OPTIMIZATION AND CHARACTERIZATION OF RIVASTIGMINE-LOADED NANOSTRUCTURED LIPID CARRIERS
DOI:
https://doi.org/10.22159/ijcpr.2021v13i3.42093Keywords:
NLCs, Rivastigmine, SEM, AFM, DSC, FTIRAbstract
Objective: The objective of the present study was to develop Nanostructured lipid carriers (NLCs) for improvement in the oral bioavailability of RT.
Methods: RT-loaded NLCs were prepared by high shear homogenization technique using fish oil and flaxseed oil respectively. The prepared RT-NLCs were characterized using a phase-contrast microscope, scanning electron microscope (SEM), atomic force microscope (AFM), Fourier transform-infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Further, particle size, entrapment efficiency and sustained release of the drug were also studied.
Results: SEM results revealed that the RT-NLCs were spherical in shape with a smooth surface. AFM results confirmed the formation of spherical particle dispersions by the NLCs in nanoscale. FTIR spectroscopy and DSC analyses revealed that there is no chemical interaction between the ingredients of RT-NLCs. The particle size of the RT-NLCs was found to be exponentially decreased with the increase in a surfactant solution.
Conclusion: The results confirmed pronounced improvement in entrapment efficiency of optimized formulation of RT-NLCs. In vitro, drug release studies showed that RT-NLCs were capable of releasing the drug in a sustained manner. The experimental results showed that the NLCs are potential carriers for providing sustained delivery of rivastigmine.
Downloads
Download data is not yet available.
References
1. Petrasek T, Skurlova M, Maleninska K, Vojtechova I, Kristofikova Z, Matuskova H, et al. A rat model of Alzheimer’s disease based on Abeta42 and pro-oxidative substances exhibits cognitive deficit and alterations in glutamatergic and cholinergic neurotransmitter systems. Frontiers Aging Neurosci 2016;20:8-83.
2. Kalaria RN, Maestre GE, Arizaga R, Friedland RP, Galasko D, Hall K, et al. Alzheimer's disease and vascular dementia in developing countries: prevalence, management, and risk factors. Lancet Neurol 2008;7:812-26.
3. Jack CR, Wiste HJ, Lesnick TG, Weigand SD, Knopman DS, Vemuri P, et al. Brain ?-amyloid load approaches a plateau. Neurology 2013;80:890-6.
4. Banks WA. From blood-brain barrier to blood-brain interface: new opportunities for CNS drug delivery. Nat Rev Drug Discovery 2016;15:275.
5. Pardridge WM. Alzheimer's disease drug development and the problem of the blood-brain barrier. Alzheimer's Dementia 2009;5:427-32.
6. Raschetti R, Albanese E, Vanacore N, Maggini M. Cholinesterase inhibitors in mild cognitive impairment: a systematic review of randomised trials. PLoS Med 2007;4:338.
7. Pharmaceuticals N. Inventor; Excelon monograph, USA; 2004.
8. Ismail MF, ElMeshad AN, Salem NA. Potential therapeutic effect of nano-based formulation of rivastigmine on rat model of Alzheimer’s disease. Int J Nanomed 2013;8:393.
9. Arumugam K, Subramanian G, Mallayasamy S, Averineni R, Reddy M, Udupa N. A study of rivastigmine liposomes for delivery into the brain through intranasal route. Acta Pharm 2008;58:287-97.
10. Joshi SA, Chavhan SS, Sawant KK. Rivastigmine-loaded PLGA and PBCA nanoparticles: preparation, optimization, characterization, in vitro and pharmacodynamic studies. Eur J Pharm Biopharm 2010;76:189-99.
11. Sahni JK, Doggui S, Ali J, Baboota S, Dao L, Ramassamy C. Neurotherapeutic applications of nanoparticles in Alzheimer's disease. J Controlled Release 2011;152:208-31.
12. Saraiva C, Praça C, Ferreira R, Santos T, Ferreira L, Bernardino L. Nanoparticle-mediated brain drug delivery: overcoming blood-brain barrier to treat neurodegenerative diseases. J Controlled Release 2016;235:34-47.
13. Tapeinos C, Battaglini M, Ciofani G. Advances in the design of solid lipid nanoparticles and nanostructured lipid carriers for targeting brain diseases. J Controlled Release 2017;264:306-32.
14. Velmurugan R, Selvamuthukumar S. Development and optimization of ifosfamide nanostructured lipid carriers for oral delivery using response surface methodology. Appl Nanosci 2016;6:159-73.
