Metronidazole-Loaded Polyethyleneimine and Chitosan-Based Liquid Crystalline System for Treatment of Staphylococcal Skin Infections

Author(s)

Victorelli, Francesca Damiani ^[1] ; Fioramonti Calixto, Giovana Maria ^[1] ; Dos Santos Ramos, Matheus Aparecido ^[1] ; Bauab, Tais Maria ^[1] ; Chorilli, Marlus ^[1]

Affiliation

^[1] Sao Paulo State Univ UNESP, Sch Pharmaceut Sci, BR-14800903 Araraquara, SP - Brazil

• Document type: Journal article
• Source: JOURNAL OF BIOMEDICAL NANOTECHNOLOGY; v. 14, n. 1, p. 227-237, JAN 2018.
• Web of Science Citations: 4

Abstract

Staphylococcus aureus is a common gram-positive bacterium of the human skin microbiota. It is also a dangerous pathogen that can cause serious and even lethal skin infections. The topical administration of metronidazole via nanotechnology-based drug delivery systems, such as liquid crystalline systems, can modulate both the drug permeation and activity, decreasing its side effects and increasing the drug potent activity against the gram-positive bacteria. This study aimed at: (1) structurally developing and characterizing a liquid crystalline systems composed of chitosan and polyethyleneimine dispersion as the aqueous phase, oleic acid as the oily phase, and ethoxylated and propoxylated cetyl alcohol as the surfactant (FPC) for metronidazole incorporation (0.5% w/w); (2) evaluating the in vitro release and skin permeation and retention properties of the metronidazole-loaded liquid crystalline systems (FPC-M); (3) investigating the in vitro antibacterial activity of FPC-M against Staphylococcus aureus. Polarised light microscopy indicated that both FPC and FPC-M are hexagonal systems. Rheological, texture, and bioadhesion assays showed that both are elastic and bioadhesive systems. According to the results of the in vitro release, permeation, and retention assays, FPC can modulate metronidazole release and allow metronidazole to stay for a longer time on the skin. The determination of FPC-M activity against Staphylococcus aureus showed that it could target the bacterial cell. In conclusion, the liquid crystalline systems developed in this study can improve the clinical performance of metronidazole in the treatment of staphylococcal skin infections. (AU)

• FAPESP's process: 14/50928-2 - INCT 2014: Pharmaceutical Nanotechnology: a transdisciplinary approach
• Grantee: Maria Vitória Lopes Badra Bentley
• Support Opportunities: Research Projects - Thematic Grants
• FAPESP's process: 13/01565-1 - Mucoadhesive precursor systems of liquids crystals for buccal admnistration of antigelatinolytic peptide associated with photodynamic therapy in the treatment of oral cancer
• Grantee: Giovana Maria Fioramonti Calixto Balian
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 17/10016-2 - Liquid crystal precursor systems as a strategy for vaginal administration of CTT1 peptide: pharmacotechnical development and potential application for the treatment of cervical cancer
• Grantee: Marlus Chorilli
• Support Opportunities: Regular Research Grants