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Pharmaceutical Nanotechnology

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ISSN (Print): 2211-7385
ISSN (Online): 2211-7393

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Research Article

Effect of the Surfactant and Liquid Lipid Type in the Physico-chemical Characteristics of Beeswax-based Nanostructured Lipid Carrier (NLC) of Metformin

Author(s): Mona Qushawy*

Volume 9, Issue 3, 2021

Published on: 22 February, 2021

Page: [200 - 209] Pages: 10

DOI: 10.2174/2211738509666210222143716

Price: $65

Abstract

Background: Metformin (MF) is an antidiabetic drug that belongs to class III of the biopharmaceutical classification system (BCS) characterized by high solubility and low permeability.

Objective: The study aimed to prepare metformin as nanostructured lipid carriers (MF-NLCs) to control the drug release and enhance its permeability through the biological membrane.

Methods: 22 full factorial design was used to make the design of MF-NLCs formulations. MFNLCs were prepared by hot-melt homogenization-ultra sonication technique using beeswax as solid lipid in the presence of liquid lipid (either capryol 90 or oleic acid) and surfactant (either poloxamer 188 or tween 80).

Results: The entrapment efficiency (EE%) of MF-NLCs was ranged from 85.2±2.5 to 96.5±1.8%. The particle size was in the nanoscale (134.6±4.1 to 264.1±4.6 nm). The value of zeta potential has a negative value ranged from -25.6±1.1 to -39.4±0.9 mV. The PDI value was in the range of 0.253±0.01 to 0.496±0.02. The cumulative drug release was calculated for MF-NLCs and it was found that Q12h ranged from 90.5±1.7% for MF-NLC1 to 99.3±2.8 for MF-NLC4. Infra-red (IR) spectroscopy and differential scanning calorimetry (DSC) studies revealed the compatibility of the drug with other ingredients. MF-NLC4 was found to be the optimized formulation with the best responses.

Conclusion: 22 full factorial design succeed to obtain an optimized formulation which controls the drug release and increases the drug penetration.

Keywords: Metformin (MF), nanostructured lipid carrier (NLCs), bees wax, optimization, permeability, entrapment efficiency (EE%), drug release.

