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基于新型可裂解 mPEG-Hz-CHEMS 聚合物的 pH 和温度双重敏感脂质体凝胶阴道递药系统。

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

机构信息

School of Pharmacy, Yantai University, Yantai, People’s Republic of China.

出版信息

Int J Nanomedicine. 2012;7:2621-30. doi: 10.2147/IJN.S31757. Epub 2012 May 28.

DOI:10.2147/IJN.S31757
PMID:22679372
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3368511/
Abstract

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.

摘要

背景

在这项研究中，一种基于新型可裂解腙基 pH 敏感甲氧基聚乙二醇 2000-腙-胆固醇琥珀酸酯（mPEG-Hz-CHEMS）聚合物的 pH 和温度双重敏感脂质体凝胶被用于阴道给药。

方法

设计 pH 敏感、可裂解的 mPEG-Hz-CHEMS 作为一种改良的 pH 敏感脂质体，可在局部酸性阴道条件下选择性降解。新型 pH 敏感脂质体设计为在体温下形成温敏凝胶，并在酸性环境中降解。

结果

形成了一种具有高阿魏酸包封效率的双重敏感脂质体凝胶，并通过傅里叶变换红外光谱和差示扫描量热法改善了阿魏酸的溶解度。具有体温下溶胶-凝胶转变的双重敏感脂质体凝胶以 pH 依赖性方式降解，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。包封在双重敏感脂质体凝胶中的阿魏酸比负载在 pH 敏感脂质体中的阿魏酸更稳定且毒性更小。体外药物释放结果表明，双重敏感脂质体凝胶在 3 天内持续释放阿魏酸，但在 pH 7.4 和 pH 9.0 的缓冲液中持续释放阿魏酸。

结论

本研究为使用可裂解的 mPEG-Hz-CHEMS 聚合物用于阴道递药的 pH 和温度双重敏感脂质体凝胶提供了一些启示。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/f298e89227b8/ijn-7-2621f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/159cc3bed42d/ijn-7-2621f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/62519f76ccdc/ijn-7-2621f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/28e6209f2ddb/ijn-7-2621f3a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/8c8313138704/ijn-7-2621f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/e20b4ce56a8e/ijn-7-2621f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/e4592ddce7f8/ijn-7-2621f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/7bdd8fb7f937/ijn-7-2621f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/f298e89227b8/ijn-7-2621f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/159cc3bed42d/ijn-7-2621f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/62519f76ccdc/ijn-7-2621f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/28e6209f2ddb/ijn-7-2621f3a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/8c8313138704/ijn-7-2621f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/e20b4ce56a8e/ijn-7-2621f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/e4592ddce7f8/ijn-7-2621f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/7bdd8fb7f937/ijn-7-2621f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24f6/3368511/f298e89227b8/ijn-7-2621f8.jpg

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