SCREENING AND OPTIMIZATION OF VALACYCLOVIR NIOSOMES BY DESIGN OF EXPERIMENTS
DOI:
https://doi.org/10.22159/ijap.2018v10i1.22566Keywords:
Design of Experiments, Full factorial design, Niosomes, Optimization, ValacyclovirAbstract
Objective: The objective of the study was to perform a screening, optimization of valacyclovir niosomal formulation to achieve a sustained release of drug using the design of experiments by 32Â full factorial design.
Methods: Valacyclovir loaded niosomes were prepared using thin film hydration method by varying the ratio of Span 60 and Cholesterol. The prepared niosomes were evaluated for vesicle size, entrapment efficiency, cumulative drug release, fourier transformed infrared spectroscopy (FTIR), zeta potential and surface morphology by field emission scanning electron microscopy (FESEM).
Results: The valacyclovir was successfully encapsulated and its entrapment efficiency ranged from 36.70 % to 50.62 %. The average vesicle size of the niosomes was found to be 431 to 623 nm. At 8th hour the drug release varied from 77.50% to 96.31 %. The optimized niosomes were multilamellar with a surface charge potential of about-43.2 mV. The studies revealed that the interaction of cholesterol and surfactant had a substantial effect on vesicle size, entrapment efficiency and drug release from the niosomes. The release kinetics of the optimized niosomes followed zero order kinetics with fickian diffusion controlled mechanism. The stability studies were performed for the optimized formulation and found that the formulation is stable at 4°C ± 2°C.
Conclusion: Model equations were developed for the responses. No significant difference was observed between the predicted and observed value, showing that the developed model is reliable.
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Purnima Madhivanan, Karl Krupp, Arthur L Reingold. The epidemiology of Herpes simplex virus type-2 infection among married women in mysore, India. Sex Transm Dis 2007;34:935-7.
Alex Azwa, Simon E Barton. Aspects of herpes simplex virus: a clinical review. J Fam Plann Repod Healthcare 2009;35:237-42.
Cunningham AL, Diefenbach RJ, Miranda-Saksena M, Bosnjak L, Kim M, Jones C, Douglas MW. The cycle of human herpes simplex infection: virus transport and Immune control. J Infect Dis 2006;194:S11-S18.
Erlich KS. Management of herpes simplex and varicella-zoster viral infections. West J Med 1997;166:211-5.
Pradeep B, Nagamadhu M, David Banji, Shekar K, Bindu Madhavi B, Arjun G. Valacyclovir: development, treatment and pharmacokinetics. Int J Appl Biol Pharm 2010;3:1076-83.
Conan MacDougall, B Joseph Guglielmo. Pharmacokinetics of valaciclovir. J Antimicrob Chemother 2004;53:899-901.
David B Kimberlin. Acyclovir derivatives and other new antiviral agents. Semin Pediatr Infect Dis 2001;12:224-34.
Ganesh M, Narasimharao CV, Saravana Kumar A, Kamalakannan K, Vinoba M, Mahajan HS, Sivakumar T. UV spectrophotometric method for the estimation of Valacyclovir HCl in tablet dosage form. E J Chem 2009;6:814–8.
Rafik Karaman, Khuloud K Dajani, Alaa Qtait, Mustafa Khamis. Prodrugs of acyclovir–a computational approach. Chem Biol Drug Des 2012;79:819-34.
Jain NK. Advances in controlled and novel drug delivery. 1st ed. India: CBS Publishers and Distributors, New Delhi; 2004.
Saeid Moghassemi, Afra Hadjizadeh. Nano-niosomes as nanoscale drug delivery systems: an illustrated review. J Controlled Release 2014;191:82-9.
Ali Bhageri, Boon Seang Chu, Hariszun Yaakob. Niosomal drug delivery systems: formulation, preparation and applications. World Appl Sci J 2014;32:1671-85.
