Kinetics of neomycin release from polylactide spheres and its antimicrobial activity.


Journal

Polimery w medycynie
ISSN: 0370-0747
Titre abrégé: Polim Med
Pays: Poland
ID NLM: 7509477

Informations de publication

Date de publication:
Historique:
pubmed: 31 7 2021
medline: 12 10 2021
entrez: 30 7 2021
Statut: ppublish

Résumé

Neomycin is a natural aminoglycoside antibiotic produced by actinomycete Streptomyces fradiae. It exerts bacteriostatic and bactericidal activity against Gram-negative bacteria, certain Gram-positive bacteria and Mycobacterium tuberculosis. Neomycin inhibits the biosynthesis of bacterial proteins by impairing their life functions, leading to death of cells. To examine the effect of molecular weight of polylactide (PLA), the applied stabilizer as well as mixing speed used in the encapsulation process on the size of obtained spheres. Examination of the kinetics of neomycin release from the obtained PLA spheres and determination of the antimicrobial activity of the neomycin-containing spheres against selected strains of bacteria, yeast and fungi have also been necessary. Polylactide (Mn 3000-40,000 g/mol) was obtained in-house. Other materials used in the study were as follows: L-lactic acid (PLLA; Mn 66,500 g/mol and 86,000 g/mol), polyvinyl alcohol (PVA) as a stabilizer of emulsion (Mw 30,000 g/mol, 130,000 g/mol; degree of hydrolysis 88%) as well as dichloromethane, p.a. and dimethyl sulfoxide (DMSO), p.a. as solvents. Distilled water was obtained in-house. Neomycin sulfate was used for encapsulation; phosphate (pH 7.2) and acetate (pH 4.5) buffers were used for the examination of the active pharmaceutical ingredient (API) dissolution profile. Antimicrobial activity was tested using commercial cell lines and the following media: Mueller-Hinton agar (MHA), Mueller-Hinton broth (MHB), yeast extract peptone dextrose (YPD), and potato dextrose agar (PDA). Neomycin-containing PLA spheres were obtained using an emulsion method. The average molecular weight of PLA, the average molecular weight of PVA and mixing speed on the size of obtained spheres were investigated. Furthermore, the profile of API dissolution from the spheres and antimicrobial activity of neomycin-containing spheres against certain strains of bacteria, yeast and fungi were determined. We demonstrated that efficient encapsulation of neomycin requires spheres of a <200 mm diameter.

Sections du résumé

BACKGROUND BACKGROUND
Neomycin is a natural aminoglycoside antibiotic produced by actinomycete Streptomyces fradiae. It exerts bacteriostatic and bactericidal activity against Gram-negative bacteria, certain Gram-positive bacteria and Mycobacterium tuberculosis. Neomycin inhibits the biosynthesis of bacterial proteins by impairing their life functions, leading to death of cells.
OBJECTIVES OBJECTIVE
To examine the effect of molecular weight of polylactide (PLA), the applied stabilizer as well as mixing speed used in the encapsulation process on the size of obtained spheres. Examination of the kinetics of neomycin release from the obtained PLA spheres and determination of the antimicrobial activity of the neomycin-containing spheres against selected strains of bacteria, yeast and fungi have also been necessary.
MATERIAL AND METHODS METHODS
Polylactide (Mn 3000-40,000 g/mol) was obtained in-house. Other materials used in the study were as follows: L-lactic acid (PLLA; Mn 66,500 g/mol and 86,000 g/mol), polyvinyl alcohol (PVA) as a stabilizer of emulsion (Mw 30,000 g/mol, 130,000 g/mol; degree of hydrolysis 88%) as well as dichloromethane, p.a. and dimethyl sulfoxide (DMSO), p.a. as solvents. Distilled water was obtained in-house. Neomycin sulfate was used for encapsulation; phosphate (pH 7.2) and acetate (pH 4.5) buffers were used for the examination of the active pharmaceutical ingredient (API) dissolution profile. Antimicrobial activity was tested using commercial cell lines and the following media: Mueller-Hinton agar (MHA), Mueller-Hinton broth (MHB), yeast extract peptone dextrose (YPD), and potato dextrose agar (PDA).
RESULTS RESULTS
Neomycin-containing PLA spheres were obtained using an emulsion method. The average molecular weight of PLA, the average molecular weight of PVA and mixing speed on the size of obtained spheres were investigated. Furthermore, the profile of API dissolution from the spheres and antimicrobial activity of neomycin-containing spheres against certain strains of bacteria, yeast and fungi were determined.
CONCLUSIONS CONCLUSIONS
We demonstrated that efficient encapsulation of neomycin requires spheres of a <200 mm diameter.

Identifiants

pubmed: 34327877
doi: 10.17219/pim/139586
doi:

Substances chimiques

Anti-Bacterial Agents 0
Polyesters 0
poly(lactide) 459TN2L5F5
Neomycin I16QD7X297

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

17-24

Auteurs

Agnieszka Gadomska-Gajadhur (A)

Chair of Polymer Chemistry and Technology, Faculty of Chemistry, Warsaw University of Technology, Poland.

Paweł Ruśkowski (P)

Chair of Polymer Chemistry and Technology, Faculty of Chemistry, Warsaw University of Technology, Poland.

Aleksandra Kruk (A)

Department of Pharmacognosy and Molecular Basis of Phytotherapy, Faculty of Pharmacy, Medical University of Warsaw, Poland.

Jolanta Mierzejewska (J)

Chair of Drug and Cosmetics Biotechnology, Faculty of Chemistry, Warsaw University of Technology, Poland.

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Classifications MeSH