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Nanoscience & Nanotechnology-Asia

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ISSN (Print): 2210-6812
ISSN (Online): 2210-6820

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Research Article

Development and Characterization of Oral Nanosuspension Using Esomeprazole Magnesium Trihydrate

Author(s): Surya Goel*, Vijay Agarwal and Monika Sachdeva

Volume 10, Issue 6, 2020

Page: [909 - 917] Pages: 9

DOI: 10.2174/2210681209666191111113850

Price: $65

Abstract

Background: Nanosuspension has arisen as a lucrative, remunerative, as well as a potent approach to improve the solubility and dissolution rate of poorly soluble drug entities. Several challenges are still present in this technology which need more research.

Objective: The prime aim of this research work is to develop, optimize and characterize the oral nanosuspension using esomeprazole magnesium trihydrate as a drug candidate.

Methods: The drug nanosuspensions were prepared using both approaches; Top-down and Bottom-up as the combinational approach. Poloxamer 188 was used as a stabilizer in this study. All the important formulation variables, like concentration of stabilizers that may influence characteristics of the nanosuspensions, were optimized. Formulation screening was performed using the optimization process, and the optimized nanosuspension was evaluated for its particle size, polydispersity index, zeta potential, shape, in vitro drug release and stability.

Results: For optimization of drug nanosuspension, the effect of Poloxamer 188 concentration and esomeprazole concentration was investigated and the optimal values were 0.3% w/v and 4 mg/ml, respectively. The particle size of nanosuspensions was in the range of 185 to 1048 nm with varying the zeta potential values from -11.2 to -27.5 mV. The in vitro dissolution rate of esomeprazole was increased up to 3-folds, approximately (92% in 90 min) as compared with crude esomeprazole drug (31% in 90 min) due to the decrease in particle size.

Conclusion: The result indicated that the combination of top-down and bottom-up approach used for preparing the oral nanosuspension is a suitable approach for poorly aqueous soluble drug moieties like esomeprazole magnesium.

Keywords: Esomeprazole magnesium, nanosuspension, particle size, drug, formulation, nanosuspension technology.

