Enhancing the Intestinal Permeation of the Chondroprotective Nutraceuticals Glucosamine Sulphate and Chondroitin Sulphate Using Conventional and Modified Liposomes
| Autor: | Ahmed Badr Eldin, Ahmed M. Agiba, Maha Nasr, Ahmed S. Geneidi, Sameh Abdel-Hamid |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Pharmaceutical Science
02 engineering and technology Cetylpyridinium chloride 030226 pharmacology & pharmacy Permeability 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Intestinal mucosa Glucosamine Intestine Small Osteoarthritis Zeta potential medicine Animals Particle Size Liposome Chromatography Viscosity Chondroitin Sulfates Permeation 021001 nanoscience & nanotechnology Bioavailability chemistry Dietary Supplements Liposomes Poloxamer 407 Rabbits 0210 nano-technology Deoxycholic Acid medicine.drug |
| Zdroj: | Current Drug Delivery. 15:907-916 |
| ISSN: | 1567-2018 |
| DOI: | 10.2174/1567201815666180123100148 |
| Popis: | Background Liposomes are promising systems for the delivery of macromolecules and poorly absorbed drugs, owing to their ability to compartmentalize drugs, their biodegradability and biocompatibility. Objective The aim of the present study was to formulate and evaluate conventional and modified glucosamine sulphate (GluS) and chondroitin sulphate (CS) liposomal formulations, to enhance their oral permeation for the treatment of osteoarthritis (OA). Method Liposomal formulations were prepared by the thin-film hydration method using two types of phospholipids; Epikuron 200© and Epikuron 200© SH, and three permeation enhancers; poloxamer 407, cetylpyridinium chloride, and sodium deoxycholate. In-vitro characterization of liposomal formulations was conducted in terms of entrapment efficiency, particle size, zeta potential, viscosity, physical stability and mucoadhesive strength. Surface morphology and vesicle shape, ex-vivo intestinal permeation, and histopathological studies were further carried out on the selected formulation. Results Results showed that the liposomal formulation containing sodium deoxycholate was the most optimum formula, showing high entrapment efficiency (60.11% for GluS and 64.10% for CS) with a particle size of 4.40 µm, zeta potential of -17.2 mV and viscosity of 2.50 cP. Conclusion The aforementioned formula displayed the highest cumulative % permeated of GluS and CS through rabbit intestinal mucosa compared to the solution of drugs and other liposomal formulations (64.20% for GluS and 78.21% for CS) after 2 hours. There were no histopathological alterations in the intestinal tissue, suggesting the safety of the utilized liposomal formulation. In light of the above, liposomes can be considered promising oral permeation-enhancer system for GluS and CS, which is worthy of future bioavailability experimentation. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|