15. Naseri N, Valizadeh H, Zakeri Milani P. Solid lipid nanoparticles and nanostructured lipid carriers: structure, preparation and application. Adv Pharm Bull 2015;5:305.
16. Fang CLA, Al-Suwayeh S, Fang JY. Nanostructured lipid carriers (NLCs) for drug delivery and targeting. Recent Patents Nanotechnol 2013;7:41-55.
17. Md S, Kit B, Jagdish S, David DJ, Pandey M, Chatterjee LA. Development and in vitro evaluation of a zerumbone loaded nanosuspension drug delivery system. Crystals 2018;8:286.
18. Chen ZY, Cao J, Xie L, Li XF, Yu ZH, Tong WY. Construction of leaky strains and extracellular production of exogenous proteins in recombinant Escherichia coli. Microbial Biotechnol 2014;7:360-70.
19. Brzobohaty O, Siler M, Trojek J, Chvatal L, Karasek V, Patak A, et al. Three-dimensional optical trapping of a plasmonic nanoparticle using low numerical aperture optical tweezers. Sci Rep 2015;29:8106.
20. Mishra P, Tyagi S. Surface analysis of gutta percha after disinfecting with sodium hypochlorite and silver nanoparticles by atomic force microscopy: an in vitro study. Dental Res J 242;15:242.
21. Kumar BS, Panda PK. 1D water chain stabilized by meso-expanded calix [4] pyrrole. Cryst Eng Comm 2014;16:8669-72.
22. Janes KA, Fresneau MP, Marazuela A, Fabra A, Alonso MJ. Chitosan nanoparticles as delivery systems for doxorubicin. J Controlled Release 2001;73:255-67.
23. Li R, Song XN, Zhang H, Dai WB, He B, Zheng Y, et al. The integrity study on PEG-PCL micelles transcellular transported across MDCK epithelial cell monolayer using FRET technology. Yao Xue Xue Bao= Acta Pharm Sinica 2016;51:1316-24.
24. Shete H, Patravale V. Long chain lipid based tamoxifen NLC. Part I: preformulation studies, formulation development and physicochemical characterization. Int J Pharm 2013;454:573-83.
25. Joshi M, Pathak S, Sharma S, Patravale V. Design and in vivo pharmacodynamic evaluation of nanostructured lipid carriers for parenteral delivery of artemether: Nanoject. Int J Pharm 2008;364:119-26.
26. Subedi RK, Kang KW, Choi HK. Preparation and characterization of solid lipid nanoparticles loaded with doxorubicin. Euro J Pharm Sci 2009;37:508-13.
27. Gaba B, Fazil M, Khan S, Ali A, Baboota S, Ali J. Nanostructured lipid carrier system for topical delivery of terbinafine hydrochloride. Bull Faculty Pharm Cairo University 2015;53:147-59.
28. Bunjes H, Unruh T. Characterization of lipid nanoparticles by differential scanning calorimetry, X-ray and neutron scattering. Adv Drug Delivery Rev 2007;59:379-402.
29. Gupta H, Aqil M, Khar RK, Ali A, Bhatnagar A, Mittal G. Sparfloxacin-loaded PLGA nanoparticles for sustained ocular drug delivery. Nanomed: Nanotechnol Biol Med 2010;6:324-33.
30. 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;7:423-34.
31. Jia L, Zhang D, Li Z, Duan C, Wang Y, Feng F, et al. Nanostructured lipid carriers for parenteral delivery of silybin: Biodistribution and pharmacokinetic studie. Colloids Surf B 2010;80:213-8.
32. Elmowafy M, Ibrahim HM, Ahmed MA, Shalaby K, Salama A, Hefesha H. Atorvastatin-loaded nanostructured lipid carriers (NLCs): strategy to overcome oral delivery drawbacks. Drug Delivery 2017;24:932-41.
33. Jansook P, Pichayakorn W, Ritthidej GC. Amphotericin B-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carrier (NLCs): effect of drug loading and biopharmaceutical characterizations. Drug Dev Industrial Pharm 2018;44:1693-700.
34. Kraisit P, Sarisuta N. Development of triamcinolone acetonide-loaded nanostructured lipid carriers (NLCs) for buccal drug delivery using the Box-Behnken design. Molecules 2018;23:982.
35. Dudhipala N, Janga KY, Gorre T. Comparative study of nisoldipine-loaded nanostructured lipid carriers and solid lipid nanoparticles for oral delivery: preparation, characterization, permeation and pharmacokinetic evaluation. Artificial Cells Nanomed Biotechnol 2018;46:616-25.
