Gastroretentive Floating Microspheres of Metaxalone: A Novel Drug Delivery Approach for Muscle Relaxation
Abstract
Floating microspheres are advanced gastroretentive drug delivery systems that have the ability to extend gastric residence time and increase the oral bioavailability of drugs having narrow absorption windows. This research aimed to develop and characterize floating microspheres of metaxalone to address its short half-life and poor bioavailability, thereby enhancing its therapeutic action. Microspheres were prepared by ionotropic gelation with the aid of sodium alginate, ethylcellulose, HPMC, and sodium bicarbonate as a gas-forming agent. The systems were evaluated in a routine manner for micromeritic characteristics, entrapment efficiency, buoyancy, in vitro release patterns, and stability. Physicochemical interactions were studied by FTIR and DSC, whereas morphology was viewed through SEM. The optimized formulation (F5) had 58.43% entrapment efficiency, 81.32% buoyancy, and 82.34% sustained drug release within 12 h. SEM micrographs illustrated spherical particles with hollow cores, and compatibility studies established the lack of drug–polymer interaction. Stability studies showed minimal fluctuation in drug release and buoyancy during the storage time. Metaxalone-loaded floating microspheres had controlled release and extended gastric retention, indicating their usefulness to increase bioavailability, minimize dosing frequency, and enhance patient compliance in the therapy of muscle relaxation.
Keywords: Gastro-retentive drug delivery, floating microspheres, oral drug delivery systems, hollow microspheres, bioavailability enhancement.
Keywords:
Gastro-retentive drug delivery, floating microspheres, oral drug delivery systems, hollow microspheres, bioavailability enhancementDOI
https://doi.org/10.22270/jddt.v15i11.7407References
1. Pawar VK, Kansal S, Garg G, Awasthi R, Singodia D, Kulkarni GT. Gastroretentive dosage forms: A review with special emphasis on floating drug delivery systems. Drug Deliv. 2011;18(2):97-110. https://doi.org/10.3109/10717544.2010.520354 PMid:20958237
2. Singh BN, Kim KH. Floating drug delivery systems: An approach to oral controlled drug delivery via gastric retention. J Control Release. 2000;63(3):235-59. https://doi.org/10.1016/S0168-3659(99)00204-7 PMid:10601721
3. Deshpande A, Shah N, Rhodes CT, Malick W. Controlled-release systems for delivering drugs that remain in the stomach for a prolonged period: An overview. Drug Dev Ind Pharm. 1996;22(6):531-39. https://doi.org/10.3109/03639049609108355
4. Avdeef A. Absorption and drug development: solubility, permeability, and charge state. 2nd ed. Hoboken (NJ): John Wiley & Sons; 2012. https://doi.org/10.1002/9781118286067
5. Kotreka UK, Adeyeye MC. Gastroretentive floating drug-delivery systems: A critical review. Crit Rev Ther Drug Carrier Syst. 2011;28(1):47-99. https://doi.org/10.1615/CritRevTherDrugCarrierSyst.v28.i1.20 PMid:21395515
6. Ishak RA. Buoyancy-generating agents for stomach-specific drug delivery: An overview with special emphasis on floating behavior. J Pharm Pharm Sci. 2015;18(1):77-100. https://doi.org/10.18433/J3602K PMid:25877444
7. Shah SH, Patel JK, Patel NV. Stomach-specific floating drug delivery system: A review. Int J PharmTech Res. 2009;1(3):623-33.
8. Virmani T, Gupta J. Pharmaceutical application of microspheres: An approach for the treatment of various diseases. Int J Pharm Sci Res. 2017;8(8):3253-60.
