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that the % drug entrapment increases when concentration ® of polymer (Eudragit RLPO) increases and negative sign for coefficient of X 2 indicates that % drug entrapment of nanoparticles increases when concentration of stabilizer (Pluronic F 68) decreases. Validity of the above equations was verified by designing check point formulation (C). The particle size and % drug entrapment predicted from the equations derived and those observed from experimental results are summarized in Table No.3.The closeness of predicted and observed values for particle size and % drug entrapment indicates validity of derived equations for dependent variables. Response Surface Plots:Graphical presentation of the data can help to show the relationship between response and independent variables. Graphs gave information similar to that of the mathematical equations obtained from statistical analysis. The response surface graphs of particle size and % drug entrapment are presented in fig 3 and fig. 4 respectively. The response surface plots illustrated that as concentration ® of polymer (Eudragit RLPO) increases, the value of dependent variable, i.e. particle size increase and as concentration of stabilizer (Pluronic F 68) increases the value of dependent variable, i.e. particle size decreases. Similarly the response surface plots for % drug entrapment shows positive effects of independent variable, i.e. polymer ® concentration (Eudragit RLPO) and negative effect of other independent variable, i.e. concentration of stabilizer (Pluronic F 68). DSC gives information regarding the physical properties like crystalline or amorphous nature of the samples. The DSC thermogram of acyclovir (Fig 5a) shows an exothermic peak at 267.03° corresponding to its melting temperature , which was not detected in the thermograms for acyclovir loaded ® Eudragit RLPO nanoparticles (Fig 5b). It has been shown by a couple of authors that when the drug does not show its exothermic peak in the formed nanoparticles, it is said to be [20] in the amorphous state . Hence it could be concluded that ® in the prepared acyclovir loaded Eudragit RLPO nanoaprticles, the drug was present in the amorphous phase and may have been homogeneously dispersed in the polymer matrix. CONCLUSION ® U.V. Bhosale et al Preparation and In Vitro Evaluation of Acyclovir Loaded Eudragit RLPO Nanoparticles as Sustained Release Carriers ® Acyclovir loaded Eudragit RLPO nanoparticles were prepared by the nanoprecipitation method. The application of factorial design gave a statistically systematic approach 91 for the formulation of nanoparticles with desired particle size and high entrapment efficiency. Nanoparticles, with smallest particle size, up to 74 nm and highest drug entrapment efficiency, up to 74.5% has been achieved ® using Eudragit RLPO polymer with nanoprecipitation method. Drug: polymer ratio and concentration of surfactant were found to influence the particle size and ® entrapment efficiency of acyclovir loaded Eudragit RLPO nanoparticles. In vitro drug release study of factorial formulations showed release in 32 h in the range 67.928% to 97.957% . The release was found to follow first order release kinetics with non-Fickian diffusion mechanism for all batches except F6 where drug release follows first order release kinetics with case II diffusion mechanism.It is expected that these particulate nanodrug delivery systems will very well uptaken by Peyer's patches (PP) and disseminate systemically due to their particle size and polymer nature. These preliminary results indicate that ® acyclovir loaded Eudragit RLPO nanoparticles could be effective in sustaining drug release for a prolonged period. ACKNOWLEDGEMENT The authors express their thanks to M/S Ajanta Pharmaceuticals Ltd, Research and Development Division, Mumbai, and M/S Glenmark Pharmaceuticals Ltd Nashik, India,for providing ample supply of drug and polymers and Principal, Al-Ameen College of Pharmacy, Bangalore for providing the necessary facilities for the work. Authors thank All India Council for Technical Education (AICTE), New Delhi, India, for financial support through Research Promotion Scheme (RPS). REFERENCES 1. Tran T, Druce JD, Catton MC, Kelly H, Birch CJ. Changing epidemiology of genital herpes simplex virus infection in Melbourne, Australia, between 1980 and 2003. Sex Transm Infect 2004;80:277-79. 2. Emmert DH. Treatment of common cutaneous Herpes Simplex Virus Infections. Am Fam Physician 2000;61:1697- 704. 3. Wagstaff AG, Faulds D , Goa KL. Aciclovir: a reappraisal of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs 1994;47:153–205. 4. Ruhnese M, Sandstorm F, Andersson B. Treatment of recurrent genital herpes simplex infection with acyclovir. J Antimicrob Chemother 1985;16:621-8. 5. Fuertes I, Miranda A, Millan M, Caraballo I. Estimation of the percolation thersholds in acyclovir hydrophilic matrix tablets. Eur J Pharm Biopharm 2006;64:336–42. RJPS, Apr-Jun, 2011/ Vol 1/ Issue 1
