title: New effective azelaic acid liposomal gel formulation of enhanced pharmaceutical bioavailability.
abstract: Azelaic acid is a naturally occurring saturated C9-dicarboxylic acid which has been shown to be effective in the treatment of comedonal acne and inflammatory acne, as well as hiperpigmentary skin disorders. The aim of the present study is to compare new developed liposomal hydrogel (lipogel) and commercially available product in terms of the active substance-azelaic acid bioavailability. Topical formulations were evaluated for physical parameters, such as pH measurement, organoleptic evaluation and liposome size analysis in lipogel formulation. In addition, studies were performed on in vitro antimicrobial preservation, stability and accumulation in the stratum corneum according to guidelines established by European Pharmacopoeia and International Conferences on Harmonisation. The new formula for liposomal gel with azelaic acid has the stability required for pharmaceutical preparations. Moreover, presented formulation F2 reveals a very high accumulation (187.5μg/cm2) of an active substance in the stratum corneum, which results in opportunity to decrease of the API content to 10% in comparison to a reference formula: commercially available cream with 20% of azelaic acid. The study reveals that the final formula of lipogel F2 with azelaic acid had acceptable physical parameters that showed that they were compatible with the skin and in addition this formulation passed stability studies. In vitro antimicrobial preservation studies showed that the formulated lipogel F2 showed strong antibacterial activity; thus, no preservatives were added to the final composition of the preparation. The present study concludes that the formulated lipogel F2 with azelaic acid is stable, efficient in antimicrobial preservation and reveals improved active substance bioavailability.
authors.affiliation: Department of Microbiology and Medicinal Chemistry, Wroclaw University of Technology, Wyspiańskiego Str. 27, 50-370 Wroclaw, Poland. Electronic address: ewa.burchacka@pwr.wroc.pl.
authors.forename: E
authors.initials: E
authors.lastname: Burchacka
authors.affiliation: Research and Development Center NOVASOME, Olsztyńska Str. 5, 51-423 Wrocław, Poland.
authors.forename: P
authors.initials: P
authors.lastname: Potaczek
authors.affiliation: Research and Development Center NOVASOME, Olsztyńska Str. 5, 51-423 Wrocław, Poland.
authors.forename: P
authors.initials: P
authors.lastname: Paduszyński
authors.affiliation: Department of Industrial Pharmacy, Wrocław Medical University, Borowska Str. 211, 50-556 Wrocław, Poland.
authors.forename: K
authors.initials: K
authors.lastname: Karłowicz-Bodalska
authors.affiliation: Department of Industrial Pharmacy, Wrocław Medical University, Borowska Str. 211, 50-556 Wrocław, Poland.
authors.forename: T
authors.initials: T
authors.lastname: Han
authors.affiliation: Department of Industrial Pharmacy, Wrocław Medical University, Borowska Str. 211, 50-556 Wrocław, Poland.
authors.forename: S
authors.initials: S
authors.lastname: Han
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003998:Dicarboxylic Acids / Q000737:chemistry / Q000494:pharmacology*; D005782:Gels / Q000494:pharmacology*; D008081:Liposomes; D008826:Microbial Sensitivity Tests; D012867:Skin / Q000187:drug effects; D034421:Sus scrofa
chemical_list: D000900:Anti-Bacterial Agents; D003998:Dicarboxylic Acids; D005782:Gels; D008081:Liposomes; C010038:azelaic acid
keywords: Azelaic acid; Liposomal hydrogel; Pharmaceutical formulation