full issue - Association of Biotechnology and Pharmacy
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Current Trends in <strong>Biotechnology</strong> <strong>and</strong> <strong>Pharmacy</strong>Vol. 5 (2) 1110-1122 April 2011. ISSN 0973-8916 (Print), 2230-7303 (Online)Formulation, Characterization <strong>and</strong> Pharmacokinetic Studies <strong>of</strong>Carvedilol NanoemulsionsKoteswari Poluri 1 , Ramakrishna Sistla 2 , Prabhakar Reddy Veerareddy *3 ,Lakshmi M. Narasu 4 , Amol A Raje 5 <strong>and</strong> Sunder M. Hebsiba 51S. N. Vanitha <strong>Pharmacy</strong> Maha Vidyalaya, Nampally Exhibition Grounds, Hyderabad, A.P, India2Indian Institute <strong>of</strong> Chemical Technology, Tarnaka, Hyderabad, A.P, India3St. Peter’s Institute <strong>of</strong> Pharmaceutical Sciences, Hanamkonda, Warangal, A.P, India4Centre for Biotechnoloy, Jawaharlal Nehru Technological Unviersity, Hyderabad, A.P, India5Vimta labs Ltd., 5, S.P.Biotech Park, Shameerpet, Hyderabad, A.P, India*For Correspondence - vpreddyindia@yahoo.com1110AbstractThe present study involves the formulation<strong>and</strong> evaluation <strong>of</strong> oral o/w nanoemulsions (NE)with two simple edible oils, avoiding the largequantities <strong>of</strong> surfactants <strong>and</strong> co-surfactants whichwere prepared by high energy emulsificationtechnique. The particle size, polydispersity index(PDI), <strong>and</strong> zeta potential <strong>of</strong> prepared nanoemulsions were determined by using zeta sizer<strong>and</strong> were found to be in the range <strong>of</strong> 33.4±3.9nm, to 183.56±1.78nm, 0.051±0.04 to 0.38±0.06<strong>and</strong> -2.87±0.65 to -14.2±0.72 mv respectively.Centrifugation, freeze-thaw cycling, storage at4°C for 60days, X-ray diffraction (XRD) <strong>and</strong>Transmission electron microscopy (TEM) studiesrevealed the physical <strong>and</strong> chemical stability <strong>of</strong>the NEs. Entrapment efficiency <strong>and</strong> in-vitrorelease studies showed successful incorporation<strong>of</strong> carvedilol into NE with high drug loadingefficiency <strong>and</strong> good stability. Comparativepharmacokinetic studies <strong>of</strong> NE <strong>and</strong> marketeddosage form in male SD rats revealed a significantincrease in oral bio availability in NEs.Key words: Nano emulsions, Sesame oil, Oliveoil, Carvedilol, Sonication, LC-MS/MSIntroductionNano technology has emerged as one <strong>of</strong>the very promising fields <strong>of</strong> biomedical researchin the last few decades. Nano technology basedhealth care products will expected to reach 2trillion dollars target by the year 2015(1). Nanoemulsion technology is one <strong>of</strong> the segments <strong>of</strong>nano technology market <strong>and</strong> can be defined asthermodynamically stable, transparent ortranslucent dispersions <strong>of</strong> oil <strong>and</strong> water having asize range <strong>of</strong> 50-200 nm (2).Different types <strong>of</strong> oils <strong>and</strong> components canbe used for the preparation <strong>of</strong> NEs to impartspecific properties such as crossing different types<strong>of</strong> biological barriers like blood brain barrier uponadministration (3). NEs can also be used asexcellent vehicles in pharmaceutical field for theparenteral, oral <strong>and</strong> ocular or transdermal delivery<strong>of</strong> poorly permeable lipophilic drugs. Because <strong>of</strong>these unique properties, nano emulsions aregaining more importance as potential vehicles forthe efficient delivery <strong>of</strong> lipophilic drug molecules(3, 4, 5).Cardiovascular diseases includinghypertension are one <strong>of</strong> the major causes <strong>of</strong>mortality in the world. Delivery <strong>of</strong> therapeuticagents to cardiac organelles has the potential toincrease the efficiency <strong>of</strong> treatment protocols forheart failure. However, cardiac cells presentspecial problems to the delivery <strong>of</strong> drugs, <strong>and</strong> thenumber <strong>of</strong> papers reported in this area is also avery few (6). Carvedilol was selected for thepresent study. It is a non selective beta adrenergicFormulation, characterization <strong>and</strong> Pharmacokinetic studies