The Co-Encapsulated Antioxidant Nanoparticles of Ellagic Acid and Coenzyme Q<SUB>10</SUB> Ameliorates Hyperlipidemia in High Fat Diet Fed Rats

Abstract

Obesity is the major cause of type 2 diabetes with hyperlipidemia as one of its complications and antioxidants were found to be beneficial in such disease conditions. The present investigation is geared towards reduction of the dose required/improve the bioavailability of the combination of antioxidants, ellagic acid and coenzyme Q10 by co-encapsulating them into nanoparticles and study the possible synergism in ameliorating hyperlipidemia in high fat diet fed rats. The co-encapsulated particles at 10% (w/w of polymer) loading of ellagic acid and coenzyme Q10 have particle size of 260 nm. Male Sprague-Dawley (SD) rats on feeding high fat diet for over 4 weeks developed hyperlipidemia. The hyperlipidemic rats on 2 weeks post treatment with antioxidant combination administered as oral suspension or nanoparticles found to ameliorate the hyperlipidemic conditions and nanoparticles were found to be equally/more effective at 3 times lower dose in sustaining cholesterol lowering effect for extended periods, lowering glucose and triglycerides and in improving endothelial functioning, indicating the ability of the nanoparticles in improving efficacy of the duo. The results promise the potential of nanoparticles in improving the efficacy of ellagic acid and coenzyme Q10 in treating high fat diet induced hyperlipidemia in rats.

Strategies for oral delivery and mitochondrial targeting of CoQ10

“…A synergistic antioxidant combination of ellagic acid and CoQ10 coencapsulated in nanoparticles has been tested in hyperlipidemic rats. After a 2-weeks treatment, the combination lowered cholesterol, glucose and triglycerides levels for extended periods and improved endothelial functioning (Ratnam et al, 2009). NLC are considered a potential bioavailability enhancement tool (Gaba et al, 2014).…”

Functional benefits of PLGA particulates carrying VEGF and CoQ10 in an animal of myocardial ischemia

“…Even though a precise mechanism of action of CoQ 10 in MI is not known, in general it is attributed to its 13 antioxidant nature, ability to minimize inflammation, improve endothelium function (Dai et al, 2011;Lee et al, 2012). We have previously reported the efficacy of CoQNPs in other experimental models (Ankola et al, 2007;Ratnam et al, 2009) however a more systematic understanding is required on their therapeutic potential before much efforts are put in to prove the performance of these compounds that are in general high dose molecules and currently in use as supplements.…”

“…However, CoQ 10 is still seeking solutions to overcome poor oral bioavailability problems (Beg et al, 2010). Strategies to improve gastrointestinal absorption have been previously studied with proven success in several pathologies (Ankola et al, 2007;Ratnam et al, 2009). …”

Preparation and characterization of micronized ellagic acid using antisolvent precipitation for oral delivery

“…Meanwhile, the water solubility also increased (Kesisoglou and Mitra, 2012). Up to now, diverse nanotechnologies were used to prepare EA micro-or nanoparticulate systems including microspheres of EA (Jeong et al, 2001;Ogawa et al, 2002), pH dependent microassemblies of EA (Barnaby et al, 2011), amorphous solid dispersions of EA with cellulose ester , EA encapsulated chitosan nanoparticles (Arulmozhi et al, 2013a), poly(lactide-co-glycolide) (PLGA) and polycaprolactone (PCL) (Bala et al, 2005a;Sharma et al, 2007;Sonaje et al, 2007), co-encapsulated antioxidant nanoparticles of EA and coenzyme Q(10) (Ratnam et al, 2009). During above preparation processes of EA micro-or nanoparticulate systems, emulsion-diffusion-evaporation (Bala et al, 2005a;Sharma et al, 2007;Sonaje et al, 2007), spray drying , co-precipitation , rotary evaporation and ionic gelation (Arulmozhi et al, 2013a) methods were utilized.…”