Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics
Worldwide, 40 to 50% of women suffer from reproductive tract infections. Most of these infections are mixed infections, are recurrent and difficult to treat with antimicrobials or antifungals alone. For symptomatic relief of infections, oral antimicrobial therapy must be combined with topical therap...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-10-01
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| Series: | Gels |
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| Online Access: | https://www.mdpi.com/2310-2861/9/11/851 |
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| author | Sanjeevani Deshkar Purva Yeole Jayashri Mahore Ankita Shinde Prabhanjan Giram |
| author_facet | Sanjeevani Deshkar Purva Yeole Jayashri Mahore Ankita Shinde Prabhanjan Giram |
| author_sort | Sanjeevani Deshkar |
| collection | DOAJ |
| description | Worldwide, 40 to 50% of women suffer from reproductive tract infections. Most of these infections are mixed infections, are recurrent and difficult to treat with antimicrobials or antifungals alone. For symptomatic relief of infections, oral antimicrobial therapy must be combined with topical therapy. The purpose of this work is to optimize and develop a polyelectrolyte complex (PEC) of chitosan/anion for the formulation of posaconazole- and probiotic-loaded vaginal hydrogel inserts with prolonged release and significant mucoadhesion. PECs were prepared using chitosan as cationic and carrageenan, pectin and polycarbophil as anionic polymers via a lyophilization technique. PEC formation was confirmed by scanning electron microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry, by observing changes in its surface, physical and thermal properties. The probiotic, <i>Lactobacillus casei</i>, was added to the PEC during the lyophilization process and the effect on the probiotic viability was studied. The PECs were further compressed along with posaconazole to form hydrogel inserts and optimized using a 3<sup>2</sup> full-factorial design. The hydrogel inserts were assessed for swelling behavior, drug release, in vitro mucoadhesion and in vitro antifungal activity. The chitosan–pectin hydrogel insert demonstrated excellent mucoadhesion (1.25 N), sustained drug release (88.2 ± 2.4% in 8 h) and a swelling index of 154.7%. The efficacy of hydrogel inserts was evaluated using in vitro study with a co-culture of <i>Lactobacillus casei</i> and <i>Candida albicans</i>. This study revealed an increase in <i>Lactobacilli casei</i> count and a significant drop in the viable count of <i>Candida albicans</i> (4-log reduction in 24 h), indicating the effectiveness of hydrogel inserts in alleviating the fungal infection. Overall, our study demonstrated the potential of the hydrogel insert for preventing vaginal infection and restoring normal vaginal microbiota. |
| first_indexed | 2024-03-09T16:48:40Z |
| format | Article |
| id | doaj.art-3b41fee56e86425aa9da687abe6e3ab4 |
| institution | Directory Open Access Journal |
| issn | 2310-2861 |
| language | English |
| last_indexed | 2024-03-09T16:48:40Z |
| publishDate | 2023-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Gels |
| spelling | doaj.art-3b41fee56e86425aa9da687abe6e3ab42023-11-24T14:43:16ZengMDPI AGGels2310-28612023-10-0191185110.3390/gels9110851Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and ProbioticsSanjeevani Deshkar0Purva Yeole1Jayashri Mahore2Ankita Shinde3Prabhanjan Giram4Department of Pharmaceutics, Dr. D. Y. Patil Unitech Society’s, Dr. D. Y. Patil Institute of Pharmaceutical Science & Research, Pune 411018, IndiaDepartment of Pharmaceutics, Dr. D. Y. Patil Unitech Society’s, Dr. D. Y. Patil Institute of Pharmaceutical Science & Research, Pune 411018, IndiaDepartment of Pharmaceutics, Dr. D. Y. Patil Unitech Society’s, Dr. D. Y. Patil Institute of Pharmaceutical Science & Research, Pune 411018, IndiaDepartment of Pharmaceutics, Dr. D. Y. Patil Unitech Society’s, Dr. D. Y. Patil Institute of Pharmaceutical Science & Research, Pune 411018, IndiaDepartment of Pharmaceutics, Dr. D. Y. Patil Unitech Society’s, Dr. D. Y. Patil Institute of Pharmaceutical Science & Research, Pune 411018, IndiaWorldwide, 40 to 50% of women suffer from reproductive tract infections. Most of these infections are mixed infections, are recurrent and difficult to treat with antimicrobials or antifungals alone. For symptomatic relief of infections, oral antimicrobial therapy must be combined with topical therapy. The purpose of this work is to optimize and develop a polyelectrolyte complex (PEC) of chitosan/anion for the formulation of posaconazole- and probiotic-loaded vaginal hydrogel inserts with prolonged release and significant mucoadhesion. PECs were prepared using chitosan as cationic and carrageenan, pectin and polycarbophil as anionic polymers via a lyophilization technique. PEC formation was confirmed by scanning electron microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry, by observing changes in its surface, physical and thermal properties. The probiotic, <i>Lactobacillus casei</i>, was added to the PEC during the lyophilization process and the effect on the probiotic viability was studied. The PECs were further compressed along with posaconazole to form hydrogel inserts and optimized using a 3<sup>2</sup> full-factorial design. The hydrogel inserts were assessed for swelling behavior, drug release, in vitro mucoadhesion and in vitro antifungal activity. The chitosan–pectin hydrogel insert demonstrated excellent mucoadhesion (1.25 N), sustained drug release (88.2 ± 2.4% in 8 h) and a swelling index of 154.7%. The efficacy of hydrogel inserts was evaluated using in vitro study with a co-culture of <i>Lactobacillus casei</i> and <i>Candida albicans</i>. This study revealed an increase in <i>Lactobacilli casei</i> count and a significant drop in the viable count of <i>Candida albicans</i> (4-log reduction in 24 h), indicating the effectiveness of hydrogel inserts in alleviating the fungal infection. Overall, our study demonstrated the potential of the hydrogel insert for preventing vaginal infection and restoring normal vaginal microbiota.https://www.mdpi.com/2310-2861/9/11/851vaginal candidiasispolyelectrolyte complexhydrogel insertposaconazolechitosanprobiotic |
| spellingShingle | Sanjeevani Deshkar Purva Yeole Jayashri Mahore Ankita Shinde Prabhanjan Giram Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics Gels vaginal candidiasis polyelectrolyte complex hydrogel insert posaconazole chitosan probiotic |
| title | Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics |
| title_full | Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics |
| title_fullStr | Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics |
| title_full_unstemmed | Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics |
| title_short | Polyelectrolyte-Complex-Based Hydrogel Inserts for Vaginal Delivery of Posaconazole and Probiotics |
| title_sort | polyelectrolyte complex based hydrogel inserts for vaginal delivery of posaconazole and probiotics |
| topic | vaginal candidiasis polyelectrolyte complex hydrogel insert posaconazole chitosan probiotic |
| url | https://www.mdpi.com/2310-2861/9/11/851 |
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