Author(s):
Kumara Swamy S, Ramesh Alli
Email(s):
kumar4koti@gmail.com , rameshalli567@gmail.com
DOI:
10.52711/2231-5713.2021.00016 
Address:
Kumara Swamy S1*, Ramesh Alli2
1Asst. Professor, Department of Pharmaceutics, Vaagdevi Pharmacy College, Bollikunta, Warangal, Telangana State, India.
2Department of Pharmaceutics, Vaagdevi Pharmacy College, Bollikunta, Warangal, Telangana State, India.
*Corresponding Author
Published In:
Volume - 11,
Issue - 2,
Year - 2021
ABSTRACT:
The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.
Cite this article:
Kumara Swamy S, Ramesh Alli. Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery. Asian Journal of Pharmacy and Technology. 2021; 11(2):97-4. doi: 10.52711/2231-5713.2021.00016
Cite(Electronic):
Kumara Swamy S, Ramesh Alli. Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery. Asian Journal of Pharmacy and Technology. 2021; 11(2):97-4. doi: 10.52711/2231-5713.2021.00016 Available on: https://ajptonline.com/AbstractView.aspx?PID=2021-11-2-1
REFERENCES:
1. Allen TM. Liposomes. Opportunities in drug delivery. Drugs. 1997; 54 (4): 8–14.
2. Dudhipala N. A Comprehensive Review on Solid Lipid Nanoparticles as Delivery Vehicle for Enhanced Pharmacokinetic and Pharmacodynamic Activity of Poorly Soluble Drugs. Int J Pharm Sci Nanotech. 2019; 12: 4421-40.
3. Bakthavachalam A, Remya P N, Damodharan N. Review on Solid lipid nanoparticles. Research J Pharm and Tech. 2020; 13(9): 4430-4434.
4. Palem CR, Reddy ND, Satyanarayana G, Varsha BP. Development and optimization of Atorvastatin calcium-cyclodextrin inclusion complexed oral disintegrating tablets for enhancement of solubility, dissolution, pharmacokinetic and pharmacodynamic activity by central composite design. Int J Pharm Sci Nanotech. 2016; 9(2): 1-1.
5. Giri TK, Desmukh M, Jaiswal A, Tripathi DK. β-Cyclodextrin and Its Derivatives Based Drug Delivery. Research Journal of Pharmaceutical Dosage Forms and Technology. 2010; 2(6): 361-9.
6. Swetha E, Narendar D. Influence of β-cyclodextrin and hydroxypropyl-β-cyclodextrin on enhancement of solubility and dissolution of isradipine. Int J Pharm Sci Nanotech. 2017; 10(3): 3752-3757.
7. Butreddy A, Dudhipala N. Enhancement of solubility and dissolution rate of trandolapril sustained release matrix tablets by liquisolid compact approach. Asian Journal of Pharmaceutic• Oct-Dec. 2015;9(4): 1.
8. Palem CR, Dudhipala NR, Battu SK, Repka MA, Rao Yamsani M. Development, optimization and in vivo characterization of domperidone-controlled release hot-melt-extruded films for buccal delivery. Drug development and industrial pharmacy. 2016 Mar 3; 42(3) : 473-84.
9. Peddapalli H, Dudhipala N, Chinnala KM, Banala N. Transmucosal Delivery of Duloxetine Hydrochloride for Prolonged Release: Preparation, in vitro, ex vivo Characteri-zation and in vitro-ex vivo Correlation. Int J Pharm Sci Nanotech. 2018; 11(5): 29-4258.
10. Palem CR, Gannu R, Doodipala N, Yamsani VV, Yamsani MR. Transmucosal delivery of domperidone from bilayered buccal patches: in vitro, ex vivo and in vivo characterization. Archives of pharmacal research. 2011 Oct 1; 34(10): 1701-10.
11. Palem CR, Dudhipala N, Battu SK, Goda S, Repka MA, Yamsani MR. Combined dosage form of pioglitazone and felodipine as mucoadhesive pellets via hot melt extrusion for improved buccal delivery with application of quality by design approach. Journal of Drug Delivery Science and Technology. 2015 Dec 1; 30: 209-19.
12. Narendar D, Arjun N, Dinesh S, Karthik J. Biopharmaceutical and preclinical studies of efficient oral delivery of zaleplon as semisolid dispersions with self-emulsifying lipid surfactants. Int J Pharm Sci Nanotech. 2016; 9(1): 1-8.
