BIOAVAILABILITY ENHANCEMENT STRATEGIES FOR RIVAROXABAN: A NOTEWORTHY REVIEW
DOI:
https://doi.org/10.22159/ijap.2023v15i6.48839Keywords:
Rivaroxaban, Bioavailability enhancement, Microspheres, Liposomes, Self-nanoemulsifying drug delivery system, Solid lipid nanoparticles, Cocrystals, Sustained release, Solid dispersionAbstract
This review article discusses Rivaroxaban (RXB), an anticoagulant that has gained much attention due to its ability to prevent blood clots from forming in the body. However, one of the major challenges pharmaceutical companies face is the low water solubility of RXB, which can lead to difficulties in formulating the drug for oral administration and affect the drug's bioavailability. However, to the best of our knowledge, limited studies have explored enhancing the bioavailability of the RXB. Most of these studies have been purely academic and impractical for industrial use. Therefore, this review article aims to discuss successful studies that have increased the bioavailability of RXB. The goal is to inspire researchers to develop this new drug further. The article covers seven strategies for enhancing the bioavailability of RXB, including microspheres, liposomes, self-nano emulsifying drug delivery system, solid lipid nanoparticles, cocrystals, sustained release, and solid dispersion. The studies discussed in this review offer valuable insights into developing novel drug delivery systems that can help overcome the limitations of existing drugs.
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Cohen AT, Hamilton M, Mitchell S, Phatak H, Liu X, Bird A. Comparison of the novel oral anticoagulants apixaban, dabigatran, edoxaban, and rivaroxaban in the initial and long-term treatment and prevention of venous thromboembolism: systematic review and network meta-analysis. Plos One. 2015 Dec 30:10(12):e0144856. doi: 10.1371/journal.pone.0144856, PMID 26716830, PMCID PMC4696796.
Patel MR, Mahaffey KW, Garg J, Pan G, Singer DE, Hacke W. Rivaroxaban versus warfarin in nonvalvular atrial fibrillation. N Engl J Med. 2011 Sep 8;365(10):883-91. doi: 10.1056/NEJMoa1009638, PMID 21830957.
Hernandez I, Zhang Y. Comparing stroke and bleeding with rivaroxaban and dabigatran in atrial fibrillation: analysis of the US medicare part d data. Am J Cardiovasc Drugs. 2017;17(1):37-47. doi: 10.1007/s40256-016-0189-9, PMID 27637493, PMCID PMC6572759.
Lee JH, Jeong HS, Jeong JW, Koo TS, Kim DK, Cho YH. The development and optimization of hot-melt extruded amorphous solid dispersions containing Rivaroxaban in combination with polymers. Pharmaceutics. 2021 Mar 6;13(3):344. doi: 10.3390/pharmaceutics13030344, PMID 33800741, PMCID PMC8001048.
El-Hashemy HA, Salama A, Rashad A. Experimental design, formulation, and in vivo evaluation of novel anticoagulant rivaroxaban loaded cubosomes in rats model. J Liposome Res. 2023;33(2):189-96. doi: 10.1080/08982104.2022.2153137. PMID 36440581.
Meng Y, Tan F, Yao J, Cui Y, Feng Y, Li Z. Preparation, characterization, and pharmacokinetics of rivaroxaban cocrystals with enhanced in vitro and in vivo properties in beagle dogs. Int J Pharm X. 2022;4:100119. doi: 10.1016/j.ijpx.2022.100119. PMID 35663355.
Stampfuss J, Kubitza D, Becka M, Mueck W. The effect of food on the absorption and pharmacokinetics of rivaroxaban. Int J Clin Pharmacol Ther. 2013 Jul 1;51(7):549-61. doi: 10.5414/CP201812, PMID 23458226.
Liu XQ, Li ZR, Wang CY, Chen YT, Jiao Z. Is a lower dose of rivaroxaban required for asians? A systematic review of a population pharmacokinetics and pharmacodynamics analysis of rivaroxaban. Pharmaceutics. 2023 Feb 9;15(2):588. doi: 10.3390/pharmaceutics15020588, PMID 36839909, PMCID PMC9964148.
Sudhamani KB, Daclatasvir Dihydrochloride JJ. Microspheres, process parameters for enhanced permeability and liver targeting. Asian Journal of Pharmaceutical and Clinical Research. 2022 Dec 7;15(12):179-83. doi: 10.22159/ajpcr.2022.v15i12.46596.
Neelam S, Meenakshi B. Formulation and evaluation of polymeric microspheres using box–behnken design. Asian J Pharm Clin Res 2022;15(10):47-55. doi: 10.22159/ajpcr.2022.v15i10.45250.
