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Recent Advances in Drug Delivery and Formulation

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ISSN (Print): 2667-3878
ISSN (Online): 2667-3886

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Research Article

Nanoemulsion-Based Strategy for Maximizing Nitrofurantoin Absorption: In-vitro and In-vivo Investigations

Author(s): Gouri Prasad Nanda, Mrunali Patel and Rashmin Patel*

Volume 17, Issue 3, 2023

Published on: 02 October, 2023

Page: [241 - 253] Pages: 13

DOI: 10.2174/0126673878259374230921045432

Price: $65

Abstract

Background: The main objective of the current research work is to improve the absorption of Nitrofurantoin (NFT) by minimizing gastrointestinal (GI) intolerance and variations in its absorption by formulating the drug into a nanoemulsion (NE).

Method: Based on the highest saturation solubility of NFT, soybean oil, transcutol HP, and labrafil M1944CS were selected as oil, co-surfactant, and surfactant, and a Smix ratio of 1:2 was selected based on pseudoternary phase diagrams. The formulation prepared with an equal ratio of oil and Smix exhibited the lowest globule size, highest zeta potential, and higher drug release and hence was selected for further evaluation.

Result: Optimized formulation (NF5) showed improved membrane permeability against pure drug suspension (2.30 times) and marketed suspension formulation (1.43 times). NF5 exhibited similar % cell viability and % cell toxicity in Caco-2 cell lines compared to the marketed suspension. The relative bioavailability of NFT-NE was enhanced by 1.10 and 1.17 times compared to the marketed and pure drug suspension, respectively.

Conclusion: Thus, it can be concluded that the optimized nanoemulsion formulation of NFT exhibited improved membrane permeability, comparable cell viability, and increased relative bioavailability. These findings suggest the potential of the nanoemulsion approach as a strategy to overcome the variability of oral absorption and GI intolerance of NFT.

