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

Chen D, Sun K, Mu H, Tang M, Liang R, Wang A, Zhou S, Sun H, Zhao F, Yao J, Liu W - Int J Nanomedicine (2012)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

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

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.

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Related in: MedlinePlus

A schematic diagram of the strategy of mPEG-Hz-CHEMS cleavable dual-sensitive liposome gels.Abbreviation: mPEG-Hz-CHEMS, methoxy polyethylene glycol 2000-hydrazonecholesteryl hemisuccinate.
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f1-ijn-7-2621: A schematic diagram of the strategy of mPEG-Hz-CHEMS cleavable dual-sensitive liposome gels.Abbreviation: mPEG-Hz-CHEMS, methoxy polyethylene glycol 2000-hydrazonecholesteryl hemisuccinate.

Mentions: In this study, a pH and temperature dual-sensitive mucoadhesive vaginal gel formulation was developed for gynecological purposes. A schematic diagram of the mPEGHz-CHEMS cleavable dual-sensitive liposome gel strategy is shown in Figure 1. 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. To this end, we prepared pH and temperature dual-sensitive cleavable arctigenin-encapsulating liposome gels, composed of phosphatidylcholine, mPEG-Hz-CHEMS, and cholesterol. The physicochemical properties of the pH-sensitive liposomes and the dual-sensitive liposome gel were characterized, and the in vitro release and cytotoxicity of these arctigenin-encapsulated dual-sensitive liposome gels was investigated.


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

Chen D, Sun K, Mu H, Tang M, Liang R, Wang A, Zhou S, Sun H, Zhao F, Yao J, Liu W - Int J Nanomedicine (2012)

A schematic diagram of the strategy of mPEG-Hz-CHEMS cleavable dual-sensitive liposome gels.Abbreviation: mPEG-Hz-CHEMS, methoxy polyethylene glycol 2000-hydrazonecholesteryl hemisuccinate.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3368511&req=5

f1-ijn-7-2621: A schematic diagram of the strategy of mPEG-Hz-CHEMS cleavable dual-sensitive liposome gels.Abbreviation: mPEG-Hz-CHEMS, methoxy polyethylene glycol 2000-hydrazonecholesteryl hemisuccinate.
Mentions: In this study, a pH and temperature dual-sensitive mucoadhesive vaginal gel formulation was developed for gynecological purposes. A schematic diagram of the mPEGHz-CHEMS cleavable dual-sensitive liposome gel strategy is shown in Figure 1. 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. To this end, we prepared pH and temperature dual-sensitive cleavable arctigenin-encapsulating liposome gels, composed of phosphatidylcholine, mPEG-Hz-CHEMS, and cholesterol. The physicochemical properties of the pH-sensitive liposomes and the dual-sensitive liposome gel were characterized, and the in vitro release and cytotoxicity of these arctigenin-encapsulated dual-sensitive liposome gels was investigated.

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

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

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.

Show MeSH
Related in: MedlinePlus