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Recent Patents on Nanotechnology

Editor-in-Chief

ISSN (Print): 1872-2105
ISSN (Online): 2212-4020

Research Article

Formulation and Characterization of Febuxostat Loaded Nanostructured Lipid Carriers (NLCs) - Gel for Topical Treatment of Gout

Author(s): Navni Sharma, Sandeep Kumar, Garima Joshi* and Deepak Choudhary *

Volume 16, Issue 3, 2022

Published on: 15 April, 2021

Page: [250 - 258] Pages: 9

DOI: 10.2174/1872210515666210415114118

Price: $65

Abstract

Background: The aim of the present study was to formulate and characterize Nano- Structured Lipid Carriers (NLCs) of Febuxostat (FB) incorporated in the gel for the treatment of Gout. FB is a Xanthine Oxidase (XO) inhibitor drug used for chronic Gout and hyperuricemia. FB is a BCS class II drug, therefore, water solubility is very poor, and due to its poor solubility and wettability, it leads to poor dissolution. The hot high-pressure homogenization technique was used in this study to improve the physicochemical property of FB.

Methods: The carbopol 934 was used to prepare NLCs gel of FB. The NLCs of FB was prepared in different drug: polymer ratios w/w (2:1), (1:1), (1:2), (1:3) and (1:4) with solid lipid (Stearic Acid) and liquid lipid (Oleic acid). The preformulation study of FB included FTIR study melting point, standard calibration curves, and drug-polymer interaction study.

Results: The NLCs (1:3) showed high entrapment and drug content. The NLCs gel formulation was 87% released within 6 hours in a controlled manner.

Conclusion: NLCs gel modifies the drug release, increases the bioavailability, and reduces side effects of FB. The prepared gel is the efficient formulation for the better treatment of chronic gout and hyperuricemia. The research findings have shown the undesirable side effects associated with the oral route that can be reduced by the use of NLCs formulation through the transdermal route in an effective manner.

Keywords: Febuxostat, NLCs, carbopol gel, gout, monosodium urate, uric acid.

