Login Register Cart 0
Generic placeholder image

Current Drug Therapy

Editor-in-Chief

ISSN (Print): 1574-8855
ISSN (Online): 2212-3903

Back
Journal Home About Journal Editorial Board Journal Insight Current Issue Volumes/Issues
Subscribe
Research Article

Polymeric Nanoparticles: A Promising Tool to Enhance the Solubility of Poorly Water Soluble Drug

Author(s): Nirmal M. Kasekar*, Sarabjit Singh, K.R. Jadhav and V.J. Kadam

Volume 15, Issue 1, 2020

Page: [67 - 77] Pages: 11

DOI: 10.2174/1574885514666190610125127

Price: $65

Abstract

Objective: The objective of this study was to entrap water-insoluble drug itraconazole into polymer to form drug entrapped nanoparticles by using simple formulation strategy and characterize them for various in vitro properties.

Method: Itraconazole (ITZ) encapsulated Eudragit E 100 nanoparticles (IEENs) were formulated by emulsification solvent evaporation technique.

Results: Developed IEENs were evaluated for entrapment efficiency, particle size, polydispersity index, and drug release profile. It was clear that drug polymer ratio along with homogenization speed are the factors affecting droplet size of an emulsion. Evaluation was done by HPLC at 263nm. DSC, XRD studies were carried out. The in vitro antifungal study of nanoparticles suggested that they are more effective in inhibiting growth of Candida albicans.

Conclusion: The results from this study suggest the potential use of IEENs to provide a possible way of improving solubility and thus oral absorption of Itraconazole. Thus the study concluded that IEENs have potential to effectively treat the fungal infection.

Keywords: Itraconazole, poorly water soluble, eudragit, nanoparticles, HPLC, bioavailabilty.

