Deepak Patil, Seema Pattewar, Sarvesh Palival, Gargi Patil, Swapnil Sharma
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Deepak Patil1*, Seema Pattewar1, 2, Sarvesh Palival1, Gargi Patil3, Swapnil Sharma1
1Department of Pharmacy, Banasthali Vidyapith, Banasthali, Rajasthan- 304 022, India.
2Sanjivani Institute of Pharmacy and Research, Kopargaon- 423 603, India.
3Institute of Chemical Technology, Marathwada campus, Jalna- 431203, India.
Volume - 14,
Issue - 12,
Year - 2021
The aim of present study is to investigate the potential of nanostructured lipid carriers (NLCs) in improving the oral bioavailability of quetiapine fumarate, a second-generation antipsychotic drug. Quetiapine Fumarate (QF) loaded NLC were prepared by hot homogenization followed by an ultrasonication method. Response surface methodology - central composite design (CCD) was used to systemically examine the influence of concentration of capmul MCM EP, concentration of poloxamer 188 and concentration of egg lecithin on particle size (PS) and % entrapment efficiency (% EE) and to optimize the NLC formulation. The CCD consists of three factored design with five levels, plus and minus alpha (axial points), plus and minus 1 (factorial points) and the centre point. A mathematical relationship between variables was created by using Design Expert software Version 12. The statistical evaluations revealed that three independent variables were the important factors that affected the PS and % EE of QF loaded NLC. The best fitted mathematical model was linear and quadratic for PS and % EE respectively. The optimized formulations found with 218.1±0.14nm of PS and 93±0.16% of % EE. Results illustrated the superiority of developed QF loaded NLC formulation as a stable drug delivery system, providing better bioavailability with the possibility of better treatment for psychological disorders.
Cite this article:
Deepak Patil, Seema Pattewar, Sarvesh Palival, Gargi Patil, Swapnil Sharma. Fabrication and characterization of nanostructured lipid carrier system for effective delivery of poorly water-soluble drug quetiapine fumarate. Research Journal of Pharmacy and Technology. 2021; 14(12):6235-4. doi: 10.52711/0974-360X.2021.01079
Deepak Patil, Seema Pattewar, Sarvesh Palival, Gargi Patil, Swapnil Sharma. Fabrication and characterization of nanostructured lipid carrier system for effective delivery of poorly water-soluble drug quetiapine fumarate. Research Journal of Pharmacy and Technology. 2021; 14(12):6235-4. doi: 10.52711/0974-360X.2021.01079 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2021-14-12-9
1. Merikangas KR, Akiskal HS, Angst J, et al. Lifetime and 12-month prevalence of bipolar spectrum disorder in the national comorbidity survey replication. Archives of General Psychiatry. 2007; 64(5):543-552.
2. Grunze H, Vieta E, Goodwin GM, et al. The World Federation of Societies of Biological Psychiatry (WFSBP) Guidelines for the Biological Treatment of Bipolar Disorders: Update 2010 on the treatment of acute bipolar depression. World Journal of Biological Psychiatry. 2010; 11(2):81-109.
3. Yatham LN, Kennedy SH, Parikh SV. Canadian network for mood and anxiety treatments (CANMAT) and international society for bipolar disorders (ISBD) collaborative update of CANMAT guidelines for the management of patients with bipolar disorder: update. Bipolar Disorders. 2013; 15(1):1-44.
4. Mehetre GD, Patki SS, Thenge RR, et al. Quetiapine Fumarate Buccoadhesive Tablet- Formulation and In Vitro Evaluation. Research Journal of Pharmacy and Technology. 2020; 13(11):5095-5102.
5. Arulappa RX, Sundarapandian M, Venkataraman S, et al. Spectrophotometric Determination of Quetiapine Fumarate in Bulk and Dosage Form. Research Journal of Pharmacy and Technology. 2009; 2(4):884-885.