13. Doodipala NR, Sunil R, Rao M. Development of floating matrix tablets of Ofloxacin and Ornidazole in combined dosage form: in vitro and in vivo evaluation in healthy human volunteers. International Journal of Drug Delivery. 2012 Oct 1; 4(4): 462.
14. Dudhipala N, K. Someshwar, N. Arjun and Y. Madhusudan Rao. Quality by design approach for development and optimization of quetiapine fumarate effervescent floating matrix tablets for improved oral delivery. J Pharm Investigation., 2016; 46(3): 253-263.
15. Donthi MR, Dudipala N, Komalla DR, Suram D, Banala N. Design and Evaluation of Floating Multi Unit Mini Tablets (MUMTS) Muco Adhesive Drug Delivery System of Famotidine to Treat Upper Gastro Intestinal Ulcers. Journal of Pharmacovigilance. 2015 Oct 12.
16. Doodipala N, Palem C, Reddy S, Rao Y. Pharmaceutical development and clinical pharmacokinetic evaluation of gastroretentive floating matrix tablets of levofloxacin. Int J Pharm Sci Nanotech. 2011; 4(3): 1461-7.
17. Nagaraj B. Development of Osmotically Controlled Oral Drug Delivery Systems of Tramadol Hydrochloride: Effect of Formulation Variables on In Vitro Release Kinetics. Asian Journal of Pharmaceutics (AJP): Free full text articles from Asian J Pharm. 2016 Sep 10; 10(03).
18. Reddy AB, Reddy ND. Development of multiple-unit floating drug delivery system of clarithromycin: formulation, in vitro dissolution by modified dissolution apparatus, in vivo radiographic studies in human volunteers. Drug research. 2017 Jul; 67(07): 412-8.
19. Krishna VM, Kumar VB, Dudhipala N. In-situ Intestinal absorption and pharmacokinetic investigations of carvedilol loaded supersaturated self-emulsifying drug system. Pharmaceutical nanotechnology. 2020 Jun 1; 8(3): 207-24.
20. Narendar D and Kishan V. Candesartan cilexetil nanoparticles for improved oral bioavailability. Ther deli, 2017; 8(2): 79-88.
21. Butreddy A, Narala A, Dudhipala N. Formulation and characterization of Liquid Crystalline Hydrogel of Agomelatin: In vitro and Ex vivo evaluation. Journal of Applied Pharmaceutical Science. 2015 Sep; 5(09): 110-4.
22. Nagaraj K, Narendar D and Kishan V. Development of olmesartan medoxomil optimized nanosuspension using Box-Behnken design to improve oral bioavailability. Drug Dev Ind Pharm. 2017; 43(7): 1186-1196.
23. Pitta S, Dudhipala N, Narala A, Veerabrahma K. Development and evaluation of zolmitriptan transfersomes by Box-Behnken design for improved bioavailability by nasal delivery. Drug Dev Ind Pharm. 2018; 44(3): 484-92.
24. Narendar D, Riyaz PMD, Ahmed AY, Nagaraj B. Effect of lipid and edge activator concentration on development of Aceclofenac loaded transfersomes gel for transdermal application: in vitro and ex vivo skin permeation. Dru Dev Ind Pharm. 2020. 46(8): 1334-1344.
25. Karri V, Butreddy A, Dudhipala N. Fabrication of Efavirenz Freeze Dried Nanocrystals: Formulation, Physicochemical Characterization, In Vitro and Ex Vivo Evaluation. Advanced Science, Engineering and Medicine. 2015 May 1; 7(5): 385-92.
26. Nagaraj B, Anusha K, Narendar D, Sushma P. Formulation and evaluation of microemulsion-based transdermal delivery of duloxetine hydrochloride. Int J Pharm Sci Nanotech. 2020 Jan 31; 13(1): 4773-82.
27. Corinne Sweeney, Narendar Dudhipala, Ruchi Thakkar, Tabish Mehraj, Sushrut Marathe, Waseem Gul, Mahmoud. A. ElSohly, Brian Murphy, Soumyajit Majumdar. Effect of surfactant concentration and sterilization process on intraocular pressure–lowering activity of Δ9‑tetrahydrocannabinolvaline‑hemisuccinate (NB1111) nanoemulsions. Drug Delivery and Translational Research. 2020 https://doi.org/10.1007/s13346-020-00871-9.
