title: Preparation and optimization of chlorophene-loaded nanospheres as controlled release antimicrobial delivery systems.
abstract: Chlorophene-loaded nanospheres with various formulation parameters were evaluated. The optimal formulation was found at 0.1% w/v of poloxamer 407, 15 mL of ethyl acetate and 20% initial chlorophene loading that provided the suitable size (179 nm), the highest loading content (19.2%), encapsulation efficiency (88.0%) and yield (91.6%). Moreover, encapsulation of chlorophene in nanospheres was able to prolong and sustain drug release over one month. Chlorophene-loaded nanospheres were effective against Staphylococcus aureus (S. aureus) and Candida albicans (C. albicans), the main cause of hospital-acquired infections. Chlorophene-loaded nanospheres were effective against S. aureus (>46 µg/mL) and C. albicans (>184 µg/mL). These nanospheres appeared to have profound effect on the time-dependent hemolytic activity due to gradual release of chlorophene. At the concentration of 46 µg/mL, nearly no HRBC hemolysis in 24 h compared to 80% of hemolysis from free drug. In conclusion, polymeric nanospheres were successfully fabricated to encapsulate chlorophene which can eliminate inherent toxicity of drugs and have potential uses in prolonged release of antimicrobial.
authors.affiliation: a Department of Biomedical Engineering, Faculty of Engineering , Mahidol University , NakornPathom , Thailand .|b Department of Chemistry , Mahidol University , Bangkok , Thailand .|c Faculty of Science, Center of Excellence for Innovation in Chemistry , Mahidol University , Bangkok , Thailand , and.
authors.forename: Hathaichanok
authors.initials: H
authors.lastname: Phuengkham
authors.affiliation: d Research and Development Division , SJI , Bangkok , Thailand.
authors.forename: Veerawat
authors.initials: V
authors.lastname: Teeranachaideekul
authors.affiliation: d Research and Development Division , SJI , Bangkok , Thailand.
authors.forename: Malyn
authors.initials: M
authors.lastname: Chulasiri
authors.affiliation: a Department of Biomedical Engineering, Faculty of Engineering , Mahidol University , NakornPathom , Thailand .|b Department of Chemistry , Mahidol University , Bangkok , Thailand .|c Faculty of Science, Center of Excellence for Innovation in Chemistry , Mahidol University , Bangkok , Thailand , and.
authors.forename: Norased
authors.initials: N
authors.lastname: Nasongkla
mesh_terms: D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000138:chemical synthesis*; D002176:Candida albicans / Q000187:drug effects / Q000502:physiology; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004003:Dichlorophen / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D008826:Microbial Sensitivity Tests / Q000379:methods; D054118:Nanospheres / Q000008:administration & dosage / Q000737:chemistry*; D013211:Staphylococcus aureus / Q000187:drug effects / Q000502:physiology
chemical_list: D000890:Anti-Infective Agents; D003692:Delayed-Action Preparations; C004660:clorophene; D004003:Dichlorophen
keywords: Antimicrobial; chlorophene; controlled release; nanospheres