title: Lipase-Sensitive Transfersomes Based on Photosensitizer/Polymerizable Lipid Conjugate for Selective Antimicrobial Photodynamic Therapy of Acne.
abstract: Acne vulgaris is a common skin problem affecting nearly 90% of adolescents and its development is associated with a colonization of Propionibacterium acnes (P. acnes). Although antibiotics have commonly been used to treat acne, antibiotic resistance of P. acnes is an emerging issue to be solved. In this study, a new way of photodynamic acne therapy is developed using P. acnes lipase-sensitive transfersome (DSPE-PEG-Pheo A (DPP) transfersome). For enhanced selectivity and skin penetration efficiency, DPP transfersomes are prepared from 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)-2000], pheophorbide A (Pheo A), cholesterol, and Tween-80. Incorporation of Tween-80 as an edge activator increases the deformability of DPP transfersomes, enhancing skin penetration efficiency to four times that of free Pheo A. The photoactivity of Pheo A quenched by DPP transfersomes is gradually recovered by selective cleavage of the ester linkage in DPP transfersomes by P. acnes lipases. In vitro P. acnes-specific photoactivity and subsequent selective antimicrobial effect exhibit a greater than 99% loss of P. acnes viability. In vivo antiacne therapeutic effect is confirmed by reduction of swelling volume and thickness of P. acnes-induced nude mice skin. These results demonstrate that DPP transfersome-mediated photodynamic therapy can be used as an alternative method to treat bacterial skin infections.
authors.affiliation: Center for Photomedicine, Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do, 420-743, South Korea.
authors.forename: Hyung
authors.initials: H
authors.lastname: Park
authors.affiliation: Center for Photomedicine, Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do, 420-743, South Korea.
authors.forename: Jonghwan
authors.initials: J
authors.lastname: Lee
authors.affiliation: Center for Photomedicine, Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do, 420-743, South Korea.
authors.forename: Songhee
authors.initials: S
authors.lastname: Jeong
authors.affiliation: Center for Photomedicine, Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do, 420-743, South Korea.
authors.forename: Byeong Nam
authors.initials: BN
authors.lastname: Im
authors.affiliation: Department of New Drug Development, School of Medicine, Inha University, 2F A-dong, Jeongseok Bldg., Sinheung-dong 3-ga, Jung-gu, Incheon, 400-712, Republic of Korea.
authors.forename: Min-Kyoung
authors.initials: MK
authors.lastname: Kim
authors.affiliation: Department of New Drug Development, School of Medicine, Inha University, 2F A-dong, Jeongseok Bldg., Sinheung-dong 3-ga, Jung-gu, Incheon, 400-712, Republic of Korea.
authors.forename: Su-Geun
authors.initials: SG
authors.lastname: Yang
authors.affiliation: Center for Photomedicine, Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do, 420-743, South Korea.
authors.forename: Kun
authors.initials: K
authors.lastname: Na
mesh_terms: D000152:Acne Vulgaris / Q000188:drug therapy* / Q000378:metabolism; D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology*; D008049:Lipase / Q000378:metabolism*; D008055:Lipids / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D010778:Photochemotherapy / Q000379:methods; D017319:Photosensitizing Agents / Q000494:pharmacology*; D011108:Polymers / Q000494:pharmacology*; D011425:Propionibacterium acnes / Q000187:drug effects; D012867:Skin / Q000187:drug effects / Q000382:microbiology
chemical_list: D000890:Anti-Infective Agents; D008055:Lipids; D017319:Photosensitizing Agents; D011108:Polymers; D008049:Lipase
keywords: acne; enzyme sensitive; photodynamic therapy; propionibacterium acnes; transfersome