Bioavailability of Bilastine Oral Self-nanoemulsion: Comparative Study with Commercial Formula in Rats

Ishraq Kadhim Abbas; Shaimaa Nazar Abd AlHammid; Ammar Amer Fadhil; Marwah Mohammed Hareeja

doi:10.54133/ajms.v7i1.1024

Authors

Ishraq Kadhim Abbas Department of Pharmaceutics, Faculty of Pharmacy, Al-Rafidain University College, Baghdad 10052, Iraq
Shaimaa Nazar Abd AlHammid Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq https://orcid.org/0000-0002-6650-1997
Ammar Amer Fadhil Department of Pharmacology and Toxicology; College of Pharmacy- University of Baghdad, Baghdad, Iraq https://orcid.org/0000-0003-4174-6063
Marwah Mohammed Hareeja Department of Pharmaceutics, Faculty of Pharmacy, Al-Rafidain University College, Baghdad, Iraq https://orcid.org/0000-0003-1650-7917

DOI:

https://doi.org/10.54133/ajms.v7i1.1024

Keywords:

Bilastine, Bioavailability, Pharmacokinetics, Self-nanoemulsion

Abstract

Background: Bilastine (BL) is a novel non-sedating second-generation antihistamine, and its bioavailability is about 60%. Objective: To compare the bioavailability of prepared oral self-nanoemulsions of BL (BL-SNE) with that of pure BL and marketed tablets. Methods: Four groups of Wistar rats were used in this study, each with six rats weighing between 200 and 250 g. They were treated orally using a a gavage tube. The groups were fed either with conventional tablets ("Alerbix®") after being ground and dispersed with deionized water (DIW), treated with BL-SNE or fed with pure BL powder suspension. The fourth group did not receive any medication. The concentration of BL in the rat’s plasma was measured using HPLC. We used Trandolapril as an an internal standard. Results: The bioavailability results for the the prepared formula, tablet, and pure BL were 24289.91 ng/ml, 0.75 h, 12.81, 97844.7 ng.h/ml, and 98732.9 ng/ml, respectively, for the BL-SNE formula, and 15840.37, 1.0, 13.014, 66140.4, and 67088.3 for the tablets. Meanwhile, the BL suspension demonstrates 10830.12, 1.0 h, 12.96, 59397.12 ng/ml, and 60534.64 ng/ml, respectively. Conclusions: The relative bioavailability of BL-SNE was 1.47 and 1.6 times higher than that of marketed tablets and pure BL, respectively. This indicates an improvement in BL's bioavailability.

Downloads

Download data is not yet available.

References

Singh Randhawa A, Mohd Noor N, Md Daud MK, Abdullah B. Efficacy and safety of bilastine in the treatment of allergic rhinitis: A systematic review and meta-analysis. Front Pharmacol. 2022;1–12. doi: 10.3389/fphar.2021.731201.

Prathyusha P, Sundararajan R. UV spectrophotometric method for determination of Bilastine in bulk and pharmaceutical formulation. Res J Pharm Technol. 2020;13(2):933-938. doi: 10.5958/0974-360X.2020.00176.6.

Elks J, (editor), The dictionary of drugs: chemical data: chemical data, structures and bibliographies. Springer; 2014;131. doi: 10.1007/978-1-4757-2085-3.

Wolthers OD. Bilastine: A new nonsedating oral h1 antihistamine for treatment of allergic rhinoconjunctivitis and urticaria. Biomed Res Int. 2013;1–6. doi: 10.1155/2013/626837.

Vozmediano V, Sologuren A, Lukas JC, Leal N, Rodriguez M. Model informed pediatric development applied to bilastine: ontogenic PK model development, dose selection for first time in children and PK study design. Pharm Res. 2017;34:2720-2734. doi: 10.1007/s11095-017-2248-6.

Rathi SG, Chaudhari DB. Physicochemical characterization and dissolution enhancement of bilastine by solid dispersion. Int J Pharm Sci Rev Res. 2021;69(1). doi: 10.47583/ijpsrr.2021.v69i01.028.

Kumer A, Chakma U, Matin MM. Bilastine based drugs as SARS-CoV-2 protease inhibitors: molecular docking, dynamics, and ADMET related studies. Orbital. 2022;14(1):15–23. doi: 10.17807/orbital.v14i1.1642.