Choi MJ, Woo MR, Baek K, Park JH, Joung S, Choi YS. Enhanced oral bioavailability of Rivaroxaban-Loaded microspheres by optimizing the polymer and surfactant based on molecular interaction mechanisms. Mol Pharm. 2023 Jul 11;20(8):4153-64. doi: 10.1021/acs.molpharmaceut.3c00281, PMID 37433746.
Chaerunisaa AY, Dewi MK, Sriwidodo, Joni IM, Dwiyana RF. Development of cathelicidin in liposome carrier using thin layer hydration method. Int J App Pharm. 2022;14(4):178-85. doi: 10.22159/ijap.2022v14i4.44480.
Elsayad MK, Mowafy HA, Zaky AA, Samy AM. Chitosan caged liposomes for improving oral bioavailability of rivaroxaban: in vitro and in vivo evaluation. Pharm Dev Technol. 2021 Jan 6;26(3):316-27. doi: 10.1080/10837450.2020.1870237, PMID 33356742.
Mathew R, Varkey J. Formulation and in vitro evaluation of self NANO emulsifying drug delivery system of quercetin for enhancement of oral bioavailability. Int J Curr Pharm Res. 2022 Jan 15;14(1):60-9. doi: 10.22159/ijcpr.2022v14i1.44113.
Reddy MR, Gubbiyappa KS. A systematic review on supersaturable SELF-NANO emulsifying drug delivery system: a potential strategy for drugs with poor oral bioavailability. Int J App Pharm. 2022 May 7;14(3):16-33. doi: 10.22159/ijap.2022v14i3.44178.
Jayapal N, Vishnu YV. Formulation and in vivo evaluation of self-nanoemulsifying drug delivery system of ramipril in Wistar rats. Asian Journal of Pharmaceutical and Clinical Research. 2021;14(7):126-36. doi: 10.22159/ajpcr.2021.v14i7.42003.
Xue X, Cao M, Ren L, Qian Y, Chen G. Preparation and optimization of rivaroxaban by self-nanoemulsifying drug delivery system (SNEDDS) for enhanced oral bioavailability and no food effect. AAPS PharmSciTech. 2018 Apr 10;19(4):1847-59. doi: 10.1208/s12249-018-0991-6, PMID 29637496.
Shah J, Patel S, Bhairy S, Hirlekar R. Formulation optimization, characterization and in vitro anticancer activity of curcumin loaded nanostructured lipid carriers. Int J Curr Pharm Res. 2022 Jan 15:31-43. doi: 10.22159/ijcpr.2022v14i1.44110.
Luo X, Saleem A, Shafique U, Sarwar S, Ullah K, Imran M. Rivaroxaban-loaded SLNs with treatment potential of deep vein thrombosis: in vitro, in vivo, and toxicity evaluation. Pharm Dev Technol. 2023;28(7):625-37. doi: 10.1080/10837450.2023.2231069. PMID 37366661.
Rajadhyax AB, Shinde U, Desai HR, Mane S. Hot melt extrusion in engineering of drug cocrystals: a review. Asian Journal of Pharmaceutical and Clinical Research. 2021 Aug 7;14(8):10-9. doi: 10.22159/ajpcr.2021.v14i8.41857.
Alam S, Bishal A, Bandyopadhyay B. Formulation and evaluation of metformin hydrochloride sustained release matrix tablets. Int J Curr Pharm Res. 2021 Sep 15;13(5):82-8. doi: 10.22159/ijcpr.2021v13i5.1899.
Anwer MdK, Mohammad MA, Iqbal M, Ansari MN, Ezzeldin E, Fatima F. Sustained release and enhanced oral bioavailability of rivaroxaban by PLGA nanoparticles with no food effect. J Thromb Thrombolysis. 2020 Jan 2;49(3):404-12. doi: 10.1007/s11239-019-02022-5, PMID 31898270.
Sarkar P, Majee SB. Formulation development and in vitro characterization of ternary hydrotropic solid dispersions of aceclofenac. Asian Journal of Pharmaceutical and Clinical Research. 2022 Sep 7;15(9):174-9. doi: 10.22159/ajpcr.2022.v15i9.45158.
Shah PJ, Patel MP, Shah J, Nair AB, Kotta S, Vyas B. Amalgamation of solid dispersion and melt adsorption techniques for augmentation of oral bioavailability of novel anticoagulant rivaroxaban. Drug Deliv Transl Res. 2022 Apr 25;12(12):3029-46. doi: 10.1007/s13346-022-01168-9, PMID 35467325.
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Copyright (c) 2023 Adam Al-Shoubki, Mahmoud H. Teaima, Rehab A. Abdelmonem, Mohamed A. El-Nabarawi, Sammar Fathy Elhabal
This work is licensed under a Creative Commons Attribution 4.0 International License.