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[1]
Kumar M, Bishnoi RS, Shukla AK, Jain CP. Techniques for formulation of nanoemulsion drug delivery system: a review. Prev Nutr Food Sci 2019; 24(3): 225-34.
[http://dx.doi.org/10.3746/pnf.2019.24.3.225] [PMID: 31608247]
[2]
Karthik P, Ezhilarasi PN, Anandharamakrishnan C. Challenges associated in stability of food grade nanoemulsions. Crit Rev Food Sci Nutr 2017; 57(7): 1435-50.
[http://dx.doi.org/10.1080/10408398.2015.1006767] [PMID: 26114624]
[3]
Mu H, Holm R, Müllertz A. Lipid-based formulations for oral administration of poorly water-soluble drugs. Int J Pharm 2013; 453(1): 215-24.
[http://dx.doi.org/10.1016/j.ijpharm.2013.03.054] [PMID: 23578826]
[4]
Qian C, McClements DJ. Formation of nanoemulsions stabilized by model food-grade emulsifiers using high-pressure homogenization: Factors affecting particle size. Food Hydrocoll 2011; 25(5): 1000-8.
[http://dx.doi.org/10.1016/j.foodhyd.2010.09.017]
[5]
Chatterjee B, Hamed Almurisi S, Ahmed Mahdi Dukhan A, Mandal UK, Sengupta P. Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view. Drug Deliv 2016; 23(9): 3639-52.
[http://dx.doi.org/10.1080/10717544.2016.1214990] [PMID: 27685505]
[6]
Dokania S, Joshi AK. Self-microemulsifying drug delivery system (SMEDDS) – challenges and road ahead. Drug Deliv 2015; 22(6): 675-90.
[http://dx.doi.org/10.3109/10717544.2014.896058] [PMID: 24670091]
[7]
Feeney OM, Crum MF, McEvoy CL, et al. 50 years of oral lipid-based formulations: Provenance, progress and future perspectives. Adv Drug Deliv Rev 2016; 101: 167-94.
[http://dx.doi.org/10.1016/j.addr.2016.04.007] [PMID: 27089810]
[8]
Belhaj N, Arab-Tehrany E, Linder M. Oxidative kinetics of salmon oil in bulk and in nanoemulsion stabilized by marine lecithin. Process Biochem 2010; 45(2): 187-95.
[http://dx.doi.org/10.1016/j.procbio.2009.09.005]
[9]
Neslihan Gursoy R, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother 2004; 58(3): 173-82.
[http://dx.doi.org/10.1016/j.biopha.2004.02.001] [PMID: 15082340]
[10]
Yuan Y, Gao Y, Zhao J, Mao L. Characterization and stability evaluation of β-carotene nanoemulsions prepared by high pressure homogenization under various emulsifying conditions. Food Res Int 2008; 41(1): 61-8.
[http://dx.doi.org/10.1016/j.foodres.2007.09.006]
[11]
Cherukuvada S, Babu NJ, Nangia A. Nitrofurantoin– p ‐aminobenzoic acid cocrystal: Hydration stability and dissolution rate studies. J Pharm Sci 2011; 100(8): 3233-44.
[http://dx.doi.org/10.1002/jps.22546] [PMID: 21425165]
[12]
Paul HE, Hayes KJ, Paul MF, Borgmann AR. Laboratory studies with nitrofurantoin. Relationship between crystal size, urinary excretion in the rat and man, and emesis in dogs. J Pharm Sci 1967; 56(7): 882-5.
[http://dx.doi.org/10.1002/jps.2600560719] [PMID: 6034831]
[13]
Meyer MC, Slywka GWA, Dann RE, Whyatt PL. Bioavailability of 14 nitrofurantoin products. J Pharm Sci 1974; 63(11): 1693-8.
[http://dx.doi.org/10.1002/jps.2600631105] [PMID: 4427226]
[14]
Meyer MC, Wood GC, Straughn AB. In vitro and in vivo evaluation of seven 50 mg and 100 mg nitrofurantoin tablets. Biopharm Drug Dispos 1989; 10(3): 321-9.
[http://dx.doi.org/10.1002/bdd.2510100310] [PMID: 2720135]
[15]
Calderaro A, Maugeri A, Magazù S, Laganà G, Navarra M, Barreca D. Molecular basis of interactions between the antibiotic nitrofurantoin and human serum albumin: a mechanism for the rapid drug blood transportation. Int J Mol Sci 2021; 22(16): 8740.
[http://dx.doi.org/10.3390/ijms22168740] [PMID: 34445446]
[16]
Bates TR, Young JM, Wu CM, Rosenberg HA. pH-dependent dissolution rate of nitrofurantoin from commercial suspensions, tablets, and capsules. J Pharm Sci 1974; 63(4): 643-5.
[http://dx.doi.org/10.1002/jps.2600630441] [PMID: 4828728]
[17]
Monika R, Wojciech S, Krystyna P, Ewa K. Combined effect of nitrofurantoin and plant surfactant on bacteria phospholipid membrane. Mol 2020; 25(2527): 1-14.
[18]
Balasubramanian P, Annalakshmi M, Chen SM, Sathesh T, Balamurugan TST. Ultrasonic energy-assisted preparation of β-cyclodextrin-carbon nanofiber composite: Application for electrochemical sensing of nitrofurantoin. Ultrason Sonochem 2019; 52: 391-400.