Rathore C, Hemrajani C, Sharma AK, Gupta PK, Jha NK, Aljabali AAA, et al. Self-nanoemulsifying drug delivery system (SNEDDS) mediated improved oral bioavailability of thymoquinone: optimization, characterization, pharmacokinetic, and hepatotoxicity studies. Drug Deliv Transl Res. 2023;13(1):292–307. doi: 10.1007/s13346-022-01193-8.

Buya AB, Beloqui A, Memvanga PB, Préat V. Self-nano-emulsifying drug-delivery systems: From the development to the current applications and challenges in oral drug delivery. Pharmaceutics. 2020;12(12):1–52. doi: 10.3390/pharmaceutics12121194.

Tekeli MC, Aktas Y, Celebi N. Oral self-nanoemulsifying formulation of GLP-1 agonist peptide exendin-4: development, characterization and permeability assesment on Caco-2 cell monolayer. Amino Acids. 2021;53(1):73–88. doi: 10.1007/s00726-020-02926-0.

Subramanian P, Rajnikanth PS, Kumar M, Chidambram K. In-vitro and in-vivo evaluation of supersaturable self-nanoemulsifying drug delivery system (SNEDDS) of dutasteride. Curr Drug Deliv. 2020;17(1):74-86.

Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profile. Eur J Pharm Sci. 2001;13(2):123-33. doi: 10.1016/s0928-0987(01)00095-1.

Shrestha B, Dunn L. The declaration of Helsinki on medical research involving human subjects: A review of seventh revision. J Nepal Health Res Counc. 2020;17(4):548-552. doi: 10.33314/jnhrc.v17i4.1042.

Reagan‐Shaw S, Nihal M, Ahmad N. Dose translation from animal to human studies revisited. FASEB J. 2008;22(3):6596-61. doi: 10.1096/fj.7-9574LSF.

Firdous S, Rizwan DS. Development and validation of stability indicating UPLC method for the estimation of bilastine in bulk and pharmaceutical dosage form. Int J Pharm Sci Rev Res. 2020;65(1):131-135. doi: 10.47583/ijpsrr.2020.v65i01.019.

Sádaba B, Gómez-Guiu A, Azanza JR, Ortega I, Valiente R. Oral availability of bilastine. Clin Drug Investig. 2013;33:375-381. doi: 10.1007/s40261-013-0076-y.

Hashim AA, Rajab NA. Anastrozole loaded nanostructured lipid carriers: preparation and evaluation. Iraqi J Pharm Sci. 2021;30(2):185-195. doi: 10.31351/vol30iss2pp185-195.

Kurji HA, Ghareeb MM, Zalzala MH, Numan AT, Hussain SA. Serum level profile and pharmacokinetic parameters of single oral dose of metronidazole in type II diabetic patients. Iraqi J Pharm Sci. 2011;20(1):14-18. doi: 10.31351/vol20iss1pp14-18.

Porter CJH, Trevaskis NL, Charman WN. Lipids and lipid-based formulations: Optimizing the oral delivery of lipophilic drugs. Nat Rev Drug Discov. 2007;6(3):231–248. doi: 10.1038/nrd2197.

Patel V, Lalani R, Bardoliwala D, Ghosh S, Misra A. Lipid-based oral formulation strategies for lipophilic drugs. AAPS PharmSciTech. 2018;19(8):3609–3630. doi: 10.1208/s12249-018-1188-8.

Singh B, Singh R, Bandyopadhyay S, Kapil R, Garg B. Optimized nanoemulsifying systems with enhanced bioavailability of carvedilol. Colloid Surfaces B: Biointerfaces. 2013;101:465-74. doi: 10.1016/j.colsurfb.2012.07.017.

Beg S, Swain S, Rizwan M, Irfanuddin M, Shobha Malini D. Bioavailability enhancement strategies: basics, formulation approaches and regulatory considerations. Curr Drug Deliv. 2011;8(6):691-702. doi: 10.2174/156720111797635504

Kanwal T, Saifullah S, Rehman J, Kawish M, Razzak A, Maharjan R, et al. Design of absorption enhancer containing self-nanoemulsifying drug delivery system (SNEDDS) for curcumin improved anti-cancer activity and oral bioavailability. J Mol Liquids. 2021;324:114774. doi: 10.1016/j.molliq.2020.114774.

Zafar A, Imam SS, Alruwaili NK, Alsaidan OA, Elkomy MH, Ghoneim MM, et al. Development of piperine-loaded solid self-nanoemulsifying drug delivery system: optimization, in-vitro, ex-vivo, and in-vivo evaluation. Nanomaterials. 2021;11(11):2920. doi: 10.3390/nano/11112920.