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Investigation of Fatty Acid Ketohydrazone Modified Liposome's Properties as a Drug Carrier.

Hayashi K, Kiriishi M, Suga K, Okamoto Y, Umakoshi H - J Drug Deliv (2015)

Bottom Line: The interface of the P-KH modified liposome at acidic pH was found to become more hydrophobic and less fluidic as compared with that at neutral pH; that is, P-KH modified liposome became more rigid structure.Therefore, it seems that the P-KH modified liposome could protect encapsulated drugs from the enzymes in the lysosome.This study shows the novel approach about design of pH-responsive liposomes based on the membrane properties.

View Article: PubMed Central - PubMed

Affiliation: Department of Chemical Engineering, National Institute of Technology, Nara College, 22 Yata-cho, Yamatokoriyama, Nara 639-1080, Japan.

ABSTRACT
pH-responsive liposomes were prepared by modifying the liposome with acid-cleaving amphiphiles. Palmitic ketohydrazone (P-KH) or stearic ketohydrazone (S-KH), composed of hydrophilic sugar headgroup and hydrophobic acyl chain, was used as a modifier of the DMPC liposome. Because the ketohydrazone group of P-KH or S-KH was cleaved at low pH conditions (

No MeSH data available.


Related in: MedlinePlus

Entrapment of calcein in the liposomes. P-KH liposome and S-KH liposome could encapsulate equal amount of calcein as compared with DMPC liposome.
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fig2: Entrapment of calcein in the liposomes. P-KH liposome and S-KH liposome could encapsulate equal amount of calcein as compared with DMPC liposome.

Mentions: Entrapment of model drug (calcein) in P-KH liposome and S-KH liposome was evaluated by monitoring its fluorescence intensity. The number of calcein molecules per liposome was calculated as shown in Figure 2. The number of calcein molecules in the DMPC liposome was 1441 mol-calcein/mol-lipid, and those in the 10% P-KH liposome and 10% S-KH liposome were 1112 units and 1181 units, respectively. Although the number of calcein molecules in the P-KH liposome and S-KH liposome was slightly lower than that in DMPC liposome, P-KH liposome and S-KH liposome were found to encapsulate the calcein molecules inside their inner water pool. Moreover, the increase of the molar ratio of P-KH and S-KH hardly affected the numbers of calcein molecules in the liposomes, implying that the DMPC liposomes were successfully modified with P-KH and S-KH within the modifier ratio of 0–50%.


Investigation of Fatty Acid Ketohydrazone Modified Liposome's Properties as a Drug Carrier.

Hayashi K, Kiriishi M, Suga K, Okamoto Y, Umakoshi H - J Drug Deliv (2015)

Entrapment of calcein in the liposomes. P-KH liposome and S-KH liposome could encapsulate equal amount of calcein as compared with DMPC liposome.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4663332&req=5

fig2: Entrapment of calcein in the liposomes. P-KH liposome and S-KH liposome could encapsulate equal amount of calcein as compared with DMPC liposome.
Mentions: Entrapment of model drug (calcein) in P-KH liposome and S-KH liposome was evaluated by monitoring its fluorescence intensity. The number of calcein molecules per liposome was calculated as shown in Figure 2. The number of calcein molecules in the DMPC liposome was 1441 mol-calcein/mol-lipid, and those in the 10% P-KH liposome and 10% S-KH liposome were 1112 units and 1181 units, respectively. Although the number of calcein molecules in the P-KH liposome and S-KH liposome was slightly lower than that in DMPC liposome, P-KH liposome and S-KH liposome were found to encapsulate the calcein molecules inside their inner water pool. Moreover, the increase of the molar ratio of P-KH and S-KH hardly affected the numbers of calcein molecules in the liposomes, implying that the DMPC liposomes were successfully modified with P-KH and S-KH within the modifier ratio of 0–50%.

Bottom Line: The interface of the P-KH modified liposome at acidic pH was found to become more hydrophobic and less fluidic as compared with that at neutral pH; that is, P-KH modified liposome became more rigid structure.Therefore, it seems that the P-KH modified liposome could protect encapsulated drugs from the enzymes in the lysosome.This study shows the novel approach about design of pH-responsive liposomes based on the membrane properties.

View Article: PubMed Central - PubMed

Affiliation: Department of Chemical Engineering, National Institute of Technology, Nara College, 22 Yata-cho, Yamatokoriyama, Nara 639-1080, Japan.

ABSTRACT
pH-responsive liposomes were prepared by modifying the liposome with acid-cleaving amphiphiles. Palmitic ketohydrazone (P-KH) or stearic ketohydrazone (S-KH), composed of hydrophilic sugar headgroup and hydrophobic acyl chain, was used as a modifier of the DMPC liposome. Because the ketohydrazone group of P-KH or S-KH was cleaved at low pH conditions (

No MeSH data available.


Related in: MedlinePlus