Fabrication of surfactant-stabilized nanosuspension of naringenin to surpass its poor physiochemical properties and low oral bioavailability
Autor: | Hitesh Kulhari, Ramakrishna Sistla, Mayank K. Singh, Halley Gora Ravuri, Anusha Gunukula, Deep Pooja |
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Rok vydání: | 2018 |
Předmět: |
Male
Administration Oral Biological Availability Pharmaceutical Science 02 engineering and technology Polyethylene glycol 030226 pharmacology & pharmacy Polyethylene Glycols Rats Sprague-Dawley Surface-Active Agents 03 medical and health sciences chemistry.chemical_compound Drug Delivery Systems 0302 clinical medicine Drug Stability Suspensions Pulmonary surfactant Pharmacokinetics Drug Discovery PEG ratio Animals Vitamin E Dissolution testing Particle Size Solubility Pharmacology Chromatography Chemistry 021001 nanoscience & nanotechnology Nanostructures Bioavailability Complementary and alternative medicine Flavanones Drug delivery Nanoparticles Molecular Medicine 0210 nano-technology |
Zdroj: | Phytomedicine. 40:48-54 |
ISSN: | 0944-7113 |
Popis: | Background Nanosuspension is a biphasic system consisting of native drug particles dispersed in an aqueous surfactant or polymeric solution with a particle size between 10 to 1000 nm. In contrast to other drug delivery systems, nanosuspension offer the unique advantage of increasing solubility of the native drug resulting into faster drug absorption and hence achieving faster maximum plasma concentration. Hypothesis/Purpose The present study aims to evaluate surfactants/polymer stabilized nanosuspensions of naringenin (NN), a phytomedicine, to surpass its poor physiochemical properties and low oral bioavailability. Study design Optimization and characterization (DLS, SEM, PXRD and DSC) of nanosuspensions followed by in-vitro drug dissolution studies and pharmacokinetic study in male Sprague–Dawley rats were performed. Methods Nanosuspensions were prepared by precipitation-ultrasonication method with varying concentrations of different surfactants and polymer such as sodium cholate (SC), sodium lauryl sulphate (SLS), poly ethylene glycol 4000 (PEG), polysorbate 80 (Tween® 80), poloxomer-188 and D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS or Vitamin E-TPGS). Results Nanosuspension prepared with 0.5% w/v d -α-Tocopherol polyethylene glycol 1000 succinate (TPNS) and 7.5 mg NN, showed the smallest size of 118.1 ± 2.7 nm. TPNS showed increase in drug dissolution in simulated gastric fluid pH 1.2 (SGF) and phosphate buffer pH 6.8 (PB). TPNS demonstrated an improved pharmacokinetic profile compared to pure NN resulting 2.14 and 3.76 folds increase in Cmax and AUC, respectively. In addition, TPNS were stable over a period of six months. Conclusion The developed formulation strategy of nanosuspension could be exploited to improve the solubility and bio-availability of poorly soluble NN and other phytomedicines. |
Databáze: | OpenAIRE |
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