6. Patel TM, Gohel MC. Development of Extended Release Pellets of Quetiapine Fumarate by using HPMC and Eudragit RSPO. Research Journal of Pharmacy and Technology. 2014; 7(7):771-775.
7. Doppalapudi S, Suryadevara V, Yallam S et al. Formulation and Pharmacodynamic Evaluation of Quetiapine Solid Dispersions using Plasdone K-29/32 as Carrier. Research Journal of Pharmacy and Technology. 2020; 13(5):2359-2365.
8. Parvathi M, Prathyusha A, Kiran RS, et al. Preparation and evaluation of Quetiapine Fumarate microemulsions: a novel delivery system. Asian Journal of Pharmaceutical and Clinical Research. 2014; 7(1):208-13.
9. Babu AK, Ramana MV. In vitro and in vivo evaluation of quetiapine fumarate controlled gastroretentive floating drug delivery system. International Journal of Drug Delivery. 2016; 8 (1): 12-22.
10. Olbrich C, Gessner A, Schroder W, et al. Lipid-drug conjugates nanoparticles of the hydrophilic drug diminazene - cytotoxicity testing and mouse serum adsorption. Journal of Controlled Release. 2004; 96(3): 425-35.
11. Das RJ, Baishya K, Pathak K. Recent advancement of lipid drug conjugates as nanoparticulate drug delivery system. International research journal of pharmacy. 2013; 4(1): 73-78.
12. Radtke M, Souto EB, Muller RH. Nanostructured lipid carriers: a novel generation of solid lipid drug carriers. Pharmaceutical Technology Europe. 2005; 17(4):45-50.
13. Cavalli R, Caputo O, Gasco MR. Solid lipospheres of doxorubicin and idarubicin. International Journal of Pharmaceutics.1993; 89:R9–R12.
14. Sarangi MK, Padhi S. Solid lipid nanoparticles- a review. Journal of Critical Reviews. 2016; 3(3): 5-12.
15. Baviskar A, Hiremath S, Akul M, et al. Effect of Lipids and Surfactants on Solid Lipid Nanoparticle Engineering. Research Journal of Pharmacy and Technology. 2011; 4(4):521-526.
16. Bornare AS, Saudagar RB. Nanostructured Lipid Carrier (NLC): A Modern Approach for Transdermal Drug Delivery. Research Journal of Pharmacy and Technology.2017; 10(8):2784-2792.
17. Sarma A, Das MK, Chakraborty T, et al. Nanostructured lipid carriers (NLCs)-based intranasal Drug Delivery System of Tenofovir disoproxil fumerate (TDF) for brain targeting. Research Journal of Pharmacy and Technology.2020; 13(11):5411-5424.
18. Jaiswal A, Senthil V, Das TK. Design and Development of Valsartan Loaded Nanostructured Lipid Carrier for the Treatment of Diabetic wound Healing. Research Journal of Pharmacy and Technology.2019; 12(6):2922-2928.
19. Majumdar A, Dubey N, Dubey N. Cisplatin loaded Nano Lipid Carriers for the Treatment of Skin Cancer. Research Journal of Pharmacy and Technology.2020; 13(3):1483-1488.
20. Bakthavachalam A, Remya PN, Damodharan N. Review on Solid lipid nanoparticles. Research Journal of Pharmacy and Technology.2020; 13(9):4430-4434.
21. Shah B, Khunt D, Misra M, et al. Non-invasive intranasal delivery of quetiapine fumarate loaded microemulsion for brain targeting: Formulation, physicochemical and pharmacokinetic consideration. European Journal of Pharmaceutical Sciences. 2016; 91:196-207.
22. Sansare V, Pathak G, Zambharakar B, et al. Box-behnken study design for optimization of clotrimazole loaded nanostructured lipid carriers. World Journal of Pharmaceutical Sciences. 2019; 7(2): 92-104.
23. Talele SG, Derle DV. Solubility and thermodynamic modeling of quetiapine fumarate in self nanoemulsifying drug delivery system (SNEDDS). International Journal of Applied Pharmaceutics. 2018; 10(4):127-132.
