DEVELOPMENT AND EVALUATION OF BIOADHESIVE MUCOSAL DOSAGE FORMS OF PILOCARPINE HCL FOR XEROSTOMIA THERAPY

Objective: Saliva maintains vital mouth functions and acts as a barrier to dental health. Xerostomia, which is characterised as a feeling of dry mouth, adversely affects the patient’s quality of life. Palliative therapies, such as sialagogues, form the based on treatment of xerostomia. The FDAapprov...

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Main Authors: Özlem Akbal Dağıstan, Nur Sena Başarır, Sinem Yaprak Karavana, Ayça Yıldız Peköz
Format: Article
Language:English
Published: Istanbul University Press 2025-03-01
Series:Sabiad
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Online Access:https://cdn.istanbul.edu.tr/file/JTA6CLJ8T5/7F807DCE4D4843D49CF03BBAFE3900D5
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author Özlem Akbal Dağıstan
Nur Sena Başarır
Sinem Yaprak Karavana
Ayça Yıldız Peköz
author_facet Özlem Akbal Dağıstan
Nur Sena Başarır
Sinem Yaprak Karavana
Ayça Yıldız Peköz
author_sort Özlem Akbal Dağıstan
collection DOAJ
description Objective: Saliva maintains vital mouth functions and acts as a barrier to dental health. Xerostomia, which is characterised as a feeling of dry mouth, adversely affects the patient’s quality of life. Palliative therapies, such as sialagogues, form the based on treatment of xerostomia. The FDAapproved sialagogue pilocarpine is currently recommended as the firstline medication for patients. Owing to its wide range of action, oral pilocarpine users may experience several negative side effects. The purpose of this study was to increase the duration of action and prevent systemic side effects of pilocarpine hydrochloride by designing and evaluating prolonged-release formulations of the drug using either xanthan gum, hydroxyethyl cellulose, or a combination of these two natural polymers buccal bioadhesive films. Material and Methods: The films were analysed for their physicochemical, mechanical, bioadhesive, swelling, in vitro release, and in vitro cytotoxicity. Results: Physicochemical and mechanical feature examinations revealed that the Xanthan-HEC combinations showed better results compared to the single polymer-used formulations. The in vitro dissolving profiles of all the optimal formulations showed a sustained release pattern with a steady-state plateau after an initial fast release. Using various release kinetic models to assess drug release kinetics revealed that the Higuchi and Korsmeyer-Peppas correlations are primarily followed by drug release from buccal films. Conclusion: The findings show that the mucoadhesive buccal formulation is a viable method for pilocarpine localised distribution that is both safe and effective in treating xerostomia. Further in vivo studies are planned to assess the pharmacokinetic and histopathological effects of the formulation.
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publishDate 2025-03-01
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spelling doaj-art-1f4ccaf5d47541c6a51686ed45e9cedc2025-08-20T02:14:06ZengIstanbul University PressSabiad2651-40602025-03-0181344110.26650/JARHS2025-1517952123456DEVELOPMENT AND EVALUATION OF BIOADHESIVE MUCOSAL DOSAGE FORMS OF PILOCARPINE HCL FOR XEROSTOMIA THERAPYÖzlem Akbal Dağıstan0https://orcid.org/0000-0002-6524-3535Nur Sena Başarır1https://orcid.org/0000-0002-0695-5292Sinem Yaprak Karavana2https://orcid.org/0000-0001-6010-5902Ayça Yıldız Peköz3https://orcid.org/0000-0003-2243-6684İstanbul Üniversitesi, İstanbul, Türkiyeİstanbul Üniversitesi, İstanbul, TürkiyeEge Üniversitesi, Izmir, Turkiyeİstanbul