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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

Cytotoxic effect of P-KH liposome and S-KH liposome on colon 26 cells. High concentration of P-KH liposome shows cytotoxicity effect on colon 26 cells. It is important to control a concentration of P-KH liposome in order to be used as a drug carrier.
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fig4: Cytotoxic effect of P-KH liposome and S-KH liposome on colon 26 cells. High concentration of P-KH liposome shows cytotoxicity effect on colon 26 cells. It is important to control a concentration of P-KH liposome in order to be used as a drug carrier.

Mentions: The cytotoxicity of P-KH liposome and S-KH liposome is an important factor to apply them as a drug carrier. The cytotoxicity of the liposomes (DMPC liposome, P-KH liposome, and S-KH liposome) for colon 26 cells was evaluated by MTT assay. Figure 4 shows the viability of colon 26 cells after their coincubation with DMPC liposome, P-KH liposome, or S-KH liposome. DMPC liposome and S-KH liposome hardly showed cytotoxic effect for colon 26 cells, although the cell viability of colon 26 cells was reduced to ~80% by the treatment with S-KH liposome. On the other hand, the viability of colon 26 cells was significantly reduced by P-KH liposome (10% and 30%) and reached less than 40%. It was thus investigated that only P-KH liposome showed cytotoxicity for colon 26 cells.


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)

Cytotoxic effect of P-KH liposome and S-KH liposome on colon 26 cells. High concentration of P-KH liposome shows cytotoxicity effect on colon 26 cells. It is important to control a concentration of P-KH liposome in order to be used as a drug carrier.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig4: Cytotoxic effect of P-KH liposome and S-KH liposome on colon 26 cells. High concentration of P-KH liposome shows cytotoxicity effect on colon 26 cells. It is important to control a concentration of P-KH liposome in order to be used as a drug carrier.
Mentions: The cytotoxicity of P-KH liposome and S-KH liposome is an important factor to apply them as a drug carrier. The cytotoxicity of the liposomes (DMPC liposome, P-KH liposome, and S-KH liposome) for colon 26 cells was evaluated by MTT assay. Figure 4 shows the viability of colon 26 cells after their coincubation with DMPC liposome, P-KH liposome, or S-KH liposome. DMPC liposome and S-KH liposome hardly showed cytotoxic effect for colon 26 cells, although the cell viability of colon 26 cells was reduced to ~80% by the treatment with S-KH liposome. On the other hand, the viability of colon 26 cells was significantly reduced by P-KH liposome (10% and 30%) and reached less than 40%. It was thus investigated that only P-KH liposome showed cytotoxicity for colon 26 cells.

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