« Previous Next »
Graphical Abstract

[1]
Nallaguntla L, Muzib YI, Aukunuru J, Balekari U. Novel nanoparticles for oral delivery of low molecular weight heparin: In vitro and in vivo assessment. Asian J Pharm Clin Res 2017; 10: 254-61.
[http://dx.doi.org/10.22159/ajpcr.2017.v10i2.15514]
[2]
Mohanty B, Majumdar DK, Mishra SK, Panda AK, Patnaik S. Development and characterization of itraconazole-loaded solid lipid nanoparticles for ocular delivery. Pharm Dev Technol 2015; 20(4): 458-64.
[http://dx.doi.org/10.3109/10837450.2014.882935] [PMID: 24490828]
[3]
Hiendrawan S, Hartanti AW, Veriansyah B, Widjojosusumo E, Tjandrawinata RR. Solubility enhancement of ketoconazole via salt and cocrystal formation. Int J Pharm Pharm Sci 2015; 7: 160-4.
[4]
Pragna S, Mandowaraa VK, Deepak G, Shetulv P. Formulation of curcuminoid loaded solid lipid nanoparticles in order to improve oral bioavailability. Int J Pharm Pharm Sci 2015; 7: 278-82.
[5]
Thadkala K, Nanam PK, Rambabu B, Sailu C, Aukunuru J. Preparation and characterization of amorphous ezetimibe nanosuspensions intended for enhancement of oral bioavailability. Int J Pharm Investig 2014; 4(3): 131-7.
[http://dx.doi.org/10.4103/2230-973X.138344] [PMID: 25126526]
[6]
Nanam PK, Thadkala K, Chinta S, Aukunuru J. Investigation of various practical techniques to enhance dissolution of ezetimibe from oral tablets. J Young Pharm 2014; 6: 8-15.
[http://dx.doi.org/10.5530/jyp.2014.1.2]
[7]
Yi Y, Tu L, Hu K, Wu W, Feng J. The construction of puerarin nanocrystals and its pharmacokinetic and in vivo-in vitro correlation (IVIVC) studies on beagle dog. Colloids Surf B Biointerfaces 2015; 133: 164-70.
[http://dx.doi.org/10.1016/j.colsurfb.2015.04.054] [PMID: 26099971]
[8]
Ho C, Davies AM, Sangha RS, et al. Phase I/II trial of pemetrexed plus nab-paclitaxel in advanced solid tumor patients with emphasis on non-small cell lung cancer. Invest New Drugs 2013; 31(6): 1587-91.
[http://dx.doi.org/10.1007/s10637-013-0024-y] [PMID: 24013936]
[9]
Kompella UB, Bandi N, Ayalasomayajula SP. Subconjunctival nano- and microparticles sustain retinal delivery of budesonide, a corticosteroid capable of inhibiting VEGF expression. Invest Ophthalmol Vis Sci 2003; 44(3): 1192-201.
[http://dx.doi.org/10.1167/iovs.02-0791] [PMID: 12601049]
[10]
Kolluru LP, Rizvi SA, D’Souza M, D’Souza MJ. Formulation development of albumin based theragnostic nanoparticles as a potential delivery system for tumor targeting. J Drug Target 2013; 21(1): 77-86.
[http://dx.doi.org/10.3109/1061186X.2012.729214] [PMID: 23036042]
[11]
Raju A, Reddy AJ, Satheesh J, Jithan AV. Preparation and characterisation of nevirapine oral nanosuspensions. Indian J Pharm Sci 2014; 76(1): 62-71.
[PMID: 24799740]
[12]
Amidon GL, Lennernäs H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995; 12(3): 413-20.
[http://dx.doi.org/10.1023/A:1016212804288] [PMID: 7617530]
[13]
Yohei K. Formulation design for poorly water soluble drugs based on bio-pharmaceutics classification system. Int J Pharma Sci 2011; 420: 1-10.
[http://dx.doi.org/10.1016/j.ijpharm.2011.08.032]
[14]
Jinno J, Kamada N, Miyake M, et al. Effect of particle size reduction on dissolution and oral absorption of a poorly water-soluble drug, cilostazol, in beagle dogs. J Control Release 2006; 111(1-2): 56-64.
[http://dx.doi.org/10.1016/j.jconrel.2005.11.013] [PMID: 16410029]
[15]
Yellela S, Krishniah R. Pharmaceutical technologies for enhancing oral bioavailability of poorly soluble drugs. J Bioequivalence Bioavailab 2010; 2: 28-36.
[16]
Jung JY, Yoo SD, Lee SH, Kim KH, Yoon DS, Lee KH. Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique. Int J Pharm 1999; 187(2): 209-18.
[http://dx.doi.org/10.1016/S0378-5173(99)00191-X] [PMID: 10502627]
[17]
Wang SL, Lin SY, Chen TF, Cheng WT. Eudragit E accelerated the diketopiperazine formation of enalapril maleate determined by thermal FTIR microspectroscopic technique. Pharm Res 2004; 21(11): 2127-32.
[http://dx.doi.org/10.1023/B:PHAM.0000048206.62093.4e] [PMID: 15587937]
[18]
Yen FL, Wu TH, Lin LT, Cham TM, Lin CC. Naringenin-loaded nanoparticles improve the physicochemical properties and the hepatoprotective effects of naringenin in orally-administered rats with CCl(4)-induced acute liver failure. Pharm Res 2009; 26(4): 893-902.
[http://dx.doi.org/10.1007/s11095-008-9791-0] [PMID: 19034626]
[19]
Wu TH, Yen FL, Lin LT, Tsai TR, Lin CC, Cham TM. Preparation, physicochemical characterization, and antioxidant effects of quercetin nanoparticles. Int J Pharm 2008; 346(1-2): 160-8.
