Generic placeholder image

Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Research Article

Nanofabrication of Losartan Potassium Sustained Release Floating Microspheres Using Different Grades of Ethyl Cellulose and its Insight on Release Profiles

Author(s): Tanavirsing Rajput, Popat Mohite, Santosh Ghule, Kuldeep Vinchurkar and Sudarshan Singh*

Volume 30, Issue 28, 2024

Published on: 20 June, 2024

Page: [2257 - 2265] Pages: 9

DOI: 10.2174/0113816128309675240530060752

Price: $65

Abstract

Introduction: A sustained release system for losartan potassium designed to delay its residence time in the stomach through the preparation of solvent evaporation technique-based floating microspheres. The influence of the different grades of Ethocel™ such as 4 cps, 10 cps, and 22 cps as well as the drug: polymer ratio on various properties of microspheres were tested.

Methods: Thermal and functional analysis revealed no interaction between the encapsulated drug and polymer. The results indicated that the mean diameter of microspheres increased with a change in grades of ethyl cellulose relating to viscosity. However, the drug incorporation efficiency within ethyl cellulose microspheres decreased with increasing viscosity of ethyl cellulose.

Results: The bulk density of the formulations was proportionally dependent on concentration and the viscosity of the polymer, which resulted in a decrease in floating capacity from 90.02% to 73.58%. Moreover, the drug release was indirectly proportional to the viscosity of ethyl cellulose tested. The in vitro release profile exhibited a burst effect with a biphasic release pattern following Fickian diffusion, indicating a diffusioncontrolled release mechanism.

Conclusion: The results demonstrated that the viscosity of ethyl cellulose significantly affects the floating capacity and drug release pattern from microspheres.

