New Eye Drop Formulation Based on Desonide and Xanthan Gum in Dry Eye Disease: Nonclinical Studies

<b>Background/Objectives:</b> A novel ophthalmic formulation, XanterDES, containing 0.2% xanthan gum and 0.025% desonide sodium phosphate (DES), was developed to alleviate ocular surface discomfort and irritation. This study aimed to evaluate its pharmacodynamic properties and to charact...

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Main Authors: Santa Viola, Luca Rosario La Rosa, Giuseppe De Pasquale, Manuela Santonocito, Donato Spina, Ilenia Abbate, Francesco Giuliano, Maria Cristina Curatolo, Maria Grazia Mazzone, Cristina Zappulla
Format: Article
Language:English
Published: MDPI AG 2025-02-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/17/2/235
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author Santa Viola
Luca Rosario La Rosa
Giuseppe De Pasquale
Manuela Santonocito
Donato Spina
Ilenia Abbate
Francesco Giuliano
Maria Cristina Curatolo
Maria Grazia Mazzone
Cristina Zappulla
author_facet Santa Viola
Luca Rosario La Rosa
Giuseppe De Pasquale
Manuela Santonocito
Donato Spina
Ilenia Abbate
Francesco Giuliano
Maria Cristina Curatolo
Maria Grazia Mazzone
Cristina Zappulla
author_sort Santa Viola
collection DOAJ
description <b>Background/Objectives:</b> A novel ophthalmic formulation, XanterDES, containing 0.2% xanthan gum and 0.025% desonide sodium phosphate (DES), was developed to alleviate ocular surface discomfort and irritation. This study aimed to evaluate its pharmacodynamic properties and to characterize its rheological behavior and mucoadhesive characteristics, compared to another formulation containing 0.2% hyaluronic acid and 0.001% hydrocortisone (HYD). <b>Methods:</b> A rabbit (New Zealand White) model of LPS-induced uveitis was used to test different concentrations of DES on ocular markers of inflammation. The efficacy of XanterDES and HYD on induced dry eye was evaluated by assessing tear volume and corneal damage in C57BL/6 mice exposed to a controlled environmental chamber. The rheological and mucoadhesive properties of XanterDES and HYD were assessed using a HAAKE RheoStress RS600 rheometer and a TA-XT2 texture analyzer, respectively. <b>Results:</b> In the uveitis model, unlike DES 0.25%, a low concentration of 0.025% DES showed a significant inhibitory activity localized to the eye surface and effectively reduced corneal edema. In the dry eye model, XanterDES demonstrated superior efficacy compared to HYD, effectively preventing both tear volume reduction and corneal damage. XanterDES also demonstrated pseudoplastic and enhanced mucoadhesive properties compared to HYD. <b>Conclusions:</b> The ancillary anti-inflammatory effects of a low dose of DES combined with the biophysical properties of xanthan gum are supportive of a favorable therapeutic profile, promoting the maintenance or restoration of ocular surface homeostasis while minimizing the risk of adverse effects typically associated with standard-dose corticosteroids. The comparison with another low-dose corticosteroid highlights the superiority of XanterDES in pharmacodynamic and biophysical performance.
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spelling doaj-art-0b420ca0209d4a4f99ebc4f5a5e94d982025-08-20T02:01:24ZengMDPI AGPharmaceutics1999-49232025-02-0117223510.3390/pharmaceutics17020235New Eye Drop Formulation Based on Desonide and Xanthan Gum in Dry Eye Disease: Nonclinical StudiesSanta Viola0Luca Rosario La Rosa1Giuseppe De Pasquale2Manuela Santonocito3Donato Spina4Ilenia Abbate5Francesco Giuliano6Maria Cristina Curatolo7Maria Grazia Mazzone8Cristina Zappulla9Innovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyBusiness Development and Open Innovation, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyBusiness Development and Open Innovation, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, Italy<b>Background/Objectives:</b> A novel ophthalmic formulation, XanterDES, containing 0.2% xanthan gum and 0.025% desonide sodium phosphate (DES), was developed to alleviate ocular surface discomfort and irritation. This study aimed to evaluate its pharmacodynamic properties and to characterize its rheological behavior and mucoadhesive characteristics, compared to another formulation containing 0.2% hyaluronic acid and 0.001% hydrocortisone (HYD). <b>Methods:</b> A rabbit (New Zealand White) model of LPS-induced uveitis was used to test different concentrations of DES on ocular markers of inflammation. The efficacy of XanterDES and HYD on induced dry eye was evaluated by assessing tear volume and corneal damage in C57BL/6 mice exposed to a controlled environmental chamber. The rheological and mucoadhesive properties of XanterDES and HYD were assessed using a HAAKE RheoStress RS600 rheometer and a TA-XT2 texture analyzer, respectively. <b>Results:</b> In the uveitis model, unlike DES 0.25%, a low concentration of 0.025% DES showed a significant inhibitory activity localized to the eye surface and effectively reduced corneal edema. In the dry eye model, XanterDES demonstrated superior efficacy compared to HYD, effectively preventing both tear volume reduction and corneal damage. XanterDES also demonstrated pseudoplastic and enhanced mucoadhesive properties compared to HYD. <b>Conclusions:</b> The ancillary anti-inflammatory effects of a low dose of DES combined with the biophysical properties of xanthan gum are supportive of a favorable therapeutic profile, promoting the maintenance or restoration of ocular surface homeostasis while minimizing the risk of adverse effects typically associated with standard-dose corticosteroids. The comparison with another low-dose corticosteroid highlights the superiority of XanterDES in pharmacodynamic and biophysical performance.https://www.mdpi.com/1999-4923/17/2/235xanthan gumdesonide sodium phosphateocular surfacedry eye
spellingShingle Santa Viola
Luca Rosario La Rosa
Giuseppe De Pasquale
Manuela Santonocito
Donato Spina
Ilenia Abbate
Francesco Giuliano
Maria Cristina Curatolo
Maria Grazia Mazzone
Cristina Zappulla
New Eye Drop Formulation Based on Desonide and Xanthan Gum in Dry Eye Disease: Nonclinical Studies
Pharmaceutics
xanthan gum
desonide sodium phosphate
ocular surface
dry eye
title New Eye Drop Formulation Based on Desonide and Xanthan Gum in Dry Eye Disease: Nonclinical Studies
title_full New Eye Drop Formulation Based on Desonide and Xanthan Gum in Dry Eye Disease: Nonclinical Studies
title_fullStr New Eye Drop Formulation Based on Desonide and Xanthan Gum in Dry Eye Disease: Nonclinical Studies
title_full_unstemmed New Eye Drop Formulation Based on Desonide and Xanthan Gum in Dry Eye Disease: Nonclinical Studies
title_short New Eye Drop Formulation Based on Desonide and Xanthan Gum in Dry Eye Disease: Nonclinical Studies
title_sort new eye drop formulation based on desonide and xanthan gum in dry eye disease nonclinical studies
topic xanthan gum
desonide sodium phosphate
ocular surface
dry eye
url https://www.mdpi.com/1999-4923/17/2/235
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