DESIGN AND CHARACTERISATION OF ROSUVASTATIN CALCIUM NANOSPONGE USING A NATURAL POLYMER  

 Bharathi, M.^1*, Rajalingam, D.¹ Mariyam Bee, A.J.¹, Muralikrishnan Dhanasekaran²,

Reeta Vijaya Rani, K³, Mullaicharam Bhupathyraaj⁴, Brito Raj, S⁵

 ¹Department of Pharmaceutics, Kamalakshi Pandurangan college of Pharmacy, Thiruvannamalai-03, India.

²Department of Drug Discovery and Development, Harrison College of Pharmacy, Auburn University, Auburn, AL, 36849, USA.

³Department of Pharmaceutics, Surya School of Pharmacy, Surya Group of Institutions, Vikravandi, Villupuram, Tamilnadu, India

⁴College of Pharmacy, National University of Science and Technology, Muscat, Oman.

⁵Department of Pharmaceutics, Chettinad School of Pharmaceutical Sciences,  Chennai, India.

ABSTRACT: 

Background: As per the latest monitoring of advances in noncommunicable diseases (NCDs) published by the World Health Organization (WHO), NCDs are the leading reason for global mortality (70%).  NCDs share common risk factors, including biological intermediaries such as hyperlipidemias which comprise a set of alterations in blood lipid levels secondary to genetic factors or lifestyles.  Hyperlipidemia (elevated lipids content in the blood), specifically elevated LDL, is one of the most prevalent risk factors associated with the etiology and pathogenesis of atherosclerosis and ensuing vascular disorders.  Rosuvastatin calcium (ROSCa) is the most effective antilipidemic drug.  However, ROSCa is a poorly water-soluble drug with only 20% oral bioavailability.  The poor solubility of ROSCa affects its dissolution rate and, in turn, its bioavailability.  Therefore, effectively enhancing the dissolution of ROSCa can improve its oral bioavailability.   Accordingly, several nanosization approaches were adopted to enhance ROSCa dissolution and bioavailability.

Objective: present study was intended to design and formulate a novel controlled-release ROSCa Nanosponge for oral delivery using natural polymers that can increase its bioavailability and release the drug in a sustained and controlled manner.  

Methods: The ROSCa Nanosponge was prepared by emulsion solvent diffusion method using different drug-polymer ratios. The present study used natural polymers from tamarind seed powder, Hibiscus rosa sinensis, Fenugreek seed powder, and Urad dal powder with agar (surfactant).  The obtained Nanosponge was evaluated for various physiochemical parameters like FT-IR, Entrapment efficiency, Zeta potential, Polydispersity index, actual drug content, in vitro drug release, and Release kinetic model.  Particle size analysis and surface morphology of Nanosponge were also performed.

Results: The emulsion solvent diffusion method is the best method for preparing Nanosponge and releasing the drug in a sustained and controlled manner. The scanning electron microscopy of Nanosponge revealed the spherical shape and spongy nature of the formulations.  Among the twelve formulations, F6 and F7 exhibited the best and optimal pharmacokinetic parameters.

Discussion: The current results validated the new and novel ROSCa Nanosponge formulation as a possible alternative drug delivery system.  Compared to conventional formulations, ROSCa Nanosponge formulation has significantly enhanced bioavailability.   

Keywords: Rosuvastatin calcium, Tamarind seed, Hibiscus rosa sinensis, Urad dal, Fenugreek seed.