[http://dx.doi.org/10.1016/j.ultsonch.2018.12.014] [PMID: 30591361]
[19]
Segalina A, Pavan B, Ferretti V, et al. Cocrystals of nitrofurantoin: how coformers can modify its solubility and permeability across intestinal cell monolayers. Cryst Growth Des 2022; 22(5): 3090-106.
[http://dx.doi.org/10.1021/acs.cgd.2c00007]
[20]
Ghawji AB, Fogg AG. Reduction in size by electrochemical pre-treatment at high negative potentials of the background currents obtained at negative potentials at glassy carbon electrodes and its application in the reductive flow injection amperometric determination of nitrofurantoin. Analyst (Lond) 1986; 111(2): 157-61.
[http://dx.doi.org/10.1039/an9861100157]
[21]
Cyprian OO, Omotosho JA. Bioavailability of nitrofurantoin from multiple w/o/w emulsions in man and the influence of the oil phase of the emulsion. Indian J Pharm Sci 1993; 55: 14-8.
[22]
Sujitkumar KD, Vinit RS, Sagar LP, Kiran SP, Sachin SM. Quality by design approach for development and evaluation of self-emulsifying drug delivery system of nitrofurantoin. Eur J Biomed Pharm Sci 2018; 5: 244-52.
[23]
Kommuru TR, Gurley B, Khan MA, Reddy IK. Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment. Int J Pharm 2001; 212(2): 233-46.
[http://dx.doi.org/10.1016/S0378-5173(00)00614-1] [PMID: 11165081]
[24]
Lanna AC, José IC, Oliveira MGA, Barros EG, Moreira MA. Effect of temperature on polyunsaturated fatty acid accumulation in soybean seeds. Braz J Plant Physiol 2005; 17(2): 213-22.
[http://dx.doi.org/10.1590/S1677-04202005000200004]
[25]
Bastos Fernandes JC, Draghi PF. Thermal Stability of Soybean Oil: When must we discard it? MOJ Food Processing & Technology 2016; 2(5): 170-4.
[http://dx.doi.org/10.15406/mojfpt.2016.02.00051]
[26]
Attama AA, Nkemnele MO. In vitro evaluation of drug release from self micro-emulsifying drug delivery systems using a biodegradable homolipid from Capra hircus. Int J Pharm 2005; 304(1-2): 4-10.
[http://dx.doi.org/10.1016/j.ijpharm.2005.08.018] [PMID: 16198521]
[27]
Balakrishnan P, Lee BJ, Oh DH, et al. Enhanced oral bioavailability of Coenzyme Q10 by self-emulsifying drug delivery systems. Int J Pharm 2009; 374(1-2): 66-72.
[http://dx.doi.org/10.1016/j.ijpharm.2009.03.008] [PMID: 19446761]
[28]
Cuiné JF, McEvoy CL, Charman WN, et al. Evaluation of the impact of surfactant digestion on the bioavailability of danazol after oral administration of lipidic self-emulsifying formulations to dogs. J Pharm Sci 2008; 97(2): 995-1012.
[http://dx.doi.org/10.1002/jps.21246] [PMID: 18064698]
[29]
Perlman M, Murdande S, Gumkowski M, et al. Development of a self-emulsifying formulation that reduces the food effect for torcetrapib. Int J Pharm 2008; 351(1-2): 15-22.
[http://dx.doi.org/10.1016/j.ijpharm.2007.09.015] [PMID: 18024021]
[30]
Nief RA, Farha KO, Abdulsalam AM. Spectrophotometric estimation of nitrofurantoin and its application in pharmaceuticals preparation. Biochem Cell Arch 2020; 20: 4325-8.
[31]
Arida AI, Al-Tabakha MM, Hamoury HAJ. Improving the high variable bioavailability of griseofulvin by SEDDS. Chem Pharm Bull (Tokyo) 2007; 55(12): 1713-9.
[http://dx.doi.org/10.1248/cpb.55.1713] [PMID: 18057745]
[32]
Mehanna MM, Mneimneh AT. Formulation and applications of lipid-based nanovehicles: spotlight on self-emulsifying systems. Adv Pharm Bull 2020; 11(1): 56-67.
[http://dx.doi.org/10.34172/apb.2021.006] [PMID: 33747852]
[33]
Chintalapudi R, Murthy TEGK, Lakshmi KR, Manohar GG. Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine. Int J Pharm Investig 2015; 5(4): 205-13.
[http://dx.doi.org/10.4103/2230-973X.167676] [PMID: 26682191]
[34]
Salamanca C, Barrera-Ocampo A, Lasso J, Camacho N, Yarce C. Franz diffusion cell approach for pre-formulation characterization of ketoprofen semi-solid dosage forms. Pharmaceutics 2018; 10(3): 148.
[http://dx.doi.org/10.3390/pharmaceutics10030148] [PMID: 30189634]
[35]
Gupta V, Trivedi P. Ex vivo localization and permeation of cisplatin from novel topical formulations through excised pig, goat, and mice skin and in vitro characterization for effective management of skin-cited malignancies. Artif Cells Nanomed Biotechnol 2015; 43(6): 373-82.
