Formulation and In-Vitro Evaluation of Lemborexant Orodispersible Film
Abstract
The current work focused on the formulation and in vitro evaluation of Lemborexant oral dispersible films (ODFs) loaded with nanoparticles to improve solubility, dissolution, and patient compliance in the treatment of insomnia. Lemborexant, a dual orexin receptor antagonist, has low water solubility, reducing its oral bioavailability. To overcome this limitation, nanoparticles were prepared using the solvent displacement method and incorporated into fast-dissolving polymeric films that contained hydroxypropyl methylcellulose (HPMC) and carboxymethyl cellulose (CMC) as film-forming agents, PEG as a plasticizer, and superdisintegrants for rapid disintegration. The produced films were tested for physicochemical and mechanical properties such as thickness, weight fluctuation, folding endurance, tensile strength, surface pH, drug content homogeneity, disintegration time, and in vitro drug release.The optimized formulation demonstrated uniform thickness and weight, as well as appropriate tensile strength. The films disintegrated quickly (15-30 seconds) and had considerably higher in vitro drug release than pure Lemborexant. FTIR tests verified the absence of drug-excipient interactions, while SEM revealed homogeneous nanoparticle dispersion. The findings suggested that Lemborexant-loaded nanoparticle oral dispersible films are a viable delivery platform for quick onset of action, increased bioavailability, and enhanced patient compliance, particularly in geriatric patients with swallowing issues. Additional in vivo investigations are needed to confirm the therapeutic efficacy and pharmacokinetic advantages of the proposed formulation.
Keywords: Lemborexant, Oral Dispersible Film, Nanoparticles, Solvent Casting, In vitro drug release studies.
Keywords:
Lemborexant, Oral Dispersible Film, Nanoparticles, Solvent Casting, In vitro drug release studiesDOI
https://doi.org/10.22270/jddt.v16i1.7528References
1. M.C. Roco Nanotechnology: convergence with modern biology and medicine Curr Opin Biotechnol, 2003;14(3):337-346. https://doi.org/10.1016/S0958-1669(03)00068-5 PMid:12849790
2. Gonzalez L, Loza RJ, Han KY, Nanotechnology in corneal neovascularization therapy-a review J Ocul Pharmacol Ther, 2013;29(2)124-134 https://doi.org/10.1089/jop.2012.0158 PMid:23425431 PMCid:PMC3601629
3. Moshed AMA, Sarkar MKI, Khaleque MA, The application of nanotechnology in medical sciences: new horizon of treatment Am J Biomed Sci, 2017;9(1):1-14 https://doi.org/10.5099/aj170100001
4. Fakruddin M, Hossain Z, Afroz H, Prospects and applications of nanobiotechnology: a medical perspective J Nanobiotechnology, 2012;10(1):31 https://doi.org/10.1186/1477-3155-10-31 PMid:22817658 PMCid:PMC3422163
5. Klymchenko AS, Liu F, Collot M. Anton N, Dye-loaded nanoemulsions: biomimetic fluorescent nanocarriers for bioimaging and nanomedicine Adv Healthc Mater, 2021;10(1). https://doi.org/10.1002/adhm.202001289 PMid:33052037
6. Surendiran A, Sandhiya S, Pradhan SC, Adithan C, Novel applications of nanotechnology in medicine Indian J Med Res, 2009;130(6)689-701.
7. Bhardwaj H, Jangde RK, Current updated review on preparation of polymeric nanoparticles for drug delivery and biomedical applications, Next Nanotechnology, 2023;2. https://doi.org/10.1016/j.nxnano.2023.100013
8. Zielińska, A.; Carreiró, F.; Oliveira, A.M.; Neves, A.; Pires, B.; Venkatesh, D.N.; Durazzo, A.; Lucarini, M.; Eder, P.; Silva, A.M.; et al. Polymeric Nanoparticles: Production, Characterization, Toxicology and Ecotoxicology. Molecules 2020;25:3731. https://doi.org/10.3390/molecules25163731 PMid:32824172 PMCid:PMC7464532
9. Ankit, Formulation and Evaluation of Polymeric Nanoparticles of an Antiviral Drug for Gastroretention, March 2012;4(4):1557-1562. https://doi.org/10.37285/ijpsn.2011.4.4.6
10. Lee D, Kwak G, Johnson TV, Suk JS. Formulation and Evaluation of Polymer-Based Nanoparticles for Intravitreal Gene-Delivery Applications. Curr Protoc. 2022;2(12):e607. https://doi.org/10.1002/cpz1.607 PMid:36469609 PMCid:PMC9731353
11. Betala S, Mohan Varma M, Abbulu K. Formulation and evaluation of polymeric nanoparticles of an antihypetensive drug for gastroretention. JDDT, 2018 ;8(6):82-6. https://doi.org/10.22270/jddt.v8i6.2018
12. Marzouk. M., El bakry. AM., El hosary. R M.,Abd El Rahman. NK. Formulation and Evaluation of Polymeric Nanoparticles Based Transdermal Hydrogel of Terbutaline Sulphate. Azhar International Journal of Pharmaceutical and Medical Sciences, 2023;3(2):20-29.
13. Balzus B, Sahle FF, Hönzke S, Gerecke C, Schumacher F, Hedtrich S, Kleuser B, Bodmeier R, Formulation and ex vivo evaluation of polymeric nanoparticles for controlled delivery of corticosteroids to the skin and the corneal epithelium, European Journal of Pharmaceutics and Biopharmaceutics, Volume 2017;115:122-130. https://doi.org/10.1016/j.ejpb.2017.02.001 PMid:28189623
14. Sharma D, Formulation and Optimization of Polymeric Nanoparticles for Intranasal Delivery of Lorazepam Using Box-Behnken Design: In Vitro and In Vivo Evaluation, BioMed Research International. 2014. https://doi.org/10.1155/2014/156010 PMid:25126544 PMCid:PMC4122152
Published
Abstract Display: 26 
PDF Downloads: 13 PDF Downloads: 3 How to Cite
Issue
Section
Copyright (c) 2026 S.M. Shahidulla , Mohammed Imtiyaz
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).
How to Cite
.