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[1]
Huttunen KM, Mannila A, Laine K, et al. The first bioreversible prodrug of metformin with improved lipophilicity and enhanced intestinal absorption. J Med Chem 2009; 52(14): 4142-8.
[http://dx.doi.org/10.1021/jm900274q]
[2]
Dadhania KP, Nadpara PA, Agrawal YK. Development and validation of spectrophotometric method for simultaneous estimation of gliclazide and metformin hydrochloride in bulk and tablet dosage form by simultaneous equation method. Int J Pharm Sci Res 2011; 2: 1559-63.
[3]
Szendroedi J, Phielix E, Roden M. The role of mitochondria in insulin resistance and type 2 diabetes mellitus. Nat Rev Endocrinol 2011; 8(2): 92-103.
[http://dx.doi.org/10.1038/nrendo.2011.138]
[4]
Rena G, Hardie DG, Pearson ER. The mechanisms of action of metformin. Diabetologia 2017; 60(9): 1577-85.
[http://dx.doi.org/10.1007/s00125-017-4342-z]
[5]
Cheng J-T, Huang C-C, Liu I-M, Tzeng TF, Chang CJ. Novel mechanism for plasma glucose-lowering action of metformin in streptozotocin-induced diabetic rats. Diabetes 2006; 55(3): 819-25.
[http://dx.doi.org/10.2337/diabetes.55.03.06.db05-0934]
[6]
Klip A, Leiter LA. Cellular mechanism of action of metformin. Diabetes Care 1990; 13(6): 696-704.
[http://dx.doi.org/10.2337/diacare.13.6.696]
[7]
Strugaru A-M, Botnariu G, Agoroaei L, Grigoriu IC, Butnaru E. Metformin induced lactic acidosis-particularities and course. Rev Med Chir Soc Med Nat Iasi 2013; 117(4): 1035-42.
[8]
Bell PM, Hadden DR. Metformin. Endocrinol Metab Clin North Am 1997; 26(3): 523-37.
[http://dx.doi.org/10.1016/S0889-8529(05)70265-6]
[9]
Aksay E, Yanturali S. A rare side effect of metformin: metformin-induced hepatotoxicity. Turk J Med Sci 2007; 37: 173-5.
[10]
Peters N, Jay N, Barraud D, et al. Metformin-associated lactic acidosis in an intensive care unit. Crit Care 2008; 12(6): R149.
[http://dx.doi.org/10.1186/cc7137]
[11]
Pandit V, Pai RS, Yadav V, et al. Pharmacokinetic and pharmacodynamic evaluation of floating microspheres of metformin hydrochloride. Drug Dev Ind Pharm 2013; 39(1): 117-27.
[http://dx.doi.org/10.3109/03639045.2012.662503]
[12]
Bhujbal S, Dash AK. Metformin-loaded hyaluronic acid nanostructure for oral delivery. AAPS PharmSciTech 2018; 19(6): 2543-53.
[http://dx.doi.org/10.1208/s12249-018-1085-1]
[13]
Ubaid M, Murtaza G. Fabrication and characterization of genipin cross-linked chitosan/gelatin hydrogel for pH-sensitive, oral delivery of metformin with an application of response surface methodology. Int J Biol Macromol 2018; 114: 1174-85.
[http://dx.doi.org/10.1016/j.ijbiomac.2018.04.023]
[14]
Shirodkar RK, Kumar L, Mutalik S, et al. Solid lipid nanoparticles and nanostructured Lipid carriers: emerging lipid based Drug delivery systems. Pharm Chem J 2019; 53: 440-53.
[http://dx.doi.org/10.1007/s11094-019-02017-9]
[15]
Fang C-L, Al-Suwayeh SA, Fang JY. Nanostructured lipid carriers (NLCs) for drug delivery and targeting. Recent Pat Nanotechnol 2013; 7(1): 41-55.
[http://dx.doi.org/10.2174/187221013804484827]
[16]
Yoon G, Park JW, Yoon I-S. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs): recent advances in drug delivery. J Pharm Investig 2013; 43: 353-62.
[http://dx.doi.org/10.1007/s40005-013-0087-y]
[17]
Piazzini V, Micheli L, Luceri C, et al. Nanostructured lipid carriers for oral delivery of silymarin: improving its absorption and in vivo efficacy in type 2 diabetes and metabolic syndrome model. Int J Pharm 2019; 572118838
[http://dx.doi.org/10.1016/j.ijpharm.2019.118838]
[18]
Han F, Li S, Yin R, et al. Effect of surfactants on the formation and characterization of a new type of colloidal drug delivery system: nanostructured lipid carriers. Colloids Surf Physicochem Eng Asp 2008; 315: 210-6.
[http://dx.doi.org/10.1016/j.colsurfa.2007.08.005]
[19]
Wu L, Zhao L, Su X, et al. Repaglinide-loaded nanostructured lipid carriers with different particle sizes for improving oral absorption: preparation, characterization, pharmacokinetics, and in situ intestinal perfusion. Drug Deliv 2020; 27(1): 400-9.
