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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

DSC curves of AC (A), AC liposomes (B), AC dual-sensitive gels (C).Abbreviation: AC, arctigenin.
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f4-ijn-7-2621: DSC curves of AC (A), AC liposomes (B), AC dual-sensitive gels (C).Abbreviation: AC, arctigenin.

Mentions: Formation of dual-sensitive liposome gel was confirmed using different techniques, including Fourier transform infrared spectrophotometry and differential scanning calorimetry. Figure 3 shows the Fourier transform infrared spectra for blank gel (A), arctigenin-loaded pH-sensitive liposomes (B), and arctigenin- loaded pH-sensitive liposome gel (C). It can be clearly observed that the arctigenin-loaded pH-sensitive liposome showed a sharp C=O stretch band at 1740 cm−1. In the case of the arctigenin-loaded pH-sensitive liposome gel, the carbonyl-stretching band of the drug disappeared, which suggested that the arctigenin-loaded pH-sensitive liposome was involved in the gel. The differential scanning calorimetry thermograms shown in Figure 4 indicate the thermal behavior of free arctigenin (A), arctigenin-loaded pH-sensitive liposomes (B), and arctigenin-loaded pH-sensitive liposome gel (C) in a range of 30°C–280°C. The arctigenin-loaded pH-sensitive liposomes and arctigenin-loaded pH-sensitive liposome gel show peaks at about 48°C in the differential scanning calorimetry curve. However, complete disappearance of the endothermic peak corresponding to arctigenin was seen for arctigenin-loaded pH-sensitive liposomes and arctigenin-loaded pH-sensitive liposome gel, indicating molecular encapsulation of the arctigenin inside the liposomes and gel.


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)

DSC curves of AC (A), AC liposomes (B), AC dual-sensitive gels (C).Abbreviation: AC, arctigenin.
© Copyright Policy
Related In: Results  -  Collection

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

f4-ijn-7-2621: DSC curves of AC (A), AC liposomes (B), AC dual-sensitive gels (C).Abbreviation: AC, arctigenin.
Mentions: Formation of dual-sensitive liposome gel was confirmed using different techniques, including Fourier transform infrared spectrophotometry and differential scanning calorimetry. Figure 3 shows the Fourier transform infrared spectra for blank gel (A), arctigenin-loaded pH-sensitive liposomes (B), and arctigenin- loaded pH-sensitive liposome gel (C). It can be clearly observed that the arctigenin-loaded pH-sensitive liposome showed a sharp C=O stretch band at 1740 cm−1. In the case of the arctigenin-loaded pH-sensitive liposome gel, the carbonyl-stretching band of the drug disappeared, which suggested that the arctigenin-loaded pH-sensitive liposome was involved in the gel. The differential scanning calorimetry thermograms shown in Figure 4 indicate the thermal behavior of free arctigenin (A), arctigenin-loaded pH-sensitive liposomes (B), and arctigenin-loaded pH-sensitive liposome gel (C) in a range of 30°C–280°C. The arctigenin-loaded pH-sensitive liposomes and arctigenin-loaded pH-sensitive liposome gel show peaks at about 48°C in the differential scanning calorimetry curve. However, complete disappearance of the endothermic peak corresponding to arctigenin was seen for arctigenin-loaded pH-sensitive liposomes and arctigenin-loaded pH-sensitive liposome gel, indicating molecular encapsulation of the arctigenin inside the liposomes and gel.

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