Copyright © 2016 American Scientiﬁc Publishers All rights reserved Printed in the United States of America Article Advanced Science, Engineering and Medicine Vol. 8, 1–10, 2016 www.aspbs.com/asem Inﬂuence of Rutoside Loaded Solid Lipid Nanoparticles to Enhance Oral Bioavailability: Characterization, Pharmacokinetic, and Pharmacodynamic Studies Satyavani Kaliamurthi ∗ , Gurudeeban Selvaraj, Ramanathan Thirugnanasambandam, and Balasubramanian Thangavel Nanobiotechnology Division, Centre of Advanced Study in Marine Biology, Faculty of Marine Sciences, Annamalai University, Parangipettai 608502, Tamil Nadu, India Incorporation of miserable soluble metabolite into the suitable colloidal carrier is a great value in the treatment of metabolic disorders. Therefore, the present study rutoside has been encapsulated with palmitic acid, characterized and evaluated their pharmacokinetics and pharmacodynamic properties in diabetic rats. Yellowish-white rutoside and solid lipid matrix formulation 5 (1:8) showed monodis- perse 85 nm spherical and rod-shaped rutoside nanoparticles (RNP) with potential encapsulation efﬁciency (78%), zeta potential (−36.3 mV) and stability. Increased peak of serum concentration and decreased the volume of distribution (35.6 ± 3.4) observed in the kinetic proﬁle of nanoparti- cles. It indicated their potential bioavailability of the intestinal system. Treatment of RNP controls the hyperglycemic condition evidenced by changes in blood glucose, body weight, tissue exami- nation, lipid and kidney proﬁle compared with rutoside. This study concluded nano-encapsulated rutoside act as carrier system to enhance the bioavailability to develop nano based anti-diabetic agents. Keywords: Diabetes, Solid Lipid Nanoparticles, Rutoside, TEM, Hepatic Lobules. 1. INTRODUCTION The common dietary ﬂavonoid Rutoside showed antiviral, anti-inﬂammatory, antioxidative, antidiabetic, anticancer effects in animal models as well as human beings. 1–3 But it is not attracted by the researchers because of the following reasons such as, poor bioavailability and sta- bility i.e., absorbed more slowly in the gastrointestinal tract and digested very fast by cecal microﬂora before reaching the target site, serum distribution was high com- pared to quercetin, modulated some changes to the glu- cose transporter type four proteins, inhibit the formation of advanced glycation end products. 4 5 New class of colloidal carriers is solid lipid nanoparticles (SLNp) that are made from biodegradable lipids are suitable for incorporation of lipophilic, hydrophilic, and hydrophobic drugs within the lipid matrix in considerable communication. SLNp over polymeric nanoparticles is formulated from physiologically tolerated lipid components, which ∗ Author to whom correspondence should be addressed. decreases the potential for acute and chronic toxicity. 6 7 SLNp had been developed and investigated for Parenteral, pulmonary, and dermal application routes. 8 Lipid nanopar- ticles consisting of biodegradable lipids are suitable for incorporation of lipophilic, hydrophilic, and poorly water- soluble drugs within the lipid matrix in considerable communication. 9 In order to overcome the disadvantages associated with the liquid state of the oil droplets, the liq- uid replaced by a solid lipid, which eventually transformed into SLNp. The reasons for the increasing interest in a lipid-based system include small size, site-speciﬁc drug delivery by SLNp, controlled release of active drug over a long period, and protection of incorporated drug against the chemical degradation. 10 FDA approved the use of palmitic acid as the solid lipid matrix in drug discovery through it is an excellent mechanical strength, biocompatibility, and non-toxicity. 11 The solid-state of a palmitic acid permit more controlled drug releases through increased mass transfer resistance. 7 Type II diabetes is well known leading metabolic disorders Adv. Sci. Eng. Med. 2016, Vol. 8, No. xx 2164-6627/2016/8/001/010 doi:10.1166/asem.2016.1864 1