24. Shah B, Khunt D, Misra M, et al. Non-invasive intranasal delivery of quetiapine fumarate loaded microemulsion for brain targeting: Formulation, physicochemical and pharmacokinetic consideration. European Journal of Pharmaceutical Sciences. 2016; 91:196-207.
25. Khunt D, Shah B, Misra M. Role of butter oil in brain targeted delivery of quetiapine fumarate microemulsion via intranasal route. Journal of Drug Delivery Science and Technology. 2017; doi: 10.1016/j.jddst.2017.05.004.
26. Mu H, Holm R, Mullertz A. Lipid-based formulations for oral administration of poorly water-soluble drugs. International Journal of Pharmaceutics. 2013; 453(1):215-24.
27. Sneh P, Koland M, Kumari SN. Nanoemulsion components screening of quetiapine fumarate: effect of surfactant and co surfactant. Asian Journal of Pharmaceutical and Clinical Research. 2015; 8(6): 136-140.
28. Lohan S, Sharma S, Murthy RR. Formulation and evaluation of solid lipid nanoparticles of quetiapine fumarate and quetiapine hemifumarate for brain delivery in rat model. Pharmaceutical Nanotechnology. 2013; 1: 239-247.
29. Narala A, Veerabrahma K. Preparation, characterization and evaluation of quetiapine fumarate solid lipid nanoparticles to improve the oral bioavailability. Journal of Pharmaceutics. 2013; 2013:1-7. Article ID 265741
30. Yuan H, Wang LL, Du YZ, et al. Preparation and characteristics of nanostructured lipid carriers for control-releasing progesterone by melt-emulsification. Colloids and Surfaces B: Biointerfaces. 2007; 60: 174-179.
31. Patel RJ, Patel ZP. Formulation optimization and evaluation of nanostructured lipid carriers containing valsartan. International journal of pharmaceutical sciences and nanotechnology. 2013; 6(2):2077-2086.
32. Kim BD, Na K, Choi HK. Preparation and characterization of solid lipid nanoparticles (SLN) made of cacao butter and curdlan. European Journal of Pharmaceutical Sciences. 2005; 24, 199-205.
33. Aland R, Ganesan M, Rao PR. In vivo evaluation of tazarotene solid lipid nanoparticles gel for topical delivery. International journal of pharmaceutical sciences and drug research. 2019; 11(1): 45-50.
34. Khan AA, Mudassir J, Akhtar S, et al. Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. Pharmaceutics. 2019; 11(97):1-19.
35. Emami J, Rezazadeh M, Varshosaz J, et al. Formulation of LDL targeted nanostructured lipid carriers loaded with paclitaxel: A detailed study of preparation, freeze drying condition, and in vitro cytotoxicity. Journal of Nanomaterials. 2012; 2012:1-10. Article ID 358782. https://doi.org/10.1155/2012/358782.
36. Fonte P, Soares S, Costa A, et al. Effect of cryoprotectants on the porosity and stability of insulin-loaded PLGA nanoparticles after freeze-drying. Biomatter. 2012; 2(4):329-339.
37. Thakkar H, Nangesh J, Parmar M, et al. Formulation and characterization of lipid-based drug delivery system of raloxifene-micro emulsion and self-micro emulsifying drug delivery system. Journal of Pharmacy And Bioallied Sciences. 2011; 3(3): 442-448.
38. Jawahar N, Hingarh PK, Arun R, et al. Enhanced oral bioavailability of an antipsychotic drug through nanostructured lipid carriers. International Journal of Biological Macromolecules. 2018; 110:269-275.
39. Madane RG, Mahajan HS. Curcumin-loaded nanostructured lipid carriers (NLCs) for nasal administration: design, characterization, and in vivo study. Drug Delivery. 2015. DOI: 10.3109/10717544.2014.975382
40. Khosa A, Reddi S, Saha RN. Nanostructured lipid carriers for site-specific drug delivery. Biomedicine & Pharmacotherapy. 2018; 103:598-613.
