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Formulation of pH responsive multilamellar vesicles for targeted delivery of hydrophilic antibiotics.
Omolo, Calvin A; Hassan, Daniel; Devnarain, Nikita; Jaglal, Yajna; Mocktar, Chunderika; Kalhapure, Rahul S; Jadhav, Mahantesh; Govender, Thirumala.
Afiliación
  • Omolo CA; Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Private Bag, Durban X54001, Durban, 4000, South Africa; Department of Pharmaceutics and Pharmacy Practice, School of Pharmacy and Health Sciences, United States International University-Africa, P. O. Box
  • Hassan D; Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Private Bag, Durban X54001, Durban, 4000, South Africa.
  • Devnarain N; Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Private Bag, Durban X54001, Durban, 4000, South Africa.
  • Jaglal Y; Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Private Bag, Durban X54001, Durban, 4000, South Africa.
  • Mocktar C; Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Private Bag, Durban X54001, Durban, 4000, South Africa.
  • Kalhapure RS; Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Private Bag, Durban X54001, Durban, 4000, South Africa.
  • Jadhav M; Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Private Bag, Durban X54001, Durban, 4000, South Africa.
  • Govender T; Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Private Bag, Durban X54001, Durban, 4000, South Africa. Electronic address: govenderth@ukzn.ac.za.
Colloids Surf B Biointerfaces ; 207: 112043, 2021 Nov.
Article en En | MEDLINE | ID: mdl-34416442
Fight against antimicrobial resistance calls for innovative strategies that can target infection sites and enhance activity of antibiotics. Herein is a pH responsive multilamellar vesicles (MLVs) for targeting bacterial infection sites. The vancomycin (VCM) loaded MLVs had 62.25 ± 8.7 nm, 0.15 ± 0.01 and -5.55 ± 2.76 mV size, PDI and zeta potential, respectively at pH 7.4. The MLVs had a negative ZP at pH 7.4 that switched to a positive charge and faster release of the drug at acidic pH. The encapsulation efficiency was found to be 46.34 ± 3.88 %. In silico studies of the lipids, interaction suggested an energetically stable system. Studies to determine the minimum inhibitory concentration studies (MIC) showed the MLVs had 2-times and 8-times MIC against Staphylococcus aureus (SA) and Methicillin resistance SA respectively at physiological pH. While at pH 6.0 there was 8 times reduction in MICs for the formulation against SA and MRSA in comparison to the bare drug. Fluorescence-activated Cell Sorting (FACS) studies demonstrated that even with 8-times lower MIC, MLVs had a similar elimination ability of MRSA cells when compared to the bare drug. Fluorescence microscopy showed MLVs had the ability to clear biofilms while the bare drug could not. Mice skin infection models studies showed that the colony finding units (CFUs) of MRSA recovered from groups treated with MLVs was 4,050 and 525-fold lower than the untreated and bare VCM treated groups, respectively. This study demonstrated pH-responsive multilamellar vesicles as effective system for targeting and enhancing antibacterial agents.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Nanopartículas / Staphylococcus aureus Resistente a Meticilina Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Colloids Surf B Biointerfaces Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Nanopartículas / Staphylococcus aureus Resistente a Meticilina Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Colloids Surf B Biointerfaces Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article Pais de publicación: Países Bajos