pH and temperature dual-sensitive liposome gel based on novel cleavable mPEG-Hz-CHEMS polymeric vaginal delivery system

被引：56

作者：

Chen, Daquan ^{[1
,2
]}

Sun, Kaoxiang ^{[1
,2
]}

Mu, Hongjie ^{[1
]}

Tang, Mingtan ^{[3
]}

Liang, Rongcai ^{[1
,2
]}

Wang, Aiping ^{[1
,2
]}

Zhou, Shasha ^{[1
]}

Sun, Haijun ^{[1
]}

Zhao, Feng ^{[1
]}

Yao, Jianwen ^{[1
]}

Liu, Wanhui ^{[1
,2
]}

机构：

[1] Yantai Univ, Sch Pharm, Yantai 264005, Peoples R China

[2] State Key Lab Longacting & Targeting Drug Deliver, Yantai, Peoples R China

[3] Shandong Univ, Sch Pharmaceut Sci, Jinan 250100, Peoples R China

来源：

INTERNATIONAL JOURNAL OF NANOMEDICINE | 2012年 / 7卷

关键词：

mPEG-Hz-CHEMS polymer; pH-sensitive liposomes; thermosensitive; liposome gel; vaginal delivery; ARCTIUM-LAPPA; MUCOADHESIVE; ARCTIGENIN; CLOTRIMAZOLE; INHIBITION; VAGINITIS; LIGNANS; CELLS;

D O I：

10.2147/IJN.S31757

中图分类号：

TB3 [工程材料学];

学科分类号：

082905 [生物质能源与材料];

摘要：

Background: 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. Methods: 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. Results: 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. Conclusion: 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.

引用

页码：2621 / 2630

页数：10

共 17 条

[1]

Identification of arctigenin as an antitumor agent having the ability to eliminate the tolerance of cancer cells to nutrient starvation [J].