Graphical Abstract

[1]
Lenhardt, T.; Vergnault, G.; Grenier, P.; Scherer, D.; Langguth, P. Evaluation of nanosuspensions for absorption enhancement of poorly soluble drugs: In vitro transport studies across intestinal epithelial monolayers. AAPS J., 2008, 10(3), 435-438.
[http://dx.doi.org/10.1208/s12248-008-9050-7] [PMID: 18690542]
[2]
Arunkumar, N.; Deecaraman, M.; Rani, C. Nanosuspension technology and its applications in drug delivery. Asian J. Pharm., 2009, 3, 168-173.
[http://dx.doi.org/10.4103/0973-8398.56293]
[3]
Fasinu, P.; Pillay, V.; Ndesendo, V.M.; du Toit, L.C.; Choonara, Y.E. Diverse approaches for the enhancement of oral drug bio-availability. Biopharm. Drug Dispos., 2011, 32(4), 185-209.
[http://dx.doi.org/10.1002/bdd.750] [PMID: 21480294]
[4]
Nakarani, M.; Misra, A.K.; Patel, J.K.; Vaghani, S.S. Itraconazole nanosuspension for oral delivery: Formulation, characterization and in vitro comparison with marketed formulation. Daru, 2010, 18(2), 84-90.
[PMID: 22615599]
[5]
Pawar, R.N.; Chavan, S.N.; Menon, M.D. Development, characterization and evaluation of tinidazole nanosuspension for treatment of amoebiasis. J. Nanomed. Nanotechnol., 2016, 7(6), 1-4.
[6]
Pawar, R.N.; Chavan, S.N.; Menon, M.D. Development, characterization and evaluation of tinidazole nanosuspension for treatment of amoebiasis. J. Nanomed. Nanotechnol., 2016, 7(6), 1-4.
[7]
Kreuter, J. Colloidal drug delivery systems; Kreuter, J., Ed.; Marcel Dekker, Inc: New York, 1994.
[8]
Nagare, S.K. A review on Nanosuspension: An innovative acceptable approach in novel delivery system. Univ. J. Pharm., 2012, 1(1), 19-31.
[9]
Debjit, B. Nanosuspension–A novel approaches in drug delivery system. Pharm. Innov. J., 2012, 1(12), 50-63.
[10]
Kamble, V.A. Nanosuspension: A novel drug delivery system. Int. J. Pharma Bio Sci., 2010, 1, 352-360.
[11]
Soni, S. Nanosuspension: An approach to enhance solubility of drugs. IJPI. J. Pharm. Cos., 2012, 2(9), 50-63.
[12]
Wagh, K.S.; Patil, S.K.; Akarte, A.K. Nanosuspension-A new approach of bioavailability enhancement. Int. J. Pharm. Sci. Rev. Res., 2011, 8, 61-65.
[13]
Geetha, G.; Poojitha, U.; Khan, U. Various techniques for preparation of nanosuspension- A review. Int. J. Pharm. Res. Rev., 2014, 3, 30-37.
[14]
Li, X.S.; Wang, J.X.; Shen, Z.G.; Zhang, P.Y.; Chen, J.F.; Yun, J. Preparation of uniform prednisolone microcrystals by a controlled microprecipitation method. Int. J. Pharm., 2007, 342(1-2), 26-32.
[http://dx.doi.org/10.1016/j.ijpharm.2007.04.025] [PMID: 17566675]
[15]
Zhang, X.; Xia, Q.; Gu, N. Preparation of all-trans retinoic acid nanosuspensions using a modified precipitation method. Drug Dev. Ind. Pharm., 2006, 32(7), 857-863.
[http://dx.doi.org/10.1080/03639040500534184] [PMID: 16908423]
[16]
Brough, C.; Williams, R.O., III Amorphous solid dispersions and nano-crystal technologies for poorly water-soluble drug delivery. Int. J. Pharm., 2013, 453(1), 157-166.
[http://dx.doi.org/10.1016/j.ijpharm.2013.05.061] [PMID: 23751341]
[17]
Borhade, V.; Pathak, S.; Sharma, S.; Patravale, V. Formulation and characterization of atovaquone nanosuspension for improved oral delivery in the treatment of malaria. Nanomedicine (Lond.), 2014, 9(5), 649-666.
[http://dx.doi.org/10.2217/nnm.13.61] [PMID: 23927590]
[18]
Merisko-Liversidge, E.; Liversidge, G.G. Nanosizing for oral and parenteral drug delivery: A perspective on formulating poorly-water soluble compounds using wet media milling technology. Adv. Drug Deliv. Rev., 2011, 63(6), 427-440.
[http://dx.doi.org/10.1016/j.addr.2010.12.007] [PMID: 21223990]
[19]
Kassem, M.A.; Abdel Rahman, A.A.; Ghorab, M.M.; Ahmed, M.B.; Khalil, R.M. Nanosuspension as an ophthalmic delivery system for certain glucocorticoid drugs. Int. J. Pharm., 2007, 340(1-2), 126-133.
[http://dx.doi.org/10.1016/j.ijpharm.2007.03.011] [PMID: 17600645]
[20]
Patel, G.V.; Patel, V.B.; Pathak, A.; Rajput, S.J. Nanosuspension of efavirenz for improved oral bioavailability: Formulation optimization, in vitro, in situ and in vivo evaluation. Drug Dev. Ind. Pharm., 2014, 40(1), 80-91.
[http://dx.doi.org/10.3109/03639045.2012.746362] [PMID: 23323843]
[21]
Yadollahi, R.; Vasilev, K.; Simovic, S. Nanosuspension technologies for delivery of poorly soluble drugs. J. Nanomater., 2015, 2015, 1-13.
[http://dx.doi.org/10.1155/2015/216375]
[22]
Patel, V.R.; Agrawal, Y.K. Nanosuspension: An approach to enhance solubility of drugs. J. Adv. Pharm. Technol. Res., 2011, 2(2), 81-87.
[http://dx.doi.org/10.4103/2231-4040.82950] [PMID: 22171298]
[23]
Sudhakar, B. NagaJyothi, K.; Murthy, K.V.R. Nanosuspensions as a versatile carrier based drug delivery systems-an overview. Curr. Drug Deliv., 2014, 11, 299-305.
