Chitosan Ascorbate Nanoparticles for the Vaginal Delivery of Antibiotic Drugs in Atrophic Vaginitis

The aim of the present work was the development of chitosan ascorbate nanoparticles (CSA NPs) loaded into a fast-dissolving matrix for the delivery of antibiotic drugs in the treatment of atrophic vaginitis. CSA NPs loaded with amoxicillin trihydrate (AX) were obtained by ionotropic gelation in the...

Full description

Bibliographic Details
Main Authors: Silvia Rossi, Barbara Vigani, Antonella Puccio, Maria Cristina Bonferoni, Giuseppina Sandri, Franca Ferrari
Format: Article
Language:English
Published: MDPI AG 2017-10-01
Series:Marine Drugs
Subjects:
Online Access:https://www.mdpi.com/1660-3397/15/10/319
_version_ 1798002389578416128
author Silvia Rossi
Barbara Vigani
Antonella Puccio
Maria Cristina Bonferoni
Giuseppina Sandri
Franca Ferrari
author_facet Silvia Rossi
Barbara Vigani
Antonella Puccio
Maria Cristina Bonferoni
Giuseppina Sandri
Franca Ferrari
author_sort Silvia Rossi
collection DOAJ
description The aim of the present work was the development of chitosan ascorbate nanoparticles (CSA NPs) loaded into a fast-dissolving matrix for the delivery of antibiotic drugs in the treatment of atrophic vaginitis. CSA NPs loaded with amoxicillin trihydrate (AX) were obtained by ionotropic gelation in the presence of pentasodium tripolyphosphate (TPP). Different CSA:TPP and CSA:AX weight ratios were considered and their influence on the particle size, polydispersion index and production yield were investigated. CSA NPs were characterized for mucoadhesive, wound healing and antimicrobial properties. Subsequently, CSA NPs were loaded in polymeric matrices, whose composition was optimized using a DoE (Design of Experiments) approach (simplex centroid design). Matrices were obtained by freeze-drying aqueous solutions of three hydrophilic excipients, polyvinylpirrolidone, mannitol and glycin. They should possess a mechanical resistance suitable for the administration into the vaginal cavity and should readily dissolve in the vaginal fluid. In addition to antioxidant properties, due to the presence of ascorbic acid, CSA NPs showed in vitro mucoadhesive, wound healing and antimicrobial properties. In particular, nanoparticles were characterized by an improved antimicrobial activity with respect to a chitosan solution, prepared at the same concentration. The optimized matrix was characterized by mechanical resistance and by the fast release in simulated vaginal fluid of nanoparticles characterized by unchanged size.
first_indexed 2024-04-11T11:51:23Z
format Article
id doaj.art-ce317f3708db43869bdc9640edd9e99c
institution Directory Open Access Journal
issn 1660-3397
language English
last_indexed 2024-04-11T11:51:23Z
publishDate 2017-10-01
publisher MDPI AG
record_format Article
series Marine Drugs
spelling doaj.art-ce317f3708db43869bdc9640edd9e99c2022-12-22T04:25:19ZengMDPI AGMarine Drugs1660-33972017-10-01151031910.3390/md15100319md15100319Chitosan Ascorbate Nanoparticles for the Vaginal Delivery of Antibiotic Drugs in Atrophic VaginitisSilvia Rossi0Barbara Vigani1Antonella Puccio2Maria Cristina Bonferoni3Giuseppina Sandri4Franca Ferrari5Department of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyThe aim of the present work was the development of chitosan ascorbate nanoparticles (CSA NPs) loaded into a fast-dissolving matrix for the delivery of antibiotic drugs in the treatment of atrophic vaginitis. CSA NPs loaded with amoxicillin trihydrate (AX) were obtained by ionotropic gelation in the presence of pentasodium tripolyphosphate (TPP). Different CSA:TPP and CSA:AX weight ratios were considered and their influence on the particle size, polydispersion index and production yield were investigated. CSA NPs were characterized for mucoadhesive, wound healing and antimicrobial properties. Subsequently, CSA NPs were loaded in polymeric matrices, whose composition was optimized using a DoE (Design of Experiments) approach (simplex centroid design). Matrices were obtained by freeze-drying aqueous solutions of three hydrophilic excipients, polyvinylpirrolidone, mannitol and glycin. They should possess a mechanical resistance suitable for the administration into the vaginal cavity and should readily dissolve in the vaginal fluid. In addition to antioxidant properties, due to the presence of ascorbic acid, CSA NPs showed in vitro mucoadhesive, wound healing and antimicrobial properties. In particular, nanoparticles were characterized by an improved antimicrobial activity with respect to a chitosan solution, prepared at the same concentration. The optimized matrix was characterized by mechanical resistance and by the fast release in simulated vaginal fluid of nanoparticles characterized by unchanged size.https://www.mdpi.com/1660-3397/15/10/319chitosan ascorbatenanoparticlesvaginal administrationfast dissolving polymeric matrixwound healing
spellingShingle Silvia Rossi
Barbara Vigani
Antonella Puccio
Maria Cristina Bonferoni
Giuseppina Sandri
Franca Ferrari
Chitosan Ascorbate Nanoparticles for the Vaginal Delivery of Antibiotic Drugs in Atrophic Vaginitis
Marine Drugs
chitosan ascorbate
nanoparticles
vaginal administration
fast dissolving polymeric matrix
wound healing
title Chitosan Ascorbate Nanoparticles for the Vaginal Delivery of Antibiotic Drugs in Atrophic Vaginitis
title_full Chitosan Ascorbate Nanoparticles for the Vaginal Delivery of Antibiotic Drugs in Atrophic Vaginitis
title_fullStr Chitosan Ascorbate Nanoparticles for the Vaginal Delivery of Antibiotic Drugs in Atrophic Vaginitis
title_full_unstemmed Chitosan Ascorbate Nanoparticles for the Vaginal Delivery of Antibiotic Drugs in Atrophic Vaginitis
title_short Chitosan Ascorbate Nanoparticles for the Vaginal Delivery of Antibiotic Drugs in Atrophic Vaginitis
title_sort chitosan ascorbate nanoparticles for the vaginal delivery of antibiotic drugs in atrophic vaginitis
topic chitosan ascorbate
nanoparticles
vaginal administration
fast dissolving polymeric matrix
wound healing
url https://www.mdpi.com/1660-3397/15/10/319
work_keys_str_mv AT silviarossi chitosanascorbatenanoparticlesforthevaginaldeliveryofantibioticdrugsinatrophicvaginitis
AT barbaravigani chitosanascorbatenanoparticlesforthevaginaldeliveryofantibioticdrugsinatrophicvaginitis
AT antonellapuccio chitosanascorbatenanoparticlesforthevaginaldeliveryofantibioticdrugsinatrophicvaginitis
AT mariacristinabonferoni chitosanascorbatenanoparticlesforthevaginaldeliveryofantibioticdrugsinatrophicvaginitis
AT giuseppinasandri chitosanascorbatenanoparticlesforthevaginaldeliveryofantibioticdrugsinatrophicvaginitis
AT francaferrari chitosanascorbatenanoparticlesforthevaginaldeliveryofantibioticdrugsinatrophicvaginitis