Üniversitesi, İstanbul, TürkiyeObjective: Saliva maintains vital mouth functions and acts as a barrier to dental health. Xerostomia, which is characterised as a feeling of dry mouth, adversely affects the patient’s quality of life. Palliative therapies, such as sialagogues, form the based on treatment of xerostomia. The FDAapproved sialagogue pilocarpine is currently recommended as the firstline medication for patients. Owing to its wide range of action, oral pilocarpine users may experience several negative side effects. The purpose of this study was to increase the duration of action and prevent systemic side effects of pilocarpine hydrochloride by designing and evaluating prolonged-release formulations of the drug using either xanthan gum, hydroxyethyl cellulose, or a combination of these two natural polymers buccal bioadhesive films. Material and Methods: The films were analysed for their physicochemical, mechanical, bioadhesive, swelling, in vitro release, and in vitro cytotoxicity. Results: Physicochemical and mechanical feature examinations revealed that the Xanthan-HEC combinations showed better results compared to the single polymer-used formulations. The in vitro dissolving profiles of all the optimal formulations showed a sustained release pattern with a steady-state plateau after an initial fast release. Using various release kinetic models to assess drug release kinetics revealed that the Higuchi and Korsmeyer-Peppas correlations are primarily followed by drug release from buccal films. Conclusion: The findings show that the mucoadhesive buccal formulation is a viable method for pilocarpine localised distribution that is both safe and effective in treating xerostomia. Further in vivo studies are planned to assess the pharmacokinetic and histopathological effects of the formulation.https://cdn.istanbul.edu.tr/file/JTA6CLJ8T5/7F807DCE4D4843D49CF03BBAFE3900D5buccal deliverybuccal filmpilocarpine hydrochloridesialogoguesxerostomia
spellingShingle Özlem Akbal Dağıstan
Nur Sena Başarır
Sinem Yaprak Karavana
Ayça Yıldız Peköz
DEVELOPMENT AND EVALUATION OF BIOADHESIVE MUCOSAL DOSAGE FORMS OF PILOCARPINE HCL FOR XEROSTOMIA THERAPY
Sabiad
buccal delivery
buccal film
pilocarpine hydrochloride
sialogogues
xerostomia
title DEVELOPMENT AND EVALUATION OF BIOADHESIVE MUCOSAL DOSAGE FORMS OF PILOCARPINE HCL FOR XEROSTOMIA THERAPY
title_full DEVELOPMENT AND EVALUATION OF BIOADHESIVE MUCOSAL DOSAGE FORMS OF PILOCARPINE HCL FOR XEROSTOMIA THERAPY
title_fullStr DEVELOPMENT AND EVALUATION OF BIOADHESIVE MUCOSAL DOSAGE FORMS OF PILOCARPINE HCL FOR XEROSTOMIA THERAPY
title_full_unstemmed DEVELOPMENT AND EVALUATION OF BIOADHESIVE MUCOSAL DOSAGE FORMS OF PILOCARPINE HCL FOR XEROSTOMIA THERAPY
title_short DEVELOPMENT AND EVALUATION OF BIOADHESIVE MUCOSAL DOSAGE FORMS OF PILOCARPINE HCL FOR XEROSTOMIA THERAPY
title_sort development and evaluation of bioadhesive mucosal dosage forms of pilocarpine hcl for xerostomia therapy
topic buccal delivery
buccal film
pilocarpine hydrochloride
sialogogues
xerostomia
url https://cdn.istanbul.edu.tr/file/JTA6CLJ8T5/7F807DCE4D4843D49CF03BBAFE3900D5
work_keys_str_mv AT ozlemakbaldagıstan developmentandevaluationofbioadhesivemucosaldosageformsofpilocarpinehclforxerostomiatherapy
AT nursenabasarır developmentandevaluationofbioadhesivemucosaldosageformsofpilocarpinehclforxerostomiatherapy
AT sinemyaprakkaravana developmentandevaluationofbioadhesivemucosaldosageformsofpilocarpinehclforxerostomiatherapy
AT aycayıldızpekoz developmentandevaluationofbioadhesivemucosaldosageformsofpilocarpinehclforxerostomiatherapy