Puerarin is a phytochemical with various pharmacological effects, but poor water solubility and low oral bioavailability limited usage of puerarin. The purpose of this study was to develop a new microemulsion (ME) based on phospholipid complex technique to improve the oral bioavailability of puerarin. Puerarin phospholipid complex (PPC) was prepared by a solvent evaporation method and was characterized by X-ray diffraction and infrared spectroscopy. Pseudo-ternary phase diagrams were constructed to investigate the effects of different oil on the emulsifying performance of the blank ME. Intestinal mucosal injury test was conducted to evaluate safety of PPC-ME, and no sign of damage on duodenum, jejunum and ileum of rats was observed using hematoxylin-eosin staining. In pharmacokinetic study of PPC-ME, a significantly greater C (1.33 µg/mL) was observed when compared to puerarin (C 0.55 µg/mL) or PPC (C 0.70 µg/mL); the relative oral bioavailability of PPC-ME was 3.16-fold higher than puerarin. In conclusion, the ME combined with the phospholipid complex technique was a promising strategy to enhance the oral bioavailability of puerarin.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1080/03639045.2018.1449856 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
The Critical Role of Polyphenols in Immunomodulation and Periodontal Regeneration.
Oral Dis
December 2024
State Key Laboratory of Oral Diseases & National Center for Stomatology & National Clinical Research Center for Oral Diseases & Department of Periodontics, West China Hospital of Stomatology, Sichuan University, Chengdu, Sichuan, China.
Objectives: Periodontitis, the main cause of tooth loss in adults, is a widespread oral disease characterized by chronic inflammation primarily triggered by periodontopathic bacterial infection. Polyphenols are a class of compounds extracted from herbs and diets, characterized by the presence of more than one phenol unit per molecule. Emerging evidence has revealed that polyphenols show significant effectiveness in ameliorating tissue destruction in periodontitis.
View Article and Find Full Text PDFpH-sensitive chitosan/sodium alginate/calcium chloride hydrogel beads for potential oral delivery of rice bran bioactive peptides.
Food Chem
December 2024
Molecular Nutrition Branch, National Engineering Research Center of Rice and By-product Deep Processing/College of Food Science and Engineering, Central South University of Forestry and Technology, Changsha, Hunan 410004, China. Electronic address:
Although rice bran active peptide (RBAP) has potent antioxidant properties, its practical applications have been limited by its low bioavailability. In this study, we hypothesized that pH-responsive hydrogels prepared from the ionic gelation between chitosan and alginate could be a promising delivery system of short-chain peptides, like RBAP, for protecting them from chemical degradation during digestion and improving their functionality. The hydrogel beads retained RBAP in the gastric environment due to strong interactions between two biopolymers and RBAP, followed by a sustained release of more than 70 % peptide in the intestinal condition, thus improving its gastrointestinal stability.
View Article and Find Full Text PDFComparison of Solid Self-Nanoemulsifying Systems and Surface-Coated Microspheres: Improving Oral Bioavailability of Niclosamide.
Int J Nanomedicine
December 2024
Department of Pharmaceutical Engineering, Dankook University, Cheonan, South Korea.
Purpose: This study aimed to develop a solid self-nanoemulsifying drug delivery system (SNEDDS) and surface-coated microspheres to improve the oral bioavailability of niclosamide.
Methods: A solubility screening study showed that liquid SNEDDS, prepared using an optimized volume ratio of corn oil, Cremophor RH40, and Tween 80 (20:24:56), formed nanoemulsions with the smallest droplet size. Niclosamide was incorporated into this liquid SNEDDS and spray-dried with calcium silicate to produce solid SNEDDS.
Enhancing leuprolide penetration through enterocytes via the ER-Golgi pathway using lipophilic complexation.
Eur J Pharm Biopharm
December 2024
School of Pharmaceutical Sciences, Beijing Advanced Innovation Center for Structural Biology, and Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology (Ministry of Education), Tsinghua University, Beijing 100084, PR China. Electronic address:
Oral delivery of peptide drugs remains one of the most formidable challenges in the frontier of pharmaceutical research. Peptide drugs typically suffer from exceptionally low oral bioavailability, primarily attributed to rigorous enzymatic degradation within the gastrointestinal (GI) tract, limited ability to traverse the enterocyte barrier, and significant first-pass hepatic metabolism. Absorption of peptide drugs via the lymphatic route could potentially bypass intracellular lysosome degradation and hepatic first-pass metabolism.
View Article and Find Full Text PDFIdentification of Novel Potential Herbal Drug Targets against Beta-Catenin in the Treatment of Oral Squamous Cell Carcinoma.
Asian Pac J Cancer Prev
December 2024
Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai, India.
Objective: The study aims to identify potential pharmacophore models for targeting beta-catenin, a crucial protein involved in the development of oral squamous cell carcinoma (OSCC), using a combination of herbal compounds and computational approaches.
Methods: Five natural compounds namely Quercetin, Lycopene, Ovatodiolide, Karsil, and Delphinidin were selected based on their reported activity against beta-catenin. Ligand characteristics were analyzed using SwissADME to evaluate drug-likeness, lipophilicity (logP), and bioavailability.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!