28. Mankar SD, Anjali Dama, M. S. Bhosale, Dr. S. S. Sidhheshwar. Design, development, characterization of solid lipid nanoparticles for oral administration. Research J. Science and Tech. 2020; 12(1): 79-95.
29. Müller RH, Mäder K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery - a review of teh state of teh art. Eur J Pharm Biopharm. 2000 Jul; 50(1): 161-77.
30. Tirumalesh C, Suram D, Dudhipala N, Banala N. Enhanced pharmacokinetic activity of Zotepine via nanostructured lipid carrier system in Wistar rats for oral application. Pharmaceutical Nanotechnology. 2020 Apr 1; 8(2):148-60.
31. Schwarz C, W.Mehnert, J.S.Lucks, R.H.Müller. Solid lipid nanoparticles (SLN) for controlled drug delivery. I. Production, characterization and sterilization. J control rel. 1994; 30(1): 83-96.
32. Nagaraj B, Tirumalesh C, Dinesh S, Narendar D. Zotepine loaded lipid nanoparticles for oral delivery: development, characterization, and in vivo pharmacokinetic studies. Future Journal of Pharmaceutical Sciences. 2020 Dec; 6(1): 1-1.
33. Mehnert W, Mader K. Solid lipid nanoparticles: Production, characterization and applications. Adv Drug Deliv Rev. 2001;47(2-3): 165–96.
34. Dudhipala N. Influence of Solid Lipid Nanoparticles on Pharmaco-dynamic Activity of Poorly Oral Bioavailable Drugs. International Journal of Pharmaceutical Sciences and Nanotechnology. 2020 Jul 11; 13(4): 4979-83.
35. Müller RH, Radtke M, Wissing SA. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations. Adv Drug Deliv Rev. 2002 54 Suppl 1:S 131-55.
36. Forni V, Wuerzner G, Pruijm M, Burnier M. Long-term use and tolerability of irbesartan for control of hypertension. Integrated blood pressure control. 2011; 4:17.
37. Croom KF, Plosker GL. Irbesartan. Drugs. 2008 Aug 1; 68(11): 1543-69.
38. Kamisetti RR, Vinitha Brungi, S. Bennuru, Sr. Cheeli, RM. Gupta Vankadari. Studies on the development of Orally Disintegrating Tablets of Irbesartan. Asian J Pharm Res. 2020; 10(1): 01-07.
39. Narendar D, Kishan V. Pharmacokinetic and pharmacodynamic studies of nisoldipine-loaded solid lipid nanoparticles developed by central composite design. Drug Dev Ind Pharm. 2015; 41 (12), 1968-77.
40. Thulasi Ram D, Subhashis Debnath, M. Niranjan Babu, T. Chakradhar Nath, Thejeswi B. A Review on solid Lipid Nanoparticles. Research J Pharm and Tech. 2012; 5(11): 1359-1368.
41. Usha G, Narendar D, Kishan V. Preparation, characterization and in vivo evaluation of felodipine solid lipid nanoparticles to improve the oral bioavailability. Int J Pharma Sci Nanotech. 2015; 8 (4), 2995-3002.
42. Arun B, Narendar D, Kishan V. Development of olmesartan medoxomil lipid-based nanoparticles and nanosuspension: preparation, characterization and comparative pharmacokinetic evaluation. Artificial cells, nanomed and biotech. 2018; 46(1), 126-137.
43. Narendar D, Kishan V. Candesartan cilexetil loaded solid lipid nanoparticles for oral delivery: characterization, pharmacokinetic and pharmacodynamic evaluation. Drug Deli. 2016; 23 (2), 395-404.
44. Nalini CN, Mathivanan N. A review on analytical methods of irbesartan and its combinations in pharmaceutical dosage forms. Current Pharmaceutical Analysis. 2020 Dec 1; 16(8): 1020-9.
45. Vishal VB, Indrajeet S. Patil, Omkar A. Patil, Srinivas K. Mohite. UV spectroscopy analysis and degradation study of irbesartan. Asian J Pharm Ana. 2018; 8(2): 69-72.
46. Gorre TR, Swetha E, Narendar D. Role of isradipine loaded solid lipid nanoparticles in the pharmacodynamic effect of isradipine in rats. Drug res. 2017; 67(03): 163-169.
47. Rohan RV, Swati S. Talokar, V. R. Salunkhe, C. S. Magdum. formulation development and optimization of simvastatin loaded solid lipid nanoparticles. Asian J Res Pharm Sci. 2017; 7(1): 49-52.