[http://dx.doi.org/10.1080/10717544.2019.1689313]
[20]
Mathur P, Sharma S, Rawal S, Patel B, Patel MM. Fabrication, optimization, and in vitro evaluation of docetaxel-loaded nanostructured lipid carriers for improved anticancer activity. J Liposome Res 2020; 30(2): 182-96.
[http://dx.doi.org/10.1080/08982104.2019.1614055]
[21]
Khan N, Shah FA, Rana I, et al. Nanostructured lipid carriers-mediated brain delivery of carbamazepine for improved in vivo anticonvulsant and anxiolytic activity. Int J Pharm 2020; 577119033
[http://dx.doi.org/10.1016/j.ijpharm.2020.119033]
[22]
Ranpise HA, Gujar KN, Pawar SC, et al. Formulation, optimization, and evaluation of ketoconazole loaded nanostructured lipid carrier gel for topical delivery. Drug Deliv Lett 2020; 10: 61-71.
[http://dx.doi.org/10.2174/2210303109666190717155731]
[23]
Iqbal MA, Md S, Mustafa G, et al. Formulation, optimization and evaluation of nanostructured lipid carrier system of acyclovir for topical delivery. J Bionanoscience 2014; 8: 235-47.
[http://dx.doi.org/10.1166/jbns.2014.1231]
[24]
Davies OL, Hay WA. The construction and uses of fractional factorial designs in industrial research. Biometrics 1950; 6(3): 233-49.
[http://dx.doi.org/10.2307/3001821]
[25]
Swidan SA, Mansour ZN, Mourad ZA, et al. DOE, formulation, and optimization of Repaglinide nanostructured lipid carriers. J Appl Pharm Sci 2018; 8: 008-16.
[26]
Qushawy M, Prabahar K, Abd-Alhaseeb M, Swidan S, Nasr A. Preparation and evaluation of carbamazepine solid lipid nanoparticle for alleviating seizure activity in Pentylenetetrazole-kindled mice. Molecules 2019; 24(21): 3971.
[http://dx.doi.org/10.3390/molecules24213971]
[27]
Swidan SA, Ghonaim HM, Samy AM, et al. Efficacy and in vitro cytotoxicity of nanostructured lipid carriers for paclitaxel delivery. J Appl Pharm Sci 2016; 6: 18-26.
[http://dx.doi.org/10.7324/JAPS.2016.60903]
[28]
Yin J, Hou Y, Yin Y, Song X. Selenium-coated nanostructured lipid carriers used for oral delivery of berberine to accomplish a synergic hypoglycemic effect. Int J Nanomedicine 2017; 12: 8671-80.
[http://dx.doi.org/10.2147/IJN.S144615]
[29]
Ahmed A, Ghourab M, Gad S, et al. The application of Plackett-Burman design and response surface methodology for optimization of formulation variables to produce Piroxicam niosomes. Int J Drug Dev Res 2013; 5: 121-30.
[30]
Youssef A, Dudhipala N, Majumdar S. Ciprofloxacin loaded nanostructured lipid carriers incorporated into in-situ gels to improve management of bacterial endophthalmitis. Pharmaceutics 2020; 12(6): 572.
[http://dx.doi.org/10.3390/pharmaceutics12060572]
[31]
Vieira R, Severino P, Nalone LA, et al. Sucupira oil-loaded nanostructured lipid carriers (NLC): lipid screening, factorial design, release profile, and cytotoxicity. Molecules 2020; 25(3): 685.
[http://dx.doi.org/10.3390/molecules25030685]
[32]
Shimojo AAM, Fernandes ARV, Ferreira NRE, Sanchez-Lopez E, Santana MHA, Souto EB. Evaluation of the influence of process parameters on the properties of resveratrol-loaded NLC using 22 full factorial design. Antioxidants 2019; 8(8): 272.
[http://dx.doi.org/10.3390/antiox8080272]
[33]
Das S, Ghosh S, De AK, Bera T. Oral delivery of ursolic acid-loaded nanostructured lipid carrier coated with chitosan oligosaccharides: development, characterization, in vitro and in vivo assessment for the therapy of leishmaniasis. Int J Biol Macromol 2017; 102: 996-1008.
[http://dx.doi.org/10.1016/j.ijbiomac.2017.04.098]
[34]
El Assasy AEI, Younes NF, Makhlouf AIA. Enhanced oral absorption of amisulpride via a nanostructured lipid carrier-based capsules: development, optimization applying the desirability function approach and in vitro pharmacokinetic study. AAPS PharmSciTech 2019; 20(2): 82.
[http://dx.doi.org/10.1208/s12249-018-1283-x]
[35]
Dong Z, Iqbal S, Zhao Z. Preparation of ergosterol-loaded nanostructured lipid carriers for enhancing oral bioavailability and antidiabetic nephropathy effects. AAPS PharmSciTech 2020; 21(2): 64.
[http://dx.doi.org/10.1208/s12249-019-1597-3]
[36]
