title: Enhanced depigmenting effects of N-glycosylation inhibitors delivered by pH-sensitive liposomes into HM3KO melanoma cells.
abstract: Delivery activity of pH-sensitive 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE):cholesteryl hemisuccinate (CHEMS) liposomes was assessed as an in vitro intracellular carrier system to increase the bioavailability of depigmentation actives. N-glycosylation inhibitors have a glycosylation-inhibiting effect, which is useful for the skin depigmentation that operates by interfering with the maturation of tyrosinase. However, an N-glycosylation inhibitor does not easily pass through skin or even cellular membranes due to its water-soluble property. Therefore, it should be transported to target cells by an efficient delivery carrier to reduce the glycosylated tyrosinase. Glycosylation-inhibiting and depigmentation effects of N-butyldeoxynojirimycine (NB-DNJ) and 1-deoxynojirimycine (DNJ)-loaded liposomes were evaluated using Western blotting and measurement of synthesized melanin. Interestingly, it was found that the pH-sensitive liposomes increased the glycosylation-inhibiting and thus, pigment-lightening effects of N-glycosylation inhibitors in vitro. In addition, cargo materials loaded in pH-sensitive liposomes were found to be much more efficiently delivered into the cytoplasm, as observed in fluorescent-activated cell sorting (FACS) and confocal laser-scanning microscopic (CLSM) analysis. These results indicate that pH-sensitive DOPE:CHEMS liposomes have a strong potential as a carrier system to promote delivery efficiency and to enhance the biological effects of water-soluble actives for applications in cosmetics, personal care products, and pharmaceutics.
authors.affiliation: Skin Research Institute, Amore Pacific Corp. R&D Center, Gyeonggi-do, 446-729, Korea.
authors.forename: Ju Young
authors.initials: JY
authors.lastname: Park
authors.forename: Hyunjung
authors.initials: H
authors.lastname: Choi
authors.forename: Jae Sung
authors.initials: JS
authors.lastname: Hwang
authors.forename: Junoh
authors.initials: J
authors.lastname: Kim
authors.forename: Ih-Seop
authors.initials: IS
authors.lastname: Chang
mesh_terms: D017485:1-Deoxynojirimycin / Q000008:administration & dosage; D015153:Blotting, Western; D045744:Cell Line, Tumor; D002788:Cholesterol Esters / Q000008:administration & dosage*; D016503:Drug Delivery Systems; D005944:Glucosamine / Q000008:administration & dosage / Q000031:analogs & derivatives*; D006031:Glycosylation / Q000187:drug effects; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000008:administration & dosage*; D008543:Melanins / Q000032:analysis / Q000378:metabolism*; D008545:Melanoma / Q000378:metabolism; D018613:Microscopy, Confocal; D010714:Phosphatidylethanolamines / Q000008:administration & dosage*; D010858:Pigmentation / Q000187:drug effects*
chemical_list: D002788:Cholesterol Esters; D008081:Liposomes; D008543:Melanins; D010714:Phosphatidylethanolamines; C501633:deoxynojirimycine; D017485:1-Deoxynojirimycin; C020888:1,2-dielaidoylphosphatidylethanolamine; D005944:Glucosamine; C013440:cholesteryl succinate