48. Dudhipala N, Ahmed AA. Amelioration of ketoconazole in lipid nanoparticles for enhanced antifungal activity and bioavailability through oral administration for management of fungal infections. Chemistry and Physics of Lipids. 2020; 232: 104953.
49. Ashok P, Meyyanathan SN, Jawahar N, Vadivelan R. Irbesartan formulation and evaluation of loaded solid lipid nanoparticles by microemulsion technique. Asian J Pharm Tech. 2020; 10(4): 228-230.
50. Suvarna G, Narender D, Kishan V. Preparation, characterization and in vivo evaluation of rosuvastatin calcium loaded solid lipid nanoparticles. Int J Pharm Sci Nanotech. 2015; 9: 2779-85.
51. 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, nanomedicine, and biotechnology. 2018 Nov 5; 46(sup2): 616-25.
52. Dudhipala N, Puchchakayala G. Capecitabine lipid nanoparticles for anti-colon cancer activity in 1,2-dimethylhydrazine-induced colon cancer: preparation, cytotoxic, pharmacokinetic, and pathological evaluation. Drug Dev Ind Pharm. 2018; 44: 1572–1582.
53. Dinesh S, Pratibha S, Pandey KN, Vishal V, Vijay K, Saxena AK. Thermal and morphological behavior of PEEK/PEI blends with polyphosphazene coated carbon nanotube. Asian J Research Chem. 2012; 5(5): 650-654.
54. Dudhipala N, Ahmed AAY, Nagaraj B. Colloidal lipid nanodispersion enriched hydrogel of antifungal agent for management of fungal infections: comparative in-vitro, ex-vivo and in-vivo evaluation for oral and topical application. Chemistry and Physics of Lipids. 2020: 104981.
55. Narendar D, Karthik yadav J. Lipid nanoparticles of zaleplon for improved oral delivery by Box-Behnken design: Optimization, in vitro and in vivo evaluation. Drug Dev Ind Pharm. 2017; 43(7): 1205-1214.
56. 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: 572.
57. Narendar D, Thirupathi G. Neuroprotective effect of ropinirole loaded lipid nanoparticles hydrogel for Parkinson’s disease: preparation, in vitro, ex vivo, pharmacokinetic and pharmacodynamic evaluation. Pharmaceutics, 2020, 12(5): 448.
58. Nachammai K, Keerthi G S Nair, Ramaiyan Velmurugan, Sathesh Kumar S Pavithra K. Sustained – release study on mefenamic acid and mosapride loaded solid lipid nanoparticles: in vitro characterization. Research J Pharm and Tech. 2020; 13(11): 5391-5395.
59. Dudhipala N, Veerabrahma K. Improved anti-hyperlipidemic activity of Rosuvastatin Calcium via lipid nanoparticles: Pharmacokinetic and pharmacodynamic evaluation. European Journal of Pharmaceutics and Biopharmaceutics. 2017 Jan 1; 110: 47-57.
60. Ramanuj Prasad Samal, Pratap Kumar Sahu. Formulation development and in vitro characterization of solid lipid nanoparticles of felbamate. Research J Pharm and Tech. 2020; 13(9): 4185-4189.
61. Butreddy A, Dudhipala N, Janga KY, Gaddam RP. Lyophilization of small-molecule injectables: an industry perspective on formulation development, process optimization, scale-up challenges, and drug product quality attributes. AAPS PharmSciTech. 2020 Oct; 21(7): 1-20.
62. Kishan V, Sandeep V, Narendar D, Arjun N. Lacidipine loaded solid lipid nanoparticles for oral delivery: preparation, characterization and in vivo evaluation. International Journal of Pharmaceutical Sciences and Nanotechnology. 2016 Nov 30; 9(6): 3524-30.
63. Narendar D, Arjun N, Someshwar K, Rao YM. Quality by design approach for development and optimization of quetiapine fumarate effervescent floating matrix tablets for improved oral bioavailability. Journal of Pharmaceutical Investigation. 2016 Jun 1; 46(3): 253-63.
64. Janga KY, Tatke A, Dudhipala N, Balguri SP, Ibrahim MM, Maria DN, Jablonski MM, Majumdar S. Gellan gum-based sol-to-gel transforming system of natamycin transfersomes improves topical ocular delivery. Journal of Pharmacology and Experimental Therapeutics. 2019 Sep 1; 370(3): 814-22.