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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 structure and 1H-NMR spectra of mPEG-Hz-CHEMS in CDCl3.
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f2-ijn-7-2621: The structure and 1H-NMR spectra of mPEG-Hz-CHEMS in CDCl3.

Mentions: If the arctigenin-loaded dual-sensitive liposome gel was applied to the vaginal membrane, the liposomes or drug released would be taken up into the cells and tissues of the vaginal membrane. Thus, the particle size, zeta potential, and entrapment efficiency of liposomes would be important factors for vaginal delivery of the drug. The structure and 1H-NMR spectrum of the mPEG-Hz-CHEMS is shown in Figure 2. As shown in Table 1, the mean particle size of arctigenin-loaded pH-sensitive liposomes was 126.6 ± 3.8 nm. The mean zeta potential was about −18.1 ± 2.3 mV. The entrapment efficiency was determined to be above 90%.


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 structure and 1H-NMR spectra of mPEG-Hz-CHEMS in CDCl3.
© Copyright Policy
Related In: Results  -  Collection

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

f2-ijn-7-2621: The structure and 1H-NMR spectra of mPEG-Hz-CHEMS in CDCl3.
Mentions: If the arctigenin-loaded dual-sensitive liposome gel was applied to the vaginal membrane, the liposomes or drug released would be taken up into the cells and tissues of the vaginal membrane. Thus, the particle size, zeta potential, and entrapment efficiency of liposomes would be important factors for vaginal delivery of the drug. The structure and 1H-NMR spectrum of the mPEG-Hz-CHEMS is shown in Figure 2. As shown in Table 1, the mean particle size of arctigenin-loaded pH-sensitive liposomes was 126.6 ± 3.8 nm. The mean zeta potential was about −18.1 ± 2.3 mV. The entrapment efficiency was determined to be above 90%.

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