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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

The sol-gel transition observation of AC dual-sensitive gels over the gelation temperature (A), gelation (B), and under the gelation temperature (C).Abbreviation: AC, arctigenin.
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f5-ijn-7-2621: The sol-gel transition observation of AC dual-sensitive gels over the gelation temperature (A), gelation (B), and under the gelation temperature (C).Abbreviation: AC, arctigenin.

Mentions: Arctigenin-loaded dual-sensitive liposome gel was prepared using P407:P188 at various ratios. With the temperature-sensitive P407 and P188 gelling polymers, the concentration of poloxamers (P407:P188, 12:20, or 15:15 w/w%) was previously demonstrated to form gels,13,15 and gelling temperatures were lowered by increasing the amount of P188 at an equal content of P407. Figure 5 shows the solgel transition of arctigenin dual-sensitive gels over gelation temperature (A), at gelation temperature (B), and under gelation temperature (C). In the absence of pH-sensitive liposomes, the mixtures of P407:P188 at weight ratios of 1:2 and 1:1 gelled at 39.6°C ± 3.02°C and 37.6°C ± 1.78°C, respectively. In our study, the pH-sensitive liposomes did not significantly affect the gelation temperatures because when pH-sensitive liposomes were added to the thermosensitive gels, the gelation temperatures decreased slightly.


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)

The sol-gel transition observation of AC dual-sensitive gels over the gelation temperature (A), gelation (B), and under the gelation temperature (C).Abbreviation: AC, arctigenin.
© Copyright Policy
Related In: Results  -  Collection

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

f5-ijn-7-2621: The sol-gel transition observation of AC dual-sensitive gels over the gelation temperature (A), gelation (B), and under the gelation temperature (C).Abbreviation: AC, arctigenin.
Mentions: Arctigenin-loaded dual-sensitive liposome gel was prepared using P407:P188 at various ratios. With the temperature-sensitive P407 and P188 gelling polymers, the concentration of poloxamers (P407:P188, 12:20, or 15:15 w/w%) was previously demonstrated to form gels,13,15 and gelling temperatures were lowered by increasing the amount of P188 at an equal content of P407. Figure 5 shows the solgel transition of arctigenin dual-sensitive gels over gelation temperature (A), at gelation temperature (B), and under gelation temperature (C). In the absence of pH-sensitive liposomes, the mixtures of P407:P188 at weight ratios of 1:2 and 1:1 gelled at 39.6°C ± 3.02°C and 37.6°C ± 1.78°C, respectively. In our study, the pH-sensitive liposomes did not significantly affect the gelation temperatures because when pH-sensitive liposomes were added to the thermosensitive gels, the gelation temperatures decreased slightly.

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