« Previous
[1]
Vargason AM, Anselmo AC, Mitragotri S. The evolution of commercial drug delivery technologies. Nat Biomed Eng 2021; 5(9): 951-67.
[http://dx.doi.org/10.1038/s41551-021-00698-w] [PMID: 33795852]
[2]
Singh MN, Hemant KS, Ram M, Shivakumar HG. Microencapsulation: A promising technique for controlled drug delivery. Res Pharm Sci 2010; 5(2): 65-77.
[PMID: 21589795]
[3]
Adepu S, Ramakrishna S. Controlled drug delivery systems: Current status and future directions. Molecules 2021; 26(19): 5905.
[http://dx.doi.org/10.3390/molecules26195905] [PMID: 34641447]
[4]
Wen H, Jung H, Li X. Drug delivery approaches in addressing clinical pharmacology-related issues: Opportunities and challenges. AAPS J 2015; 17(6): 1327-40.
[http://dx.doi.org/10.1208/s12248-015-9814-9] [PMID: 26276218]
[5]
Tripathi J, Thapa P, Maharjan R, Jeong SH. Current state and future perspectives on gastroretentive drug delivery systems. Pharmaceutics 2019; 11(4): 193.
[http://dx.doi.org/10.3390/pharmaceutics11040193] [PMID: 31010054]
[6]
Vinchurkar K, Sainy J, Khan MA, Mane S, Mishra DK, Dixit P. Features and facts of a gastroretentive drug delivery system-a review. Turk J Pharmaceut Sci 2022; 19(4): 476-87.
[http://dx.doi.org/10.4274/tjps.galenos.2021.44959] [PMID: 36047602]
[7]
Hua S. Advances in oral drug delivery for regional targeting in the gastrointestinal tract - influence of physiological, pathophysiological and pharmaceutical factors. Front Pharmacol 2020; 11: 524.
[http://dx.doi.org/10.3389/fphar.2020.00524] [PMID: 32425781]
[8]
Dickstein K, Timmermans P, Segal R. Losartan: A selective angiotensin II type 1 (AT1) receptor antagonist for the treatment of heart failure. Expert Opin Investig Drugs 1998; 7(11): 1897-914.
[http://dx.doi.org/10.1517/13543784.7.11.1897] [PMID: 15991937]
[9]
Singh S. Formulation of oral mucoadhesive tablets using mucilage isolated from buchanania lanzan spreng seeds. Int J Pharmaceut Sci Nanotechnol 7(2): 2494-503.
[http://dx.doi.org/10.37285/ijpsn.2014.7.2.11]
[10]
Singh S, Bothara SB. Development of oral mucoadhesive tablets of losartan potassium using natural gum from Manilkara Zapota seeds. Int J Pharmaceut Sci Nanotechnol 2013; 6(4): 2245-54.
[http://dx.doi.org/10.37285/ijpsn.2013.6.4.7]
[11]
Singh S, Bothara SB. Formulation development of oral mucoadhesive tablets of losartan potassium using mucilage isolated from Diospyros melonoxylon roxb seeds. Int J Pharmaceut Sci Nanotechnol 2013; 6(3): 2154-63.
[http://dx.doi.org/10.37285/ijpsn.2013.6.3.7]
[12]
Lo MW, Goldberg MR, McCrea JB, Lu H, Furtek CI, Bjornsson TD. Pharmacokinetics of losartan, an angiotensin II receptor antagonist, and its active metabolite EXP3174 in humans. Clin Pharmacol Ther 1995; 58(6): 641-9.
[http://dx.doi.org/10.1016/0009-9236(95)90020-9] [PMID: 8529329]
[13]
Derington CG, King JB, Delate T, et al. Twice-daily versus once-daily lisinopril and losartan for hypertension: Real-world effectiveness and safety. PLoS One 2020; 15(12): e0243371.
[http://dx.doi.org/10.1371/journal.pone.0243371] [PMID: 33270787]
[14]
Ahmadi P, Jahanban-Esfahlan A, Ahmadi A, Tabibiazar M, Mohammadifar M. Development of ethyl cellulose-based formulations: A perspective on the novel technical methods. Food Rev Int 2022; 38(4): 685-732.
[http://dx.doi.org/10.1080/87559129.2020.1741007]
[15]
Singh S, Bothara SB, Naveen MK. Formulation and ex-vivo evaluation of transdermal patches of glipizide using the penetration enhancer buchanania-lanzan (spreng) seed oil. Int J Pharmaceut Sci Nanotechnol 2015; 8(1): 2768-74.
[16]
Maddiboyina B, Hanumanaik M, Nakkala RK, et al. Formulation and evaluation of gastro-retentive floating bilayer tablet for the treatment of hypertension. Heliyon 2020; 6(11): e05459.
[http://dx.doi.org/10.1016/j.heliyon.2020.e05459] [PMID: 33241144]
[17]
Wani TU, Mir KB, Fazli AA, Raza SN, Khan NA. HPMC/] Carbopol based extended release gastroretentive dosage form of losartan potassium: Formulation and in vivo pharmacokinetic evaluation in rabbits. J Drug Deliv Sci Technol 2020; 60102006.
[http://dx.doi.org/10.1016/j.jddst.2020.102006]
[18]
