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.
Objective: Semen cryopreservation is an effective method of preserving genetic material, particularly in native chicken breeds facing a substantial decline. In this study, we evaluated the quality of frozen/thawed rooster semen treated with different concentrations of oral administrations of black ginger (Kaempferia parviflora: KP) extract and determined its fertility.Methods: Thirty-two Thai native roosters (Pradu Hang Dum, 42 weeks old) were used in this study. The treatments were classified into four groups according to the concentration of KP extract administered to the roosters: 0, 100, 150, and 200 mg/kg body weight. The quality of fresh semen was analyzed before cryopreservation. Post-thaw sperm quality and fertility potential were determined. Also, lipid peroxidation was determined.Results: The results showed that sperm concentration and movement increased in roosters treated with 200 mg/kg of KP extract (p0.05). The highest MDA levels were observed in the control group (p<0.05). The percentage of motile sperm (total motility and progressive motility) after semen thawing was higher in roosters that received 150 and 200 mg/kg KP extract than in those that received 100 mg/kg KP extract and the control (p<0.05). MDA levels decreased significantly in roosters that received 150 and 200 mg/kg KP extract than in those that received 100 mg/kg KP extract and the control (p<0.05). Fertility and hatchability were greater in the KP150 and KP200 groups than in the KP100 and control groups (p<0.05).Conclusion: The optimal amount of KP extract influencing initial sperm quality was determined to be 200 mg/kg. However, 150 mg/kg was the optimal low dosage of KP extract administration that maintained sperm quality and fertility following semen cryopreservation.
8 July 2024 in Journal of Drug Delivery Science and Technology
Background/Objectives: Andrographolide (AG), the primary diterpene of Andrographis paniculata, is classified as a BCS Class II substance, with its dissolution known to be restricted and inconsistent across various Andrographis extracts and formulations. This study aimed to implement liquisolid (LS) technology to enhance and reduce source-dependent variability in the dissolution of AG from Andrographis paniculata extracts (APEs). Methods: Ethanolic APEs from three distinct sources in Thailand were obtained using Soxhlet extraction. The AG content in the APEs varied between 14.9 and 24.1%. LS powders of APEs and pure AG were fabricated using microcrystalline cellulose and colloidal silicon dioxide as the carriers and coating materials. Their FTIR, PXRD, and SEM characteristics, flowability, and AG content were investigated. Results: All LS formulations exhibited good flowability and assay consistency. FTIR studies suggested intermolecular interactions between the α,β-unsaturated lactone ring of AG and the liquid vehicle. PXRD and SEM studies revealed the non-crystalline state of AG in LS powder, regardless of the AG source. All LS powders, regardless of the AG source, exhibited improved and similar dissolution profiles, with a similarity factor >51 under both sink and non-sink conditions. Preliminary stability assessments demonstrated that all formulated LS powders exhibited no marked physical changes over three months, regardless of the storage conditions. The percentage of AG remaining was significantly affected by storage temperature. Only LS powders stored under refrigerated conditions maintained dissolution patterns similar to those of fresh samples. Conclusions: This study offers foundational insights into LS strategies aimed at improving and reducing the source-dependent variability of herbal-extract powders.