[http://dx.doi.org/10.1016/j.ijpharm.2007.06.036] [PMID: 17689897]
[20]
Patel NR, Damann K, Leonardi C, Sabliov CM. Itraconazole-loaded poly(lactic-co-glycolic) acid nanoparticles for improved antifungal activity. Nanomedicine (Lond) 2010; 5(7): 1037-50.
[http://dx.doi.org/10.2217/nnm.10.68] [PMID: 20874019]
[21]
Pardeike J, Weber S, Haber T, et al. Development of an itraconazole-loaded nanostructured lipid carrier (NLC) formulation for pulmonary application. Int J Pharm 2011; 419(1-2): 329-38.
[http://dx.doi.org/10.1016/j.ijpharm.2011.07.040] [PMID: 21839157]
[22]
Prakobvaitayakit M, Nimmannit U. Optimization of polylactic-co-glycolic acid nanoparticles containing itraconazole using 2(3) factorial design. AAPS PharmSciTech 2003; 4(4): E71
[http://dx.doi.org/10.1208/pt040471] [PMID: 15198566]
[23]
Gajra B, Dalwadi C, Patel R. Formulation and optimization of itraconazole polymeric lipid hybrid nanoparticles (Lipomer) using Box Behnken design. Daru 2015; 23: 3.
[http://dx.doi.org/10.1186/s40199-014-0087-0] [PMID: 25604353]
[24]
Kumar V, Wang L, Riebe M, Tung HH, Prud’homme RK. Formulation and stability of itraconazole and odanacatib nanoparticles: governing physical parameters. Mol Pharm 2009; 6(4): 1118-24.
[http://dx.doi.org/10.1021/mp900002t] [PMID: 19366261]
[25]
Odds FC, Oris M, Van Dorsselaer P, Van Gerven F. Activities of an intravenous formulation of itraconazole in experimental disseminated Aspergillus, Candida, and Cryptococcus infections. Antimicrob Agents Chemother 2000; 44(11): 3180-3.
[http://dx.doi.org/10.1128/AAC.44.11.3180-3183.2000] [PMID: 11036047]
[26]
Xu Y, Liu X, Lian R, et al. Enhanced dissolution and oral bioavailability of aripiprazole nanosuspensions prepared by nanoprecipitation/homogenization based on acid-base neutralization. Int J Pharm 2012; 438(1-2): 287-95.
[http://dx.doi.org/10.1016/j.ijpharm.2012.09.020] [PMID: 22989976]
[27]
Mansour M, Pouretedal HR, Vida V. Preparation and characterization of ibuprofen nanoparticles by using solvent-anti-solvent precipitation. Open Conf Proc J 2011; 2: 88-94.
[http://dx.doi.org/10.2174/2210289201102010088]
[28]
Kakran M, Sahoo NG, Li L, et al. Fabrication of drug nanoparticles by evaporative precipitation of nanosuspension. Int J Pharm 2010; 383(1-2): 285-92.
[http://dx.doi.org/10.1016/j.ijpharm.2009.09.030] [PMID: 19781606]
[29]
Khachane P, Date AA, Nagarsenker MS. Eudragit EPO nanoparticles: application in improving therapeutic efficacy and reducing ulcerogenicity of meloxicam on oral administration. J Biomed Nanotechnol 2011; 7(4): 590-7.
[http://dx.doi.org/10.1166/jbn.2011.1322] [PMID: 21870464]
[30]
Xia D, Quan P, Piao H, Piao H, Sun S. Preparation of stable nitrindepine nano suspensions using precipitation-ultrasonication method for enhancement of dissolution of oral bioavailability. Adv Drug Deliv Rev 2011; 47: 19-25.
[31]
Kasekar N, Godiyal S, Jadhav K, Kadam V. Development and validation of a simple and rapid hplc method for determination of itraconazole in bulk and marketed formulation. Der Pharmacia Lettre 2017; 9: 36-43.
[32]
Ananthanarayan R, Panicker CKJ. Laboratory Control of Antimicrobial Therapy Textbook of Microbiology 2009.
[33]
Sabale V, Vora S. Formulation and evaluation of microemulsion-based hydrogel for topical delivery. Int J Pharm Investig 2012; 2(3): 140-9.
[http://dx.doi.org/10.4103/2230-973X.104397] [PMID: 23373005]
[34]
Ubrich N, Schmidt C, Bodmeier R, Hoffman M, Maincent P. Oral evaluation in rabbits of cyclosporin-loaded Eudragit RS or RL nanoparticles. Int J Pharm 2005; 288(1): 169-75.
[http://dx.doi.org/10.1016/j.ijpharm.2004.09.019] [PMID: 15607269]
[35]
Eerikainen H. Preparation of nanoparticles consisting of methacrylic polymers and drugs by an aerosol flow reactor method 2005.
[36]
Maragori V, Madhusudhan A, Bhagavnath RG, Venkatesham M, Veerabhadram G. Design and evaluation of efavirenz laoded solid lipid nanoparticles to improve the oral bioavailability. Int J Pharm & Pharm Sci Res 2012; 2: 84-9.
[37]
Koh PT, Chuah JN, Talekar M, Gorajana A, Garg S. Formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems. Indian J Pharm Sci 2013; 75(3): 291-301.
[http://dx.doi.org/10.4103/0250-474X.117434] [PMID: 24082345]
[38]
Hu DD, Lin CC, Liu L, Li S, Zhao YP. Preparation, characterization, and in vitro release investigation of lutein/zein nanoparticles via solution enhanced dispersion by supercritical fluids. J Food Eng 2011; 109: 545-52.
[http://dx.doi.org/10.1016/j.jfoodeng.2011.10.025]

Rights & Permissions Print Cite
Article Metrics
17
5
© 2024 Bentham Science Publishers | Privacy Policy