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

• Main Authors: Ekapol Limpongsa (Author), Peera Tabboon (Author), Sarunya Tuntiyasawasdikul (Author), Bungorn Sripanidkulchai (Author), Thaned Pongjanyakul (Author), Napaphak Jaipakdee (Author)
• Format: Book
• Published: MDPI AG, 2023-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

Diarylheptanoids (DAs) characterized by a 1,7-diphenylheptane structural skeleton are considered a novel class of phytoestrogens. The DAs available in <i>Curcuma comosa</i> Roxb. (<i>C. comosa</i>) 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. <i>C. comosa</i> ethanolic crude extract was used as a source of DAs. All <i>C. comosa</i> 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 <i>C. comosa</i> 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. <i>C. comosa</i> 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.

Item Description

10.3390/pharmaceutics15010264
1999-4923