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Lecithin-gold hybrid nanocarriers as efficient and pH selective vehicles for oral delivery of diacerein-In-vitro and in-vivo study
- Source :
- Colloids and surfaces. B, Biointerfaces. 141
- Publication Year :
- 2015
-
Abstract
- We report the synthesis and evaluation of lecithin-gold hybrid nanocarriers for the oral delivery of drugs with improved pharmacokinetics, Au-drug interactive bioactivity and controlled drug releasing behavior at physiological pH inside human body. For this purpose, diacerein, a hydrophobic anti-arthritic drug, was loaded in lecithin NPs (LD NPs), which were further coated by Au NPs either by in-situ production of Au NPs on LD NPs or by employing pre-synthesized Au NPs. All LDAu NPs were found to release drug selectively at the physiological pH of 7.4 and showed 2.5 times increase in the oral bioavailability of diacerein. Pharmacological efficacy was significantly improved i.e., greater than the additive effect of diacerein and Au NPs alone. LDAu NPs started suppressing inflammation at first phase, whereas LD NPs showed activity in the second phase of inflammation. These results indicate the interaction of Au NPs with prostaglandins and histaminic mediators of first phase of carrageenan induced inflammation. Acute toxicity study showed no hepatic damage but the renal toxicity parameters were close to the upper safety limits. Toxicity parameters were dependent on surface engineering of LDAu NPs. Apart from enhancing the oral bioavailability of hydrophobic drugs and improving their anti-inflammatory activity, these hybrid nanocarriers may have potential applications in gold-based photothermal therapy and the tracing of inflammation at atherosclerotic and arthritic site.
- Subjects :
- inorganic chemicals
Metabolic Clearance Rate
education
Anti-Inflammatory Agents
Administration, Oral
Biological Availability
Metal Nanoparticles
Anthraquinones
02 engineering and technology
Pharmacology
010402 general chemistry
Kidney
01 natural sciences
Colloid and Surface Chemistry
Pharmacokinetics
In vivo
Lecithins
medicine
Animals
Edema
Colloids
Physical and Theoretical Chemistry
Diacerein
health care economics and organizations
Analysis of Variance
Drug Carriers
Chemistry
technology, industry, and agriculture
Extremities
Surfaces and Interfaces
General Medicine
respiratory system
Hydrogen-Ion Concentration
021001 nanoscience & nanotechnology
Acute toxicity
0104 chemical sciences
Bioavailability
Rats
Drug Liberation
Liver
Area Under Curve
Toxicity
Gold
Rabbits
Nanocarriers
0210 nano-technology
Drug carrier
Biotechnology
medicine.drug
Subjects
Details
- ISSN :
- 18734367
- Volume :
- 141
- Database :
- OpenAIRE
- Journal :
- Colloids and surfaces. B, Biointerfaces
- Accession number :
- edsair.doi.dedup.....abae868cd030315de19e38c3301a355c