36. Montoto SS, Sbaraglini ML, Talevi A, Couyoupetrou M, Di Ianni M, Pesce GO, et al. Carbamazepine-loaded solid lipid nanoparticles and nanostructured lipid carriers: physicochemical characterization and in vitro/in vivo evaluation. Colloids Surf B 2018;167:73-81.
37. Prajapati JB, Verma SD, Patel AA. Oral bioavailability enhancement of agomelatine by loading into nanostructured lipid carriers: peyer’s patch targeting approach. Int J Nanomed 2018;13:35-8.
2. Kalaria RN, Maestre GE, Arizaga R, Friedland RP, Galasko D, Hall K, et al. Alzheimer's disease and vascular dementia in developing countries: prevalence, management, and risk factors. Lancet Neurol 2008;7:812-26.
3. Jack CR, Wiste HJ, Lesnick TG, Weigand SD, Knopman DS, Vemuri P, et al. Brain ?-amyloid load approaches a plateau. Neurology 2013;80:890-6.
4. Banks WA. From blood-brain barrier to blood-brain interface: new opportunities for CNS drug delivery. Nat Rev Drug Discovery 2016;15:275.
5. Pardridge WM. Alzheimer's disease drug development and the problem of the blood-brain barrier. Alzheimer's Dementia 2009;5:427-32.
6. Raschetti R, Albanese E, Vanacore N, Maggini M. Cholinesterase inhibitors in mild cognitive impairment: a systematic review of randomised trials. PLoS Med 2007;4:338.
7. Pharmaceuticals N. Inventor; Excelon monograph, USA; 2004.
8. Ismail MF, ElMeshad AN, Salem NA. Potential therapeutic effect of nano-based formulation of rivastigmine on rat model of Alzheimer’s disease. Int J Nanomed 2013;8:393.
9. Arumugam K, Subramanian G, Mallayasamy S, Averineni R, Reddy M, Udupa N. A study of rivastigmine liposomes for delivery into the brain through intranasal route. Acta Pharm 2008;58:287-97.
10. Joshi SA, Chavhan SS, Sawant KK. Rivastigmine-loaded PLGA and PBCA nanoparticles: preparation, optimization, characterization, in vitro and pharmacodynamic studies. Eur J Pharm Biopharm 2010;76:189-99.
11. Sahni JK, Doggui S, Ali J, Baboota S, Dao L, Ramassamy C. Neurotherapeutic applications of nanoparticles in Alzheimer's disease. J Controlled Release 2011;152:208-31.
12. Saraiva C, Praça C, Ferreira R, Santos T, Ferreira L, Bernardino L. Nanoparticle-mediated brain drug delivery: overcoming blood-brain barrier to treat neurodegenerative diseases. J Controlled Release 2016;235:34-47.
13. Tapeinos C, Battaglini M, Ciofani G. Advances in the design of solid lipid nanoparticles and nanostructured lipid carriers for targeting brain diseases. J Controlled Release 2017;264:306-32.
14. Velmurugan R, Selvamuthukumar S. Development and optimization of ifosfamide nanostructured lipid carriers for oral delivery using response surface methodology. Appl Nanosci 2016;6:159-73.
15. Naseri N, Valizadeh H, Zakeri Milani P. Solid lipid nanoparticles and nanostructured lipid carriers: structure, preparation and application. Adv Pharm Bull 2015;5:305.
16. Fang CLA, Al-Suwayeh S, Fang JY. Nanostructured lipid carriers (NLCs) for drug delivery and targeting. Recent Patents Nanotechnol 2013;7:41-55.
17. Md S, Kit B, Jagdish S, David DJ, Pandey M, Chatterjee LA. Development and in vitro evaluation of a zerumbone loaded nanosuspension drug delivery system. Crystals 2018;8:286.
18. Chen ZY, Cao J, Xie L, Li XF, Yu ZH, Tong WY. Construction of leaky strains and extracellular production of exogenous proteins in recombinant Escherichia coli. Microbial Biotechnol 2014;7:360-70.
19. Brzobohaty O, Siler M, Trojek J, Chvatal L, Karasek V, Patak A, et al. Three-dimensional optical trapping of a plasmonic nanoparticle using low numerical aperture optical tweezers. Sci Rep 2015;29:8106.