9. Thakral S, Thakral NK, Majumdar DK. Eudragit®: A technology evaluation. Expert Opin Drug Deliv. 2013;10(1):131-49. https://doi.org/10.1517/17425247.2013.736962 PMid:23102011
10. Vrettos NN, Roberts CJ, Zhu Z. Gastroretentive technologies in tandem with controlled-release strategies: A potent answer to oral drug bioavailability and patient compliance implications. Pharmaceutics. 2021;13(10):1591. https://doi.org/10.3390/pharmaceutics13101591 PMid:34683884 PMCid:PMC8539558
11. Hou JY, Li Y, Zhao N, Ji W, Ding Y, Zhang L, et al. Mucoadhesive microparticles for gastroretentive delivery: Preparation, biodistribution, and targeting evaluation. Mar Drugs. 2014;12(12):5764-87. https://doi.org/10.3390/md12125764 PMid:25470180 PMCid:PMC4278200
12. Garg R, Gupta GD. Progress in controlled gastroretentive delivery systems. Trop J Pharm Res. 2008;7(3):1055-66. https://doi.org/10.4314/tjpr.v7i3.14691
13. Keller J, Bassotti G, Clarke J, Dinning PG, Fox M, Grover M, et al. Advances in the diagnosis and classification of gastric and intestinal motility disorders. Nat Rev Gastroenterol Hepatol. 2018;15(5):291-308. https://doi.org/10.1038/nrgastro.2018.7 PMid:29622808 PMCid:PMC6646879
14. Roszczenko-Jasińska P, Wojtyś MI, Jagusztyn-Krynicka EK. Helicobacter pylori treatment in the post-antibiotics era is researching for new drug targets. Appl Microbiol Biotechnol. 2020;104(23):9891-905. https://doi.org/10.1007/s00253-020-10945-w PMid:33052519 PMCid:PMC7666284
15. O'Donnell PB, McGinity JW. Preparation of microspheres by the solvent evaporation technique. Adv Drug Deliv Rev. 1997;28(1):25-42. https://doi.org/10.1016/S0169-409X(97)00049-5 PMid:10837563
16. Gouin S. Microencapsulation: Industrial appraisal of existing technologies and trends. Trends Food Sci Technol. 2004;15(7-8):330-47. https://doi.org/10.1016/j.tifs.2003.10.005
17. Kamaly N, Yameen B, Wu J, Farokhzad OC. Degradable controlled-release polymers and polymeric nanoparticles: Mechanisms of controlling drug release. Chem Rev. 2016; 2016;116(4):2602-63. https://doi.org/10.1021/acs.chemrev.5b00346 PMid:26854975 PMCid:PMC5509216
18. Tayal S, Sharma A, Kumar A. Development and characterization of non-aqueous-based self-emulsifying nanoemulsion of curcumin. Middle East J Appl Sci Technol. 2023;6(2):144-52. https://doi.org/10.46431/MEJAST.2023.6216
19. Haseen M, Katiyar PK, Shukla B, Sharma A, Kumar P, Tyagi NTN. Synthesis and characterization of sulfamethoxazole derivatives. J Drug Deliv Ther. 2025;15(8):1-8. https://doi.org/10.22270/jddt.v15i8.7302
21. Kumar M, Arya DK, Almujri SS, Chidambaram K, Pandey P, Kumar A, et al. Mulberry silk worm pupae oil and Prussian blue nanoparticle enriched multi-faceted polyvinyl alcohol nanofiber for infectious full thickness skin wound healing. Tissue Engineering and Regenerative Medicine. 2025; 1-22. https://doi.org/10.1007/s13770-025-00751-8 PMid:40974525
22. Srujani KSN, Annapurna, Pawar AKM. Analytical Quality by Design approach in RP-HPLC method development and validation for the determination of Duvelisib. Asian Journal of Pharmaceutical and Clinical Research. 2021;14(2):99-108. https://doi.org/10.22159/ajpcr.2021.v14i2.40181
23. Srujani KSN, Harika, Pawar AKM. RP-HPLC method development and validation for the determination of Pemigatinib using the Design of Experiments approach. Journal of Pharmaceutical Research International. 2020;32(40):26-48. https://doi.org/10.9734/jpri/2020/v32i4031031
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