裂解 mPEG-Hz-CHEMS 聚合物进行阴道输送的 pH 和温度双敏感脂质体凝胶的一些进展。
In this study, a pH and temperature dual-sensitive liposome gel based on a novel cleavable hydrazone-based pH-sensitive methoxy polyethylene glycol 2000-hydrazone-cholesteryl hemisuccinate (mPEG-Hz-CHEMS) polymer was used for vaginal administration. The pH-sensitive, cleavable mPEG-Hz-CHEMS was designed as a modified pH-sensitive liposome that would selectively degrade under locally acidic vaginal conditions. The novel pH-sensitive liposome was engineered to form a thermogel at body temperature and to degrade in an acidic environment. A dual-sensitive liposome gel with a high encapsulation efficiency of arctigenin was formed and improved the solubility of arctigenin characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The dual-sensitive liposome gel with a sol-gel transition at body temperature was degraded in a pH-dependent manner, and was stable for a long period of time at neutral and basic pH, but cleavable under acidic conditions (pH 5.0). Arctigenin encapsulated in a dual-sensitive liposome gel was more stable and less toxic than arctigenin loaded into pH-sensitive liposomes. In vitro drug release results indicated that dual-sensitive liposome gels showed constant release of arctigenin over 3 days, but showed sustained release of arctigenin in buffers at pH 7.4 and pH 9.0. This research has shed some light on a pH and temperature dual-sensitive liposome gel using a cleavable mPEG-Hz-CHEMS polymer for vaginal delivery.