® U.V. Bhosale et al Preparation and In Vitro Evaluation of Acyclovir Loaded Eudragit RLPO Nanoparticles as Sustained Release Carriers 6. 6.Jalon De EG, Blanco-Prieto MJ, Ygartua P , Santoyo S. Increased efficacy of acyclovir-loaded microparticles against herpes simplex virus type 1 in cell culture. Eur J Pharm Biopharm 2003;56:183-7. 7. Rossi S, Sandri G, Ferrari F, Bonferoni MC, Caramella C. Buccal delivery of acyclovir from .lms based on chitosan and polyacrylic acid. Pharm Dev Technol 2003;8:199–208. 8. O'Brien JJ, Campoli-Richards DM. Acyclovir: an upated review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs 1989;37:233–309. 9. Allemann E, Leroux JC, Gurny R. Polymeric nano- and microparticles for the oral delivery of peptides and peptidomimetics. Adv Drug Deliv Rev 1998;34:171-89. 10. Hans ML,Lowman AM. Biodegradable nanoparticles for drug delivery and targeting. Curr. Opin. Solid State Mater. Sci. 2002; 6:319-27 11. Smart JD, KellawayIW, Worthington HEC. An in-vitro investigation of mucosa-adhesive materials for use in controlled drug delivery. J Pharm Pharmacol 1984;36:295-9. 12. Kamath KR, Park K. In Encyclopedia of Pharmaceutical Technology, Ed.; Marcel Dekker, New York;1988,10, 133-64. 13. Fessi H, Puisieux F, Devissaguet JP, Ammoury N, Benita S. Nanocapsules deposition byinterfacial polymer deposition following solvent deplacement. Int J Pharm1989;55:R1–R4. 14. Raymond C Rowe, paul J Sheskey. Handbook of th Pharmaceutical Excipients 5 edition, Pharmaceutical Press, UK, 2006 pp 551-53 15. Fessi, H., Puisieux, F., Devissaguet, J.P., Ammoury, N., Benita, S.Nanocapsules deposition by interfacial polymer deposition following solvent deplacement. Int J Pharm 1989,55, R1– R4. 16. Freitas MN ,. Marchetti JM. Nimesulide PLA microspheres as a potential sustained release system for the treatment of inflammatory diseases. Int J Pharm, 2005;13:201-11 92 17. Esposito, E., Roncarati, R., Cortesi, R., Cervellati, F., & Nastruzzi, C. (2000) Production of eudragit microparticles by spray-drying technique: Influence of experimental parameters on morphological and dimensional characteristics. Pharm Dev Technol, 2000;5: 267–78. 18. Gohel M, Patel M, Amin A, Agarwal A, Dave R, Bariya N. Formulation design and optimization of mouth dissolve tablets of nimesulide using vacuum drying technique. AAPS PharmSciTech. 2004; 5(3). Article 36 19. Freitas MN ,. Marchetti JM. Nimesulide PLA microspheres as a potential sustained release system for the treatment of inflammatory diseases. Int J Pharm, 2005;13:201-11 20. Ashish K. Mehta, Yadav KS., Krutika K. Sawant Nimodipine loaded PLGA nanoparticles: formulation optimization using factorial design, characterization and in-vitro evaluation. Curr Drug Del, 2007; 4:185-93 21. Nixon, J. R. Release characterization of microcapsules. In F. Lim (Editor), Biomedical Applications of Microcapsulation. Boca Raton, FL: CRC Press;1983. P.1227 22. Costa P, Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci,2001;13:123-33. 23. Ritger PL, Peppas NA. A simple equation for description of solute release. I. Fickian and non-Fickian release from nonswellable devices in the form of slabs, spheres, cylinders or discs. J Controll Rele,1996;5:23-36. Address for Correspondence: U.V Bhosale, Department of Pharmaceutics, Al-Ameen College of Pharmacy Near Lalbagh Main Gate, Hosur Road, Bangalore - 560 027, Karnataka, India. E-mail: udaybhosale25@gmail.com RJPS, Apr-Jun, 2011/ Vol 1/ Issue 1
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R G U H S Dr. Divakar Goli Principa
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RGUHS Journal of Pharmaceutical Sci
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Dear Readers, Rajiv Gandhi Universi
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For the determination of surface pH
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S B Shirsand et al Design and Evalu
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The formulation BT containing hydro
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many safer and newer drug delivery
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Compressibility index: This was cal
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colouration indicating the absence
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Heat Flow Endo up (mW) 8 7 6 5 4 3
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cumulative drug release (% CDR) at
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evaluated six replicate injections
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A B S T R A C T RGUHS Journal of Ph
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pharmacokinetics and dynamics, 6 on
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Mahendra Kumar BJ et al Assessment
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stress. The ISO induced increase in
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SMB Asdaqet al Pharmacodynamic inte
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CONCLUSION In conclusion, combined
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