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Formulation and In Vitro Evaluation of Mucoadhesive Sustained Release Gels of Phytoestrogen Diarylheptanoids from Curcuma comosa for Vaginal Delivery

Diarylheptanoids (DAs) characterized by a 1,7-diphenylheptane structural skeleton are considered a novel class of phytoestrogens. The DAs available in Curcuma comosa Roxb. (C. comosa) extract demonstrated significant estrogenic activities both in vitro and in vivo. This study aimed to develop and co...

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Autores principales: Limpongsa, Ekapol, Tabboon, Peera, Tuntiyasawasdikul, Sarunya, Sripanidkulchai, Bungorn, Pongjanyakul, Thaned, Jaipakdee, Napaphak
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9862155/
https://www.ncbi.nlm.nih.gov/pubmed/36678892
http://dx.doi.org/10.3390/pharmaceutics15010264
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author Limpongsa, Ekapol
Tabboon, Peera
Tuntiyasawasdikul, Sarunya
Sripanidkulchai, Bungorn
Pongjanyakul, Thaned
Jaipakdee, Napaphak
author_facet Limpongsa, Ekapol
Tabboon, Peera
Tuntiyasawasdikul, Sarunya
Sripanidkulchai, Bungorn
Pongjanyakul, Thaned
Jaipakdee, Napaphak
author_sort Limpongsa, Ekapol
collection PubMed
description Diarylheptanoids (DAs) characterized by a 1,7-diphenylheptane structural skeleton are considered a novel class of phytoestrogens. The DAs available in Curcuma comosa Roxb. (C. comosa) extract demonstrated significant estrogenic activities both in vitro and in vivo. This study aimed to develop and comprehensively evaluate a mucoadhesive vaginal gel for the sustained release of DAs. Different mucoadhesive polymers as gelling agents were investigated. C. comosa ethanolic crude extract was used as a source of DAs. All C. comosa gels were light brown homogeneous with pH within 4.4–4.6. Their flow behaviors were pseudoplastic with a flow behavior index of 0.18–0.38. The viscosity at a low shear rate varied from 6.2 to 335.4 Pa·s. Their mechanical and extrudability properties were associated well with rheological properties. Polycarbophil (PCP):hydroxypropyl methylcellulose (HPMC) blends had a higher mucoadhesiveness to porcine vaginal mucosa than those of PCP-based or HPMC-based gels. All C. comosa gels exhibited a sustained, zero-order DA release pattern over 72 h. Korsmeyer and Peppas equation fitting indicated a non-Fickian, case II transport release mechanism. C. comosa gels had good physical and chemical stability under low-temperature storage for up to 12 months. PCP:HPMC-based mucoadhesive gels could be a proper delivery system for vaginal administration of DAs.
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spelling pubmed-98621552023-01-22 Formulation and In Vitro Evaluation of Mucoadhesive Sustained Release Gels of Phytoestrogen Diarylheptanoids from Curcuma comosa for Vaginal Delivery Limpongsa, Ekapol Tabboon, Peera Tuntiyasawasdikul, Sarunya Sripanidkulchai, Bungorn Pongjanyakul, Thaned Jaipakdee, Napaphak Pharmaceutics Article Diarylheptanoids (DAs) characterized by a 1,7-diphenylheptane structural skeleton are considered a novel class of phytoestrogens. The DAs available in Curcuma comosa Roxb. (C. comosa) extract demonstrated significant estrogenic activities both in vitro and in vivo. This study aimed to develop and comprehensively evaluate a mucoadhesive vaginal gel for the sustained release of DAs. Different mucoadhesive polymers as gelling agents were investigated. C. comosa ethanolic crude extract was used as a source of DAs. All C. comosa gels were light brown homogeneous with pH within 4.4–4.6. Their flow behaviors were pseudoplastic with a flow behavior index of 0.18–0.38. The viscosity at a low shear rate varied from 6.2 to 335.4 Pa·s. Their mechanical and extrudability properties were associated well with rheological properties. Polycarbophil (PCP):hydroxypropyl methylcellulose (HPMC) blends had a higher mucoadhesiveness to porcine vaginal mucosa than those of PCP-based or HPMC-based gels. All C. comosa gels exhibited a sustained, zero-order DA release pattern over 72 h. Korsmeyer and Peppas equation fitting indicated a non-Fickian, case II transport release mechanism. C. comosa gels had good physical and chemical stability under low-temperature storage for up to 12 months. PCP:HPMC-based mucoadhesive gels could be a proper delivery system for vaginal administration of DAs. MDPI 2023-01-12 /pmc/articles/PMC9862155/ /pubmed/36678892 http://dx.doi.org/10.3390/pharmaceutics15010264 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Limpongsa, Ekapol
Tabboon, Peera
Tuntiyasawasdikul, Sarunya
Sripanidkulchai, Bungorn
Pongjanyakul, Thaned
Jaipakdee, Napaphak
Formulation and In Vitro Evaluation of Mucoadhesive Sustained Release Gels of Phytoestrogen Diarylheptanoids from Curcuma comosa for Vaginal Delivery
title Formulation and In Vitro Evaluation of Mucoadhesive Sustained Release Gels of Phytoestrogen Diarylheptanoids from Curcuma comosa for Vaginal Delivery
title_full Formulation and In Vitro Evaluation of Mucoadhesive Sustained Release Gels of Phytoestrogen Diarylheptanoids from Curcuma comosa for Vaginal Delivery
title_fullStr Formulation and In Vitro Evaluation of Mucoadhesive Sustained Release Gels of Phytoestrogen Diarylheptanoids from Curcuma comosa for Vaginal Delivery
title_full_unstemmed Formulation and In Vitro Evaluation of Mucoadhesive Sustained Release Gels of Phytoestrogen Diarylheptanoids from Curcuma comosa for Vaginal Delivery
title_short Formulation and In Vitro Evaluation of Mucoadhesive Sustained Release Gels of Phytoestrogen Diarylheptanoids from Curcuma comosa for Vaginal Delivery
title_sort formulation and in vitro evaluation of mucoadhesive sustained release gels of phytoestrogen diarylheptanoids from curcuma comosa for vaginal delivery
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9862155/
https://www.ncbi.nlm.nih.gov/pubmed/36678892
http://dx.doi.org/10.3390/pharmaceutics15010264
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