20. Mishra P, Tyagi S. Surface analysis of gutta percha after disinfecting with sodium hypochlorite and silver nanoparticles by atomic force microscopy: an in vitro study. Dental Res J 242;15:242.
21. Kumar BS, Panda PK. 1D water chain stabilized by meso-expanded calix [4] pyrrole. Cryst Eng Comm 2014;16:8669-72.
22. Janes KA, Fresneau MP, Marazuela A, Fabra A, Alonso MJ. Chitosan nanoparticles as delivery systems for doxorubicin. J Controlled Release 2001;73:255-67.
23. Li R, Song XN, Zhang H, Dai WB, He B, Zheng Y, et al. The integrity study on PEG-PCL micelles transcellular transported across MDCK epithelial cell monolayer using FRET technology. Yao Xue Xue Bao= Acta Pharm Sinica 2016;51:1316-24.
24. Shete H, Patravale V. Long chain lipid based tamoxifen NLC. Part I: preformulation studies, formulation development and physicochemical characterization. Int J Pharm 2013;454:573-83.
25. Joshi M, Pathak S, Sharma S, Patravale V. Design and in vivo pharmacodynamic evaluation of nanostructured lipid carriers for parenteral delivery of artemether: Nanoject. Int J Pharm 2008;364:119-26.
26. Subedi RK, Kang KW, Choi HK. Preparation and characterization of solid lipid nanoparticles loaded with doxorubicin. Euro J Pharm Sci 2009;37:508-13.
27. Gaba B, Fazil M, Khan S, Ali A, Baboota S, Ali J. Nanostructured lipid carrier system for topical delivery of terbinafine hydrochloride. Bull Faculty Pharm Cairo University 2015;53:147-59.
28. Bunjes H, Unruh T. Characterization of lipid nanoparticles by differential scanning calorimetry, X-ray and neutron scattering. Adv Drug Delivery Rev 2007;59:379-402.
29. Gupta H, Aqil M, Khar RK, Ali A, Bhatnagar A, Mittal G. Sparfloxacin-loaded PLGA nanoparticles for sustained ocular drug delivery. Nanomed: Nanotechnol Biol Med 2010;6:324-33.
30. 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;7:423-34.
31. Jia L, Zhang D, Li Z, Duan C, Wang Y, Feng F, et al. Nanostructured lipid carriers for parenteral delivery of silybin: Biodistribution and pharmacokinetic studie. Colloids Surf B 2010;80:213-8.
32. Elmowafy M, Ibrahim HM, Ahmed MA, Shalaby K, Salama A, Hefesha H. Atorvastatin-loaded nanostructured lipid carriers (NLCs): strategy to overcome oral delivery drawbacks. Drug Delivery 2017;24:932-41.
33. Jansook P, Pichayakorn W, Ritthidej GC. Amphotericin B-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carrier (NLCs): effect of drug loading and biopharmaceutical characterizations. Drug Dev Industrial Pharm 2018;44:1693-700.
34. Kraisit P, Sarisuta N. Development of triamcinolone acetonide-loaded nanostructured lipid carriers (NLCs) for buccal drug delivery using the Box-Behnken design. Molecules 2018;23:982.
35. Dudhipala N, Janga KY, Gorre T. Comparative study of nisoldipine-loaded nanostructured lipid carriers and solid lipid nanoparticles for oral delivery: preparation, characterization, permeation and pharmacokinetic evaluation. Artificial Cells Nanomed Biotechnol 2018;46:616-25.
36. Montoto SS, Sbaraglini ML, Talevi A, Couyoupetrou M, Di Ianni M, Pesce GO, et al. Carbamazepine-loaded solid lipid nanoparticles and nanostructured lipid carriers: physicochemical characterization and in vitro/in vivo evaluation. Colloids Surf B 2018;167:73-81.
37. Prajapati JB, Verma SD, Patel AA. Oral bioavailability enhancement of agomelatine by loading into nanostructured lipid carriers: peyer’s patch targeting approach. Int J Nanomed 2018;13:35-8.
Published
15-05-2021
How to Cite
GANNA, S., S. M. KOTAKADI, R. A. MOHAMMED, M. I. SHAIK, and J. S. NANNEPAGA. “OPTIMIZATION AND CHARACTERIZATION OF RIVASTIGMINE-LOADED NANOSTRUCTURED LIPID CARRIERS”. International Journal of Current Pharmaceutical Research, vol. 13, no. 3, May 2021, pp. 46-51, doi:10.22159/ijcpr.2021v13i3.42093.
Issue
Section
Original Article(s)