41. Albekery MA, Alharbi KT, Alarifi S, et al. Optimization of a nanostructured lipid carriers system for enhancing the biopharmaceutical properties of valsartan. Digest Journal of Nanomaterials and Biostructures. 2017; 12(2): 381 -389.
42. Joshi M, Patravale V. Formulation and evaluation of nanostructured lipid carrier (NLC)-based gel of valdecoxib. Drug Development and Industrial Pharmacy. 2006; 32(8):911-918.
43. Mohebbi M, Zardini AA, Farhoosh R, et al. Production and characterization of nanostructured lipid carriers and solid lipid nanoparticles containing lycopene for food fortification. Journal of food science and technology. 2018; 55(1):287-298.
44. Potu AR, Pujari N, Burra S, et al. Formulation and evaluation of buccoadhesive quetiapine fumarate tablets. Brazilian Journal of Pharmaceutical Sciences. 2012; 48(2):335-347.
45. Bharathi C, Prabahar KJ, Prasad CS, et al. Identification, isolation, synthesis and characterization of impurities of quetiapine fumarate. Die Pharmazie. 2008, 63(1):14-19.
46. Shahe M, Chetty M, Murthy KVR. Preformulation studies of quetiapine fumarate. Journal of Pharmacy Research. 2012; 5(1):672-677.
47. Sahu D, Rana AC. Development and in vitro evaluation of quetiapine fumarate sustain release tablets. International Journal of Pharmtech Research. 2010; 2(4):2535-2543.
48. Fang JY, Fang CL, Al-Suwayeh SA. Nanostructured lipid carriers (NLCs) for drug delivery and targeting. Recent Patents on Nanotechnology. 2013; 7:41-55.
49. Patel RJ, Patel ZP. Formulation optimization and evaluation of nanostructured lipid carriers containing valsartan. International journal of pharmaceutical sciences and nanotechnology. 2013; 6(2):2077-2086.
50. Motwani SK, Chopra S, Talegaonkar S, et al. Chitosan - sodium alginate nanoparticles as submicroscopic reservoirs for ocular delivery: Formulation, optimization and in vitro characterization. European Journal Pharmaceutical Biopharmaceutics. 2008; 68(3):513-525.
51. Gadad AP, Tigadi SG, Mallappa P, et al. Rosuvastatin loaded nanostructured lipid carrier: For enhancement of oral bioavailability. Indian Journal of Pharmaceutical Education and Research. 2016; 50(4): 605-611.
52. Mishra B, Mittal P, Vardhan H, et al. Genistein-loaded nanostructured lipid carriers for intravenous administration: A quality by design based approach. International research journal of pharmacy. 2019; 10(1):119-134.
53. Swidan SA, Mansour ZN, Mourad ZA, et al. DOE, formulation, and optimization of repaglinide nanostructured lipid carriers. Journal of Applied Pharmaceutical Science. 2018; 8(10):008-016.
54. Patil-Gadhe A, Kyadarkunte A, Patole M, et al. Montelukast-loaded nanostructured lipid carriers: Part II pulmonary drug delivery and in vitro–in vivo aerosol performance. European Journal of Pharmaceutics and Biopharmaceutics. 2014; 88(1):169-177.
55. Shah NV, Seth AK, Balaraman R, et al. Nanostructured lipid carriers for oral bioavailability enhancement of raloxifene: Design and in vivo study. Journal of Advanced Research. 2016; 7:423-434.
56. Ahn JH, Kim YP, Lee YM, et al. Optimization of microencapsulation of seed oil by response surface methodology. Food Chemistry. 2008; 107:98-105.
57. Hu FQ, Jiang SP, Du YZ, et al. Preparation and characterization of stearic acid nanostructured lipid carriers by solvent diffusion method in an aqueous system. Colloids Surface B: Biointerfaces. 2005; 5:167-173.