[http://dx.doi.org/10.2174/1567201811666140323131342] [PMID: 24655052]
[24]
Wang, Y.; Zheng, Y.; Zhang, L.; Wang, Q.; Zhang, D. Stability of nanosuspensions in drug delivery. J. Control. Release, 2013, 172(3), 1126-1141.
[http://dx.doi.org/10.1016/j.jconrel.2013.08.006] [PMID: 23954372]
[25]
Chingunpitak, J.; Puttipipatkhachorn, S.; Chavalitshewinkoon-Petmitr, P.; Tozuka, Y.; Moribe, K.; Yamamoto, K. Formation, physical stability and in vitro antimalarial activity of dihydroartemisinin nanosuspensions obtained by co-grinding method. Drug Dev. Ind. Pharm., 2008, 34(3), 314-322.
[http://dx.doi.org/10.1080/03639040701662388] [PMID: 18363147]
[26]
Muller, R.H.; Peter, K. Nanosuspensions for the formulation of poorly soluble drugs: Preparation by a size-reduction technique. Int. J. Pharm., 1998, 160, 229-237.
[http://dx.doi.org/10.1016/S0378-5173(97)00311-6]
[27]
Zhang, D.; Tan, T.; Gao, L.; Zhao, W.; Wang, P. Preparation of azithromycin nanosuspensions by high pressure homogenization and its physicochemical characteristics studies. Drug Dev. Ind. Pharm., 2007, 33(5), 569-575.
[http://dx.doi.org/10.1080/03639040600975147] [PMID: 17520449]
[28]
Möschwitzer, J.; Achleitner, G.; Pomper, H.; Müller, R.H. Development of an intravenously injectable chemically stable aqueous omeprazole formulation using nanosuspension technology. Eur. J. Pharm. Biopharm., 2004, 58(3), 615-619.
[http://dx.doi.org/10.1016/j.ejpb.2004.03.022] [PMID: 15451536]
[29]
Xiong, R.; Lu, W.; Li, J.; Wang, P.; Xu, R.; Chen, T. Preparation and characterization of intravenously injectable nimodipine nanosuspension. Int. J. Pharm., 2008, 350(1-2), 338-343.
[http://dx.doi.org/10.1016/j.ijpharm.2007.08.036] [PMID: 17920794]
[30]
Van Eerdenbrugh, B.; Van den Mooter, G.; Augustijns, P. Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products. Int. J. Pharm., 2008, 364(1), 64-75.
[http://dx.doi.org/10.1016/j.ijpharm.2008.07.023] [PMID: 18721869]
[31]
Krause, K.P.; Kayser, O.; Mäder, K.; Gust, R.; Müller, R.H. Heavy metal contamination of nanosuspensions produced by high-pressure homogenisation. Int. J. Pharm., 2000, 196(2), 169-172.
[http://dx.doi.org/10.1016/S0378-5173(99)00414-7] [PMID: 10699711]
[32]
Verma, S.; Gokhale, R.; Burgess, D.J. A comparative study of top-down and bottom-up approaches for the preparation of micro/nanosuspensions. Int. J. Pharm., 2009, 380(1-2), 216-222.
[http://dx.doi.org/10.1016/j.ijpharm.2009.07.005] [PMID: 19596059]
[33]
Esomeprazole magnesium. The American society of health system pharmacist. (Accessed on: January 4, . 2019.
[34]
Moinard-Checot, D.; Chevalier, Y.; Briançon, S.; Fessi, H.; Guinebretière, S. Nanoparticles for drug delivery: Review of the formulation and process difficulties illustrated by the emulsion-diffusion process. J. Nanosci. Nanotechnol., 2006, 6(9-10), 2664-2681.
[http://dx.doi.org/10.1166/jnn.2006.479] [PMID: 17048474]
[35]
Thodeti, S.; Bantikatla, H.B.; Kumar, Y.K.; Sathish, B. Synthesis and characterization of ZnO nanostructures by oxidation technique. Int. J. Adv. Res. Sci. Engr., 2017, 6, 539-544.
[36]
Agarwal, V.; Bajpai, M. Preparation and Optimization of esomeprazole nanosuspension using evaporative precipitation– ultrasonication. Trop. J. Pharm. Res., 2014, 13(4), 497-503.
[http://dx.doi.org/10.4314/tjpr.v13i4.2]
[37]
Papdiwal, A.P.; Pande, V.V.; Aher, S.J. Investigation of effect of different stabilizers on formulation of zaltoprofen nanosuspension. Int. J. Pharm. Sci. Rev. Res., 2014, 27(2), 244-249.
[38]
Hidenori, O.; Yukio, N.; Kazunori, K. PEG-ylated nanoparticles for biological and pharmaceutical application. Adv. Drug Del. Res., 2003, 24, 403-419.
[39]
Wang, Y.; Zhang, D.; Liu, Z.; Liu, G.; Duan, C.; Jia, L.; Feng, F.; Zhang, X.; Shi, Y.; Zhang, Q. In vitro and in vivo evaluation of silybin nanosuspensions for oral and intravenous delivery. Nanotechnology, 2010, 21(15)155104
[http://dx.doi.org/10.1088/0957-4484/21/15/155104] [PMID: 20332565]
[40]
Pal, S.L.; Jana, U.; Manna, P.K.; Mohanta, G.P.; Manavalan, R. Nanoparticle: An overview of preparation and characterization. J. Appl. Pharm. Sci., 2011, 1, 228-234.
[41]
Agarwal, V.; Bajpai, M. Investigation of formulation and process parameters for the production of esomeprazole nanosuspension by anti-solvent precipitation ultrasonication technique. Curr. Nanosci., 2013, 9, 773-779.
[http://dx.doi.org/10.2174/15734137113099990079]
[42]
Goel, S.; Sachdeva, M.; Agarwal, V. Nanosuspension technology: Recent patents on drug delivery and their characterizations. Recent Pat. Drug Deliv. Formul., 2019, 13(2), 91-104.
[http://dx.doi.org/10.2174/1872211313666190614151615] [PMID: 31203813]

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