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1.
Int J Pharm ; 479(1): 88-95, 2015 Feb 01.
Article in English | MEDLINE | ID: mdl-25527211

ABSTRACT

Zinc oxide (ZnO) appears as a promising preservative for pharmaceutical or cosmetic formulations. The other ingredients of the formulations may have specific interactions with ZnO that alter its antimicrobial properties. The influence of common formulation excipients on the antimicrobial efficacy of ZnO has been investigated in simple model systems and in typical topical products containing a complex formulation. A wide variety of formulation excipients have been investigated for their interactions with ZnO: antioxidants, chelating agents, electrolytes, titanium dioxide pigment. The antimicrobial activity of ZnO against Escherichia coli was partially inhibited by NaCl and MgSO4 salts. A synergistic influence of uncoated titanium dioxide has been observed. The interference effects of antioxidants and chelating agents were quite specific. The interactions of these substances with ZnO particles and with the soluble species released by ZnO were discussed so as to reach scientific guidelines for the choice of the ingredients. The preservative efficacy of ZnO was assessed by challenge testing in three different formulations: an oil-in-water emulsion; a water-in-oil emulsion and a dry powder. The addition of ZnO in complex formulations significantly improved the microbiological quality of the products, in spite of the presence of other ingredients that modulate the antimicrobial activity.


Subject(s)
Anti-Infective Agents , Excipients , Preservatives, Pharmaceutical , Zinc Oxide , Administration, Topical , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Ascorbic Acid/analogs & derivatives , Ascorbic Acid/chemistry , Ascorbic Acid/pharmacology , Aspergillus/drug effects , Aspergillus/growth & development , Butylated Hydroxytoluene/chemistry , Butylated Hydroxytoluene/pharmacology , Candida albicans/drug effects , Candida albicans/growth & development , Chelating Agents/chemistry , Chelating Agents/pharmacology , Edetic Acid/chemistry , Edetic Acid/pharmacology , Escherichia coli/drug effects , Escherichia coli/growth & development , Excipients/chemistry , Excipients/pharmacology , Magnesium Sulfate/chemistry , Magnesium Sulfate/pharmacology , Preservatives, Pharmaceutical/chemistry , Preservatives, Pharmaceutical/pharmacology , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/growth & development , Sodium Chloride/chemistry , Sodium Chloride/pharmacology , Staphylococcus aureus/drug effects , Staphylococcus aureus/growth & development , Titanium/chemistry , Titanium/pharmacology , Zinc Oxide/chemistry , Zinc Oxide/pharmacology
2.
Int J Pharm ; 460(1-2): 92-100, 2014 Jan 02.
Article in English | MEDLINE | ID: mdl-24211859

ABSTRACT

Zinc oxide is commonly used in pharmaceutical products to prevent or treat topical or systemic diseases owing to its antimicrobial properties, but it is scarcely used as preservative in topical formulations. The aim of this work was to investigate the antimicrobial activity of zinc oxide (ZnO) powders on the five microbial strains used for Challenge Tests in order to evaluate this inorganic compound as a preservative in topical formulation and assess relationships between the structural parameters of ZnO particles and their antimicrobial activity. For this purpose, the physicochemical characteristics of three ZnO grades were measured and their antimicrobial efficacy against the following micro-organisms - Escherichia coli; Staphylococcus aureus; Pseudomonas aeruginosa; Candida albicans; Aspergillus brasiliensis - was assessed using disc diffusion susceptibility tests and a broth dilution method. The comprehensive dataset of physicochemical characteristics and antimicrobial activities (MIC and MBC) is discussed regarding methodological issues related to the particulate nature of ZnO and structure-activity relationships. Every ZnO grade showed bactericidal and antifungal activity against the five tested micro-organisms in a concentration dependent manner. ZnO particles with smaller size, larger specific area and higher porosity exhibit higher antimicrobial activity. Such trends are related to their mechanisms of antimicrobial activity.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Zinc Oxide/pharmacology , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemistry , Aspergillus/drug effects , Aspergillus/growth & development , Candida albicans/drug effects , Candida albicans/growth & development , Escherichia coli/drug effects , Escherichia coli/growth & development , Microbial Sensitivity Tests , Particle Size , Porosity , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/growth & development , Staphylococcus aureus/drug effects , Staphylococcus aureus/growth & development , Structure-Activity Relationship , Zinc Oxide/chemistry
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