Rahamathulla M, Saisivam S, Alshetaili A, et al. Design and evaluation of losartan potassium effervescent floating matrix tablets: In vivo x-ray imaging and pharmacokinetic studies in Albino rabbits. Polymers 2021; 13(20): 3476.
[http://dx.doi.org/10.3390/polym13203476] [PMID: 34685235]
[19]
Sawant K, Goswami N, Joshi G. Floating microspheres of valacyclovir HCl: Formulation, optimization, characterization, in vitro and in vivo floatability studies. J Pharm Bioallied Sci 2012; 4(5) (Suppl. 1): 8.
[http://dx.doi.org/10.4103/0975-7406.94118] [PMID: 23066217]
[20]
Zhu CY, Wang JY, Huang J, et al. Preparation and evaluation of gastro-floating hollow adhesive microspheres of carbomer/ethyl cellulose encapsulating dipyridamole. New J Chem 2019; 43(15): 5897-903.
[http://dx.doi.org/10.1039/C8NJ06398B]
[21]
Camargo TM, Nazato VS, Silva MG, Cogo JC, Groppo FC, Oshima-Franco Y. Bothrops jararacussu venom-induced neuromuscular blockade inhibited by Casearia gossypiosperma Briquet hydroalcoholic extract. J Venom Anim Toxins Incl Trop Dis 2010; 16(3): 432-41.
[http://dx.doi.org/10.1590/S1678-91992010000300009]
[22]
Singh S, Nwabor OF, Ontong JC, Voravuthikunchai SP. Characterization and assessment of compression and compactibility of novel spray-dried, co-processed bio-based polymer. J Drug Deliv Sci Technol 2020; 56101526.
[http://dx.doi.org/10.1016/j.jddst.2020.101526]
[23]
Singh S, Nwabor OF, Ontong JC, Kaewnopparat N, Voravuthikunchai SP. Characterization of a novel, co-processed bio-based polymer, and its effect on mucoadhesive strength. Int J Biol Macromol 2020; 145: 865-75.
[http://dx.doi.org/10.1016/j.ijbiomac.2019.11.198] [PMID: 31783076]
[24]
Bulk Density and Tapped Density of Powders. 2015. Available from: https://www.usp.org/sites/default/files/usp/document/harmonization/gen-chapter/bulk_density.pdf
[25]
Pardeshi S, Patil P, Rajput R, Mujumdar A, Naik J. Preparation and characterization of sustained release pirfenidone loaded microparticles for pulmonary drug delivery: Spray drying approach. Dry Technol 2021; 39(3): 337-47.
[http://dx.doi.org/10.1080/07373937.2020.1833213]
[26]
Khairnar G, Naik J, Mokale V. A statistical study on the development of micro particulate sustained drug delivery system for Losartan potassium by 3 2 factorial design approach. Bull Fac Pharm Cairo Univ 2017; 55(1): 19-29.
[http://dx.doi.org/10.1016/j.bfopcu.2016.10.001]
[27]
El-Nahas HM, Hosny KM. Chitosan-based floating microspheres of trimetazidin dihydrochloride; Preparation and in vitro characterization. Indian J Pharm Sci 2011; 73(4): 397-403.
[PMID: 22707823]
[28]
Goyal P, Gill S, Gupta UD, Rath G, Narang RK, Goyal AK. Development and characterization of rifampicin loaded floating microspheres. Artif Cells Blood Substit Immobil Biotechnol 2011; 39(5): 330-4.
[http://dx.doi.org/10.3109/10731199.2011.573482] [PMID: 21631389]
[29]
Jelvehgari M, Hassanzadeh D, Kiafar F, Delf Loveym B, Amiri S. Preparation and determination of drug-polymer interaction and in-vitro release of mefenamic acid microspheres made of celluloseacetate phthalate and/or ethylcellulose polymers. Iran J Pharm Res 2011; 10(3): 457-67.
[PMID: 24250377]
[30]
Adeleke OA. Premium ethylcellulose polymer based architectures at work in drug delivery. Int J Pharm X 2019; 1100023.
[http://dx.doi.org/10.1016/j.ijpx.2019.100023] [PMID: 31517288]
[31]
Nath B, Kanta Nath L, Mazumder B, Kumar P, Sharma N, Pratap Sahu B. Preparation and characterization of salbutamol sulphate loaded ethyl cellulose microspheres using water-in-oil-oil emulsion technique. Iran J Pharm Res 2010; 9(2): 97-105.
[PMID: 24363714]
[32]
Wu JH, Wang XJ, Li SJ, et al. Preparation of ethyl cellulose microspheres for sustained release of sodium bicarbonate. Iran J Pharm Res 2019; 18(2): 556-68.
[PMID: 31531041]
[33]
Singh S, Chidrawar V, Ushir Y, Vadalia K, Sheth N, Singh S. Pharmaceutical characterizationof amoxicillin trihydrate as mucoadhesivemicrospheres in management of H. pylori. Int J Pharm Tech Res 2010; 2(1): 348-58.
[34]
Fu Y, Kao WJ. Drug release kinetics and transport mechanisms of non-degradable and degradable polymeric delivery systems. Expert Opin Drug Deliv 2010; 7(4): 429-44.
[http://dx.doi.org/10.1517/17425241003602259] [PMID: 20331353]

Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy