title: LeciPlex, invasomes, and liposomes: A skin penetration study.
abstract: The present study compares three vesicular systems, cationic LeciPlex, invasomes, and conventional liposomes for their ability to deliver drugs deep into the skin. Skin penetration ability of the three vesicular systems was studied for two drugs namely idebenone (antioxidant/anticancer) and azelaic acid (antiacne). All systems showed sizes in nanometer range with small polydispersity indices. Vesicular systems were characterized by CryoTEM studies to understand the differences in morphology of the vesicular systems. Ex vivo human skin penetration studies suggested a pattern in penetration of drugs in different layers of the skin: LeciPlex showed higher penetration for idebenone whereas invasomes showed higher penetration of azelaic acid. Ex vivo study using a fluorescent dye (DiI) was performed to understand the differences in the penetration behavior of the three vesicular systems on excised human skin. In vitro cytotoxicity studies on B16F10 melanoma cell lines revealed, when loaded with idebenone, LeciPlex formulations had the superior activity followed by invasomes and liposomes. In vitro antimicrobial study of azelaic acid loaded systems on Propionibacterium acne revealed high antimicrobial activity for DDAB leciplex followed by almost equal activity for invasomes and CTAB LeciPlex followed by liposomes. Whereas antiacne efficacy study in rats for azelaic acid loaded systems, invasomes exhibited the best antiacne efficacy followed by liposomes and LeciPlex.
authors.affiliation: Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), 400098 Mumbai, India.
authors.forename: Sanket M
authors.initials: SM
authors.lastname: Shah
authors.affiliation: Friedrich-Schiller-Universität Jena, Institut für Pharmazie, Lehrstuhl für Pharmazeutische Technologie, Lessingstraße 8, 07743 Jena, Germany.
authors.forename: Mukul
authors.initials: M
authors.lastname: Ashtikar
authors.affiliation: Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), 400098 Mumbai, India.
authors.forename: Ankitkumar S
authors.initials: AS
authors.lastname: Jain
authors.affiliation: Department of Pharmacology, Bombay College of Pharmacy, Kalina, Santacruz (East), 400098 Mumbai, India.
authors.forename: Dinesh T
authors.initials: DT
authors.lastname: Makhija
authors.affiliation: Advanced Centre for Treatment, Research and Education in Cancer, Kharghar, 410210 Navi Mumbai, India.
authors.forename: Yuvraj
authors.initials: Y
authors.lastname: Nikam
authors.affiliation: Advanced Centre for Treatment, Research and Education in Cancer, Kharghar, 410210 Navi Mumbai, India.
authors.forename: Rajiv P
authors.initials: RP
authors.lastname: Gude
authors.affiliation: Elektronenmikroskopisches Zentrum, Universitätsklinikum Jena, Ziegelmühlenweg 1, D07743 Jena, Germany.
authors.forename: Frank
authors.initials: F
authors.lastname: Steiniger
authors.affiliation: Department of Pharmacology, Bombay College of Pharmacy, Kalina, Santacruz (East), 400098 Mumbai, India.
authors.forename: Aarti A
authors.initials: AA
authors.lastname: Jagtap
authors.affiliation: Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), 400098 Mumbai, India. Electronic address: mangal.nagarsenker@gmail.com.
authors.forename: Mangal S
authors.initials: MS
authors.lastname: Nagarsenker
authors.affiliation: Friedrich-Schiller-Universität Jena, Institut für Pharmazie, Lehrstuhl für Pharmazeutische Technologie, Lessingstraße 8, 07743 Jena, Germany.
authors.forename: Alfred
authors.initials: A
authors.lastname: Fahr
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000737:chemistry*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003879:Dermatologic Agents / Q000008:administration & dosage* / Q000737:chemistry*; D003998:Dicarboxylic Acids / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005260:Female; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry*; D008546:Melanoma, Experimental; D011425:Propionibacterium acnes / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D014451:Ubiquinone / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000737:chemistry
chemical_list: D000890:Anti-Infective Agents; D003879:Dermatologic Agents; D003998:Dicarboxylic Acids; D008081:Liposomes; D014451:Ubiquinone; C010038:azelaic acid; C036619:idebenone
keywords: Cationic surfactants; Invasomes; LeciPlex; Liposomes; Propionibacterium acne; Skin delivery