Graphical Abstract

[1]
Dalbeth N, Merriman TR, Stamp LK. Gout Lancet 2016; 388(10055): 2039-52.
[http://dx.doi.org/10.1016/S0140-6736(16)00346-9] [PMID: 27112094]
[2]
Emmerson BT. The management of gout. N Engl J Med 1996; 334(7): 445-51.
[http://dx.doi.org/10.1056/NEJM199602153340707] [PMID: 8552148]
[3]
Singh S, Parashar P, Kanoujia J, Singh I, Saha S, Saraf SA. Transdermal potential and anti-gout efficacy of Febuxostat from niosomal gel. J Drug Deliv Sci Technol 2017; 39: 348-61.
[http://dx.doi.org/10.1016/j.jddst.2017.04.020]
[4]
Chalikwar SS, Belgamwar VS, Talele VR, Surana SJ, Patil MU. Formulation and evaluation of Nimodipine-loaded solid lipid nanoparticles delivered via lymphatic transport system. Colloids Surf B Biointerfaces 2012; 97: 109-16.
[http://dx.doi.org/10.1016/j.colsurfb.2012.04.027] [PMID: 22609590]
[5]
Cirri M, Bragagni M, Mennini N, Mura P. Development of a new delivery system consisting in “drug--in cyclodextrin--in nanostructured lipid carriers” for ketoprofen topical delivery. Eur J Pharm Biopharm 2012; 80(1): 46-53.
[http://dx.doi.org/10.1016/j.ejpb.2011.07.015] [PMID: 21839833]
[6]
Gokce EH, Korkmaz E, Dellera E, Sandri G, Bonferoni MC, Ozer O. Resveratrol-loaded solid lipid nanoparticles versus nanostructured lipid carriers: Evaluation of antioxidant potential for dermal applications. Int J Nanomedicine 2012; 7: 1841-50.
[http://dx.doi.org/10.2147/IJN.S29710] [PMID: 22605933]
[7]
Joshi M, Patravale V. Nanostructured Lipid Carrier (NLC) based gel of celecoxib. Int J Pharm 2008; 346(1-2): 124-32.
[http://dx.doi.org/10.1016/j.ijpharm.2007.05.060] [PMID: 17651933]
[8]
Khurana S, Jain NK, Bedi PM. Development and characterization of a novel controlled release drug delivery system based on nanostructured lipid carriers gel for meloxicam. Life Sci 2013; 93(21): 763-72.
[http://dx.doi.org/10.1016/j.lfs.2013.09.027] [PMID: 24113071]
[9]
Song A, Su Z, Li S, Han F. Nanostructured lipid carriers-based flurbiprofen gel after topical administration: Acute skin irritation, pharmacodynamics, and percutaneous absorption mechanism. Drug Dev Ind Pharm 2015; 41(9): 1488-92.
[http://dx.doi.org/10.3109/03639045.2014.959021] [PMID: 25231972]
[10]
Müller RH, Petersen RD, Hommoss A, Pardeike J. Nanostructured Lipid Carrier (NLC) in cosmetic dermal products. Adv Drug Deliv Rev 2007; 59(6): 522-30.
[http://dx.doi.org/10.1016/j.addr.2007.04.012] [PMID: 17602783]
[11]
Hu FQ, Jiang SP, Du YZ, Yuan H, Ye YQ, Zeng S. Preparation and characterization of stearic acid nanostructured lipid carriers by solvent diffusion method in an aqueous system. Colloids Surf B Biointerfaces 2005; 45(3-4): 167-73.
[http://dx.doi.org/10.1016/j.colsurfb.2005.08.005] [PMID: 16198092]
[12]
Han F, Yin R, Che X, et al. Nanostructured Lipid Carrier (NLC) based topical gel of flurbiprofen: Design, characterization and in vivo evaluation. Int J Pharm 2012; 439(1-2): 349-57.
[http://dx.doi.org/10.1016/j.ijpharm.2012.08.040] [PMID: 22989987]
[13]
El-Salamouni NS, Farid RM, El-Kamel AH, El-Gamal SS. Nanostructured lipid carriers for intraocular brimonidine localisation: Development, in-vitro and in-vivo evaluation. J Microencapsul 2018; 35(1): 102-13.
[http://dx.doi.org/10.1080/02652048.2018.1425753] [PMID: 29310481]
[14]
Patel P, Puri D, Bhandari A, Choudhary D, Sharma R, Bhatele V. Formulation and evaluation of chronomodulated floating drug delivery system of famotidine. FABAD J Pharm Sci 2011; 36(4): 167-80.
[15]
Sanad RA, Abdelmalak NS, Elbayoomy TS, Badawi AA. Formulation of a novel oxybenzone-loaded Nanostructured Lipid Carriers (NLCs). AAPS PharmSciTech 2010; 11(4): 1684-94.
[http://dx.doi.org/10.1208/s12249-010-9553-2] [PMID: 21107771]
[16]
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]
[17]
Shi F, Yang G, Ren J, Guo T, Du Y, Feng N. Formulation design, preparation, and in vitro and in vivo characterizations of β-Elemene-loaded nanostructured lipid carriers. Int J Nanomedicine 2013; 8: 2533-41.
[http://dx.doi.org/10.2147/IJN.S46578] [PMID: 23901271]
[18]
Nagaich U, Gulati N. Nanostructured Lipid Carrier (NLC) based controlled release topical gel of clobetasol propionate: Design and in vivo characterization. Drug Deliv Transl Res 2016; 6(3): 289-98.
[http://dx.doi.org/10.1007/s13346-016-0291-1] [PMID: 27072979]
[19]
Shah PP, Desai PR, Channer D, Singh M. Enhanced skin permeation using polyarginine modified nanostructured lipid carriers. J Control Release 2012; 161(3): 735-45.
[http://dx.doi.org/10.1016/j.jconrel.2012.05.011] [PMID: 22617521]
[20]
Vitorino C, Almeida J, Gonçalves LM, Almeida AJ, Sousa JJ, Pais AA. Co-encapsulating nanostructured lipid carriers for transdermal application: From experimental design to the molecular detail. J Control Release 2013; 167(3): 301-14.
[http://dx.doi.org/10.1016/j.jconrel.2013.02.011] [PMID: 23454133]
[21]
Shah NV, Seth AK, Balaraman R, Aundhia CJ, Maheshwari RA, Parmar GR. Nanostructured lipid carriers for oral bioavailability enhancement of raloxifene: Design and in vivo study. J Adv Res 2016; 7(3): 423-34.
[http://dx.doi.org/10.1016/j.jare.2016.03.002] [PMID: 27222747]
[22]
Patel PA, Patil SC, Kalaria DR, Kalia YN, Patravale VB. Comparative in vitro and in vivo evaluation of lipid based nanocarriers of Huperzine A. Int J Pharm 2013; 446(1-2): 16-23.
[http://dx.doi.org/10.1016/j.ijpharm.2013.02.014] [PMID: 23410989]
[23]
Uprit S, Kumar Sahu R, Roy A, Pare A. Preparation and characterization of minoxidil loaded nanostructured lipid carrier gel for effective treatment of alopecia. Saudi Pharm J 2013; 21(4): 379-85.
[http://dx.doi.org/10.1016/j.jsps.2012.11.005] [PMID: 24227958]
[24]
Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001; 13(2): 123-33.
[http://dx.doi.org/10.1016/S0928-0987(01)00095-1] [PMID: 11297896]
[25]
Tran TH, Ramasamy T, Truong DH, Choi HG, Yong CS, Kim JO. Preparation and characterization of fenofibrate-loaded nanostructured lipid carriers for oral bioavailability enhancement. AAPS PharmSciTech 2014; 15(6): 1509-15.
[http://dx.doi.org/10.1208/s12249-014-0175-y] [PMID: 25035071]
[26]
Zhao J, Piao X, Shi X, Si A, Zhang Y, Feng N. Podophyllotoxin-loaded nanostructured lipid carriers for skin targeting: In vitro and in vivo studies. Molecules 2016; 21(11): 1549.
[http://dx.doi.org/10.3390/molecules21111549] [PMID: 27869698]
[27]
Singh A, Neupane YR, Mangla B, Kohli K. Nanostructured lipid carriers for oral bioavailability enhancement of exemestane: Formulation design, in vitro, ex vivo, and in vivo studies. J Pharm Sci 2019; 108(10): 3382-95.
[http://dx.doi.org/10.1016/j.xphs.2019.06.003] [PMID: 31201904]
[28]
Motawea A, Borg T, Abd El-Gawad AEH. Topical phenytoin nanostructured lipid carriers: Design and development. Drug Dev Ind Pharm 2018; 44(1): 144-57.
[http://dx.doi.org/10.1080/03639045.2017.1386204] [PMID: 28956451]
[29]
Chauhan I, Yasir M, Verma M, Singh AP. Nanostructured lipid carriers: A groundbreaking approach for transdermal drug delivery. Adv Pharm Bull 2020; 10(2): 150-65.
[http://dx.doi.org/10.34172/apb.2020.021] [PMID: 32373485]

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