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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

In vitro release of AC dual-sensitive gels at pH 5.0, 7.4 and 9.0.Abbreviation: AC, arctigenin.
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f7-ijn-7-2621: In vitro release of AC dual-sensitive gels at pH 5.0, 7.4 and 9.0.Abbreviation: AC, arctigenin.

Mentions: In vitro release experiments were performed at 37°C for 2 days in different pH buffers to study pH-dependent drug release behavior. The cumulative release of arctigenin, as shown in Figure 7, indicates that the arctigenin-loaded dual-sensitive liposome gel had prolonged release in pH 7.4 and 9.0 buffers. At pH 5.0, the gels showed constant release, and drug release was completed within 3 days. It has been reported previously that the rate of dissolution of gel is actually the controlling factor in drug release.16 In this respect, the gel pH-sensitive pattern would explain the constant release at pH 5.0.14 The arctigenin-loaded dual-sensitive liposome gel looks interesting for vaginal drug delivery in view of vaginal pH.


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)

In vitro release of AC dual-sensitive gels at pH 5.0, 7.4 and 9.0.Abbreviation: AC, arctigenin.
© Copyright Policy
Related In: Results  -  Collection

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

f7-ijn-7-2621: In vitro release of AC dual-sensitive gels at pH 5.0, 7.4 and 9.0.Abbreviation: AC, arctigenin.
Mentions: In vitro release experiments were performed at 37°C for 2 days in different pH buffers to study pH-dependent drug release behavior. The cumulative release of arctigenin, as shown in Figure 7, indicates that the arctigenin-loaded dual-sensitive liposome gel had prolonged release in pH 7.4 and 9.0 buffers. At pH 5.0, the gels showed constant release, and drug release was completed within 3 days. It has been reported previously that the rate of dissolution of gel is actually the controlling factor in drug release.16 In this respect, the gel pH-sensitive pattern would explain the constant release at pH 5.0.14 The arctigenin-loaded dual-sensitive liposome gel looks interesting for vaginal drug delivery in view of vaginal pH.

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