58. Tamjidi F, Shahedi M, Varshosaz J, et al. Nanostructured lipid carriers (NLC): A potential delivery system for bioactive food molecules. Innovative Food Science and Emerging Technologies. 2013; 19:29-43.
59. Dai W, Zhang D, Duan C, et al. Preparation and characteristics of oridonin- loaded nanostructured lipid carriers as a controlled-release delivery system. Journal of Microencapsulation. 2010; 27(3): 234-241.
60. Mandpe L, Pokharkar V. Quality by design approach to understand the process of optimization of iloperidone nanostructured lipid carriers for oral bioavailability enhancement. Pharmaceutical development and Technology. 2013; Early Online: 1-10. DOI: 10.3109/10837450.2013.867445.
61. Muller RH, Keck CM. Challenges and solutions for the delivery of biotech drugs- a review of drug nanocrystal technology and lipid nanoparticles. Journal of Biotechnology. 2004; 113(1-3): 151-170.
62. Zhu J, Zhuang P, Luan L, et al. Preparation and characterization of novel nanocarriers containing krill oil for food application. Journal of Functional Food. 2015; 19: 902-912.
63. Ali H, El-Sayed K, Sylvester PW, et al. Molecular interaction and localization of tocotrienol-rich fraction (TRF) within the matrices of lipid nanoparticles: evidence studies by differential scanning calorimetry (DSC) and proton nuclear magnetic resonance spectroscopy (H NMR). Colloids and Surfaces B: Bio interfaces. 2010; 77:286-297.
64. Soleimanian Y, Goli SAH, Varshosaz J, et al. Formulation and characterization of novel nanostructured lipid carriers made from beeswax, propolis wax and pomegranate seed oil. Food Chemistry. 2018; 244:83-92.
65. Kudarha R, Dhas NL, Pandey A, et al. Box–behnken study design for optimization of bicalutamide-loaded nanostructured lipid carrier: stability assessment. Pharmaceutical Development and Technology. 2014; 20(5):608-618.
66. Gordillo-Galeano A, Mora-Huertas CE. Solid lipid nanoparticles and nanostructured lipid carriers: A review emphasizing on particle structure and drug release. European Journal of Pharmaceutics and Biopharmaceutics. 2018; 133:285-308.
67. Liu J, Gong T, Wang C, et al. Solid lipid nanoparticles loaded with insulin by sodium cholate-phosphatidylcholine-based mixed micelles: preparation and characterization. International Journal of Pharmaceutics. 2007; 340:153-162.
68. Tiwari R, Pathak K. Nanostructured lipid carrier versus solid lipid nanoparticles of simvastatin: comparative analysis of characteristics, pharmacokinetics and tissue uptake. International Journal of Pharmaceutics. 2011; 415(1-2):232-243.
69. Pimpalshende PM, Gupta RN. Formulation and in-vitro drug released mechanism of CNS acting venlafaxine nanostructured lipid carrier for major depressive disorder. Indian Journal of Pharmaceutical Education and Research. 2018; 52(2):230-240.
70. Das S, Ng WK, Tan RB. Are nanostructured lipid carriers (NLCs) better than solid lipid nanoparticles (SLNs): Development, characterizations and comparative evaluations of clotrimazole-loaded SLNs and NLCs? European Journal of Pharmaceutical Sciences. 2012; 47(1):139-51.
71. Hamishehkar H, Pezeshki A, Ghanbarzadeh B, et al. Encapsulation of vitamin a palmitate in nanostructured lipid carrier (NLC) - effect of surfactant concentration on the formulation properties. Advanced Pharmaceutical Bulletin. 2014; 4(2):563-568.
72. Sumit K, Bhatt DC. Preparation and Evaluation of Isoniazid Loaded Chitosan Nanostructures. Research Journal of Pharmacy and Technology. 2020; 13(9):4219-4223. doi: 10.5958/0974-360X.2020.00745.3