[http://dx.doi.org/10.3109/21691401.2014.893523] [PMID: 24628359]
[36]
Shin JW, Seol IC, Son CG. Interpretation of animal dose and human equivalent dose for drug development. J Korean Orient Med 2010; 31: 1-7.
[37]
Muth P, Metz R, Siems B, Bolten WW, Vergin H. Sensitive determination of nitrofurantoin in human plasma and urine by high-performance liquid chromatography. J Chromatogr A 1996; 729(1-2): 251-8.
[http://dx.doi.org/10.1016/0021-9673(95)00894-2] [PMID: 9004947]
[38]
Pamulapati CR, Schoenwald RD. Ocular pharmacokinetics of a novel tetrahydroquinoline analog in rabbit: absorption, disposition, and non-compartmental analysis. J Pharm Sci 2011; 100(12): 5315-23.
[http://dx.doi.org/10.1002/jps.22720] [PMID: 21850670]
[39]
Li F, Hu R, Wang B, et al. Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake. Acta Pharm Sin B 2017; 7(3): 353-60.
[http://dx.doi.org/10.1016/j.apsb.2017.02.002] [PMID: 28540173]
[40]
Nadine MF, Heike B. Drug localization and its effect on the physical stability of poloxamer 188-stabilized colloidal lipid emulsions. Int J Pharm 2021; 15(599): 120394.
[41]
Ali MS, Alam MS, Alam N, Siddiqui MR. Preparation, characterization and stability study of dutasteride loaded nanoemulsion for treatment of benign prostatic hypertrophy. Iran J Pharm Res 2014; 13(4): 1125-40.
[PMID: 25587300]
[42]
Gutiérrez JM, González C, Maestro A, Solè I, Pey CM, Nolla J. Nano-emulsions: New applications and optimization of their preparation. Curr Opin Colloid Interface Sci 2008; 13(4): 245-51.
[http://dx.doi.org/10.1016/j.cocis.2008.01.005]
[43]
Hsieh CW, Li PH, Lu IC, Wang TH. Preparing glabridin-in-water nanoemulsions by high pressure homogenization with response surface methodology. J Oleo Sci 2012; 61(9): 483-9.
[http://dx.doi.org/10.5650/jos.61.483] [PMID: 22975782]
[44]
Hu J, Johnston KP, Williams RO III. Nanoparticle engineering processes for enhancing the dissolution rates of poorly water soluble drugs. Drug Dev Ind Pharm 2004; 30(3): 233-45.
[http://dx.doi.org/10.1081/DDC-120030422] [PMID: 15109023]
[45]
Ahmad N, Ahmad R, Mohammed Buheazaha T, Salman AlHomoud H, Al-Nasif HA, Sarafroz M. A comparative ex vivo permeation evaluation of a novel 5-Fluorocuracil nanoemulsion-gel by topically applied in the different excised rat, goat, and cow skin. Saudi J Biol Sci 2020; 27(4): 1024-40.
[http://dx.doi.org/10.1016/j.sjbs.2020.02.014] [PMID: 32256163]
[46]
Bu P, Narayanan S, Dalrymple D, Cheng X, Serajuddin ATM. Cytotoxicity assessment of lipid-based self-emulsifying drug delivery system with Caco-2 cell model: Cremophor EL as the surfactant. Eur J Pharm Sci 2016; 91: 162-71.
[http://dx.doi.org/10.1016/j.ejps.2016.06.011] [PMID: 27328127]
[47]
Patel MR, Patel RB, Thakore SD, Solanki AB. Brain targeted delivery of lurasidone HCl via nasal administration of mucoadhesive nanoemulsion formulation for the potential management of schizophrenia. Pharm Dev Technol 2020; 25(8): 1018-30.
[http://dx.doi.org/10.1080/10837450.2020.1772292] [PMID: 32432956]
[48]
Patel MR, Patel MH, Patel RB. Preparation and in vitro/ex vivo evaluation of nanoemulsion for transnasal delivery of paliperidone. Appl Nanosci 2016; 6(8): 1095-104.
[http://dx.doi.org/10.1007/s13204-016-0527-x]
[49]
Simon K, Andrew JP, Yuliya N, Peter K. Quantification of lactate dehydrogenase for cell viability testing using cell lines and primary cultured astrocytes Curr Protoc Toxicol 2018; 72: 2.26.1-2.26.10.
[http://dx.doi.org/10.1002/cptx.21]
[50]
Endrenyi L, Fritsch S, Yan W. Cmax/AUC is a clearer measure than Cmax for absorption rates in investigations of bioequivalence. Int J Clin Pharmacol Ther Toxicol 1991; 29(10): 394-9.
[PMID: 1748540]
[51]
Bialer M, Look ZM, Silber BM, Yacobi A. The relationship between drug input and mean residence time in the body. Biopharm Drug Dispos 1986; 7(6): 577-83.
[http://dx.doi.org/10.1002/bdd.2510070607] [PMID: 3828487]
[52]
Szabó-Bárdos E, Cafuta A, Hegedűs P, et al. Photolytic and photocatalytic degradation of nitrofurantoin and its photohydrolytic products. J Photochem Photobiol Chem 2020; 386: 112093.
[http://dx.doi.org/10.1016/j.jphotochem.2019.112093]

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