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LeciPlex, invasomes, and liposomes: A skin penetration study.

International journal of pharmaceutics (2015-05-24)
Sanket M Shah, Mukul Ashtikar, Ankitkumar S Jain, Dinesh T Makhija, Yuvraj Nikam, Rajiv P Gude, Frank Steiniger, Aarti A Jagtap, Mangal S Nagarsenker, Alfred Fahr
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Eucalyptol, natural, ≥99%, FCC, FG
Sigma-Aldrich
Didodecyldimethylammonium bromide, 98%
Sigma-Aldrich
Dipentene, mixture of isomers
Sigma-Aldrich
Eucalyptol, 99%
Sigma-Aldrich
Dipentene, technical, for use as solvent (for the paint industry), mixture of various terpenes
Sigma-Aldrich
Didecyldimethylammonium bromide, 98%
Sigma-Aldrich
Hexadecyltrimethylammonium bromide, for molecular biology, ≥99%
Sigma-Aldrich
Hexadecyltrimethylammonium bromide, BioXtra, ≥99%
Sigma-Aldrich
Hexadecyltrimethylammonium bromide, ≥98%
Sigma-Aldrich
Azelaic acid, 98%
Sigma-Aldrich
Sebacic acid, 99%
Sigma-Aldrich
Citral, natural, ≥96%, FCC, FG
Sigma-Aldrich
Azelaic acid, technical grade, 80%
Sigma-Aldrich
Hexadecyltrimethylammonium bromide, BioUltra, for molecular biology, ≥99.0% (AT)
Sigma-Aldrich
Sebacic acid, ≥95.0% (GC)
Sigma-Aldrich
Citral, 95%
Sigma-Aldrich
Citral, mixture of cis and trans, ≥96%, FG
SAFC
Hexadecyltrimethylammonium bromide