Omega-3 Fatty Acid Based Nanolipid Formulation of Atorvastatin for Treating Hyperlipidemia.

Revathy Sreedhar,Anil Kumar Bhaskaran Pillai,Vrinda Sasi Kumar,Sabitha Mangalathillam

doi:10.15171/apb.2019.031

Revathy Sreedhar, Anil Kumar Bhaskaran Pillai + Show 2 more

Open Access

https://doi.org/10.15171/apb.2019.031

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Abstract

Purpose: In the current study, attempts have been made to formulate an omega-3 fatty acid based nanostructured lipid carriers of atorvastatin (AT), for treating hyperlipidemia; and to evaluate their antihyperlipidemic activity using in vitro and in vivo studies. Methods: Omega-3 fatty acid based AT-loaded nanolipid carriers (NLC) were formulated by the melt emulsification ultrasonication technology. The prepared NLC consist of stearic acid (as solid lipid), omega-3 fatty acid (as liquid lipid), Tween 80, poloxamer 188 (surfactants) and soya-lecithin (co-surfactant). Results: AT loaded NLCs have a particle size of 74.76 ± 4.266 nm, a zeta potential value of -36.03 ± 1.504 mV and a high drug entrapment efficiency (EE) of 86.70 % ± 0.155. The release of AT from NLCs exhibited a sustained behaviour, which made it an ideal vehicle for drug delivery. MTT assay results indicated that NLCs are compatible with L929 (mouse fibroblast) cell lines. Anti-hyperlipidemic study showed a significant reduction in LDL and TG levels in serum with the orally administered Omega-3 fatty acid based AT loaded NLCs when compared to marketed formulation. Conclusion: The results demonstrated that the omega-3 fatty acid based NLC has the potential to be a promising nanomedicine for the treatment of hyperlipidemia.

Highlights

Hyperlipidemia has afflicted humankind since middle ages.[1,2] Hyperlipidemia is one of the major cardiovascular risk factors
The results demonstrated that the omega-3 fatty acid based nanolipid carriers (NLC) has the potential to be a promising nanomedicine for the treatment of hyperlipidemia
The reported advantage of NLC of improving the bioavailability of loaded drug was leveraged for preparing Omega-3 fatty acid based AT loaded NLC

Summary

Introduction

Hyperlipidemia has afflicted humankind since middle ages.[1,2] Hyperlipidemia is one of the major cardiovascular risk factors. The drugs involved in the treatment of hyperlipidemia are classified as follows; 3- hydroxy3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins), bile acid sequestrants (Resins), Activated lipoprotein lipase (fibric acid derivatives), drugs that inhibit lipolysis and triglyceride synthesis like Nicotinic acid and Omega 3 fatty acids. Among these classes of drugs, the most commonly used one is HMGCoA reductase inhibitors (statins). Pre-systemic clearance in gastrointestinal mucosa and P-gp efflux mechanism; the oral bioavailability of AT is only 12%.9,10 the current work is aimed to formulate a nanolipid carrier (NLC) of AT for oral delivery, which will improve its bioavailability.[11]

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Conclusion