Gurinder Singh, Roopa S Pai, V Kusum Devi. Optimization of pellets containing solid dispersion prepared by extrusion/spheronization using central composite design and desirability function. J Young Pharm 2012;4:146-56.
Sonam Ranga, Manish Jaimini, Sanjay Kumar Sharma, Bhupendra Singh Chauhan, Amit Kumar. A review on the design of experiments (DoE). Int J Chem Pharm Sci 2014;3:216-24.
Chawda Himmat Singh, Jain CP, Bairwa Narendra Kumar. Formulation, characterization, stability and in vitro evaluation of nimesulide niosomes. Pharmacophore 2011;2:168–85.
Khalid M El-Say, Fathy I Abd-Allah, Ahmed E Lila, Abd El-Saboor A Hassan, Alaa Eldin A Kassem. Diacerin niosomal gel for topical delivery: development, in vitro and in vivo assessment. J Liposome Res 2015;26:57-67.
Mohawed Ola AM, El-Ashmoony MM, Omaima Elgazaerly. Niosome-encapsulated clomipramine for transdermal controlled delivery. Int J Pharm Pharm Sci 2014;6:567-75.
Mothilal M, Chaitanya M, Surya Teja SP, Manimaran V, Damodharan N. Formulation and evaluation of naproxen-eudragit RS100 nano suspension using 32 factorial design. Int J Pharm Pharm Sci 2014;6:449-55.
Purnima Negi, Farhan J Ahmad, Dabeer Ahmad, Gaurav K, Gyanendra Singh. Development of a novel formulation for transdermal delivery of an antidepressant drug. Int J Pharm Sci Res 2011;2:1766-71.
Gyati Shilakari Asthana, Abhay Asthana, Davinder Singh, Parveen Kumar Sharma. Etodolac containing topical niosomal gel: formulation development and evaluation. J Drug Delivery 2016;1-8. http://dx.doi.org/10.1155/2016/9324567
Balakrishnan P, Shanmugam S, Lee WS, Lee WM, Johg Oh Kim, Dong Hoon Oh, et al. Formulation and in vitro assessment of minoxidil niosomes for enhanced skin delivery. Int J Pharm 2009;377:1-8.
Tila D, Yazdani-arazi SN, Ghanbarzadeh S, Arami S. pH-sensitive, polymer modified, plasma stable niosomes : promising carriers for anti-cancer drugs. EXCLI J 2015;14:21–32.
Srinivas S, Anandkumar Y, Hemanth A, Anitha M. Preparation and evaluation of niosomes containing aceclofenac. Dig J Nanomater Biostruct 2010;5:249-54.
Di Marzio L, Marianecci C, Petrone M, Rinaldi F, Carafa M. Novel pH-sensitive non-ionic surfactant vesicles: Comparison between tween 21 and tween 20. Colloids Surf B 2011;82:18–24.
Suvakanta Dash, Padala Narasimha Murthy, Lilakanta Nath, Prasanta Chowdhury. Kinetic modelling on drug release from controlled drug delivery systems. Acta Poloniae Pharm Drug Res 2010;67:217-23.
Zerrin Sezgin, Bayindir, Nilufer Yuksel. Characterisation of niosomes prepared with various surfactants for paclitaxel oral delivery. J Pharm Sci 2010;99:2049-60.
Bhama Santhosh Kumar, Rakhi Krishna, Lakshmi PS, Deepa T Vasudev, Sreeja C Nair. Formulation and evaluation of niosomal suspension of cefixime. Asian J Pharm Clin Res 2016;10:194-201.
Salih OS, Samein LH, Ali WK. Formulation and in vitro evaluation of rosuvastatin calcium niosomes. Int J Pharm Pharm Sci 2013;5:525–35.
Kayes JB. Pharmaceutical suspensions: the relation between zeta potential, sedimentation volume and suspension stability. J Pharm Pharmacol 1997;29:199-204.