Pereira RR, Testi M, Rossi F, et al. Ucuùba (Virola surinamensis) Fat-based nanostructured lipid carriers for nail drug delivery of ketoconazole: development and optimization using box-behnken design. Pharmaceutics 2019; 11(6): 284.
[http://dx.doi.org/10.3390/pharmaceutics11060284]
[37]
Pokharkar V, Patil-Gadhe A, Kaur G. Physicochemical and pharmacokinetic evaluation of rosuvastatin loaded nanostructured lipid carriers: influence of long-and medium-chain fatty acid mixture. J Pharm Investig 2018; 48: 465-76.
[http://dx.doi.org/10.1007/s40005-017-0342-8]
[38]
Swidan SA, Ghonaim HM, Samy AM, et al. Comparative study of solid lipid nanoparticles and nanostructured lipid carriers for in vitro Paclitaxel delivery. J Chem Pharm Res 2016; 8: 482-93.
[39]
Hąc-Wydro K, Wydro P. The influence of fatty acids on model cholesterol/phospholipid membranes. Chem Phys Lipids 2007; 150(1): 66-81.
[http://dx.doi.org/10.1016/j.chemphyslip.2007.06.213]
[40]
Cirri M, Maestrini L, Maestrelli F, et al. Design, characterization and in vivo evaluation of nanostructured lipid carriers (NLC) as a new drug delivery system for hydrochlorothiazide oral administration in pediatric therapy. Drug Deliv 2018; 25(1): 1910-21.
[http://dx.doi.org/10.1080/10717544.2018.1529209]
[41]
Witayaudom P, Klinkesorn U. Effect of surfactant concentration and solidification temperature on the characteristics and stability of nanostructured lipid carrier (NLC) prepared from rambutan (Nephelium lappaceum L.) kernel fat. J Colloid Interface Sci 2017; 505: 1082-92.
[http://dx.doi.org/10.1016/j.jcis.2017.07.008]
[42]
Prabahar K, Udhumansha U, Qushawy M. Optimization of thiolated chitosan nanoparticles for the enhancement of in vivo hypoglycemic efficacy of sitagliptin in streptozotocin-induced diabetic rats. Pharmaceutics 2020; 12(4): 300.
[http://dx.doi.org/10.3390/pharmaceutics12040300]
[43]
Cao H, Liao S, Zhong W, et al. Synthesis, characterization, and biological evaluations of 1, 3, 5-triazine derivatives of metformin cyclization with berberine and magnolol in the presence of sodium methylate. Molecules 2017; 22(10): 1752.
[http://dx.doi.org/10.3390/molecules22101752]
[44]
Jadhav SB, Reddy PS, Narayanan KL, Bhosale PN. Development of RP-HPLC, stability indicating method for degradation products of linagliptin in presence of metformin HCl by applying 2 level factorial design; and identification of impurity-VII, VIII and IX and synthesis of impurity-VII. Sci Pharm 2017; 85(3): 25.
[http://dx.doi.org/10.3390/scipharm85030025]
[45]
Chu CC, Tan CP, Nyam KL. Development of nanostructured lipid carriers (NLCs) using pumpkin and kenaf seed oils with potential photoprotective and antioxidative properties. Eur J Lipid Sci Technol 2019; 1211900082
[http://dx.doi.org/10.1002/ejlt.201900082]
[46]
VERMA PK. Preparation and characterization of metformin loaded stearic acid coupled F127 nanoparticles. Asian J Pharm Clin Res 2018; 11: 212-7.
[http://dx.doi.org/10.22159/ajpcr.2018.v11i8.26444]
[47]
Dantas IL, Bastos KTS, Machado M, et al. Influence of stearic acid and beeswax as solid lipid matrix of lipid nanoparticles containing tacrolimus. J Therm Anal Calorim 2018; 132: 1557-66.
[http://dx.doi.org/10.1007/s10973-018-7072-7]
[48]
Latif FM, Teo YY, Misran M, et al. Formulation and physicochemical properties of nanostructured lipid carriers from beeswax and rosemary oil as a drug carrier. Warasan Khana Witthayasat Maha Witthayalai Chiang Mai 2020; 47: 114-26.
[49]
Soleimanian Y, Goli SAH, Varshosaz J, Sahafi SM. Formulation and characterization of novel nanostructured lipid carriers made from beeswax, propolis wax and pomegranate seed oil. Food Chem 2018; 244: 83-92.
[http://dx.doi.org/10.1016/j.foodchem.2017.10.010]
[50]
Jansook P, Fülöp Z, Ritthidej GC. Amphotericin B loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carrier (NLCs): physicochemical and solid-solution state characterizations. Drug Dev Ind Pharm 2019; 45(4): 560-7.
[http://dx.doi.org/10.1080/03639045.2019.1569023]

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