Phytoecdysteroids are active natural compounds that have demonstrated many beneficial pharmacological effects on mammals, including Humans. 20-Hydroxyecdysone (20E) is the major phytoecdysteroid present in plants, and gerbils are particularly good responders to the addition of 20E to their diet. We have examined the oral bioavailability of 20E in the desert gerbil, Gerbillus tarabuli. 20E (5 and 50 mg.kg body weight) was administered to gerbils by intra-peritoneal injection and oral gavage, respectively. Plasma samples were collected over 8 h and analyzed by HPLC-MS/MS to determine the 20E concentrations. The calculated oral bioavailability of 20E is approx. 12%, with a half-life of 30.6 and 33 min after per os administration or intra-peritoneal injection, respectively. This bioavailabilitty is much higher than that observed in laboratory rodents (ca. 1%). It is proposed that this unexpectedly high oral bioavailability of 20E in gerbils contributes to its high efficacy in this animal.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.steroids.2023.109262 | DOI Listing |
Bioorg Chem
December 2024
Pharmacology Division, CSIR- Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address:
Ursolic acid (3-hydroxy-urs-12-ene-28-oic acid, UA) is a pentacyclic triterpene present in numerous plants, fruits and herbs and exhibits various pharmacological effects. However, UA has limited clinical applicability since it is classified as BCS class IV molecule, characterized by low solubility, low oral bioavailability and low permeability. In the present study, UA was isolated from the biomass marc of Lavandula angustifolia and was structurally modified by an induction of indole ring at the C-3 position and amide group at the C-17 position with the aim to enhance its pharmacological potential.
View Article and Find Full Text PDFJ Chromatogr B Analyt Technol Biomed Life Sci
December 2024
Department of Pharmaceutical Analysis, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China. Electronic address:
Gemcitabine (GEM) has been extensively applied in treating various solid tumors. Nonetheless, GEM is easily metabolized in vivo by cytidine deaminase (CDA) to inactive 2', 2'-Difluorodeoxyuridine (dFdU) results in a low oral bioavailability, which limit its clinical application. It was found that Cedazuridine (CDZ) could effectively inhibit the deamination of the drug by CDA, and its combination with GEM might affect the oral bioavailability of GEM.
View Article and Find Full Text PDFPharm Dev Technol
January 2025
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Madhavnagar, Manipal - 576104, Karnataka, India.
Purpose: Supersaturated formulations have been widely explored for improving the oral bioavailability of drugs by using mesoporous silica (MS) to generate supersaturation via molecular adsorption; however, this is followed by precipitation. Several precipitation inhibitors (PI) have been explored to prevent precipitation and maintain the drug in solution for a longer period. However, the combined approach of MS and PIs, the impact of MS and Silica, and the loading of high-molecular-weight neutral molecules such as Cyclosporine A (CsA) have not yet been explored.
View Article and Find Full Text PDFJ Drug Target
January 2025
Department of Pharmaceutics, Yenepoya Pharmacy College & Research Centre, Yenepoya (Deemed to be University), Mangalore, Karnataka, 575018, India.
Breast cancer (BC) is a substantial reason for cancer-related mortality among women across the globe. Anastrozole (ANS) is an effective orally administered hormonal therapy for estrogen+ (ER+) BC treatment. However, several side effects and pharmacokinetic limitations restricted its uses in BC treatment.
View Article and Find Full Text PDFDrug Deliv Transl Res
January 2025
School of Agricultural Science and Engineering, Liaocheng University, Liaocheng, 252059, China.
Erastin, as an effective ferroptosis inducer, has received extensive attention in anti-tumor research. To develop an oral nanocarrier for high efficient loading hydrophobic erastin, here we prepared a fluoro-liposome (FA-3 F-LS) by the self-assembly of the folic acid modified fluorinated amphiphiles-FA-3 F conjugates. The hydrophobic component of three perfluorooctyl chains endows the FA-3 F-LSs with high stability to resist the harsh gastrointestinal tract condition.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!