34
Views
0
CrossRef citations to date
0
Altmetric
Research Article

Formulation development, characterization, and evaluation of bedaquiline fumarate – Soluplus® – solid dispersion

, & ORCID Icon
Received 09 Nov 2023, Accepted 22 Apr 2024, Published online: 10 May 2024

References

  • Alkholief M, Albasit H, Alhowyan A, Alshehri S, Raish M, Abul Kalam M, Alshamsan A. 2019. Employing a PLGA-TPGS based nanoparticle to improve the ocular delivery of Acyclovir. Saudi Pharm J. 27(2):293–302. doi: 10.1016/J.JSPS.2018.11.011.
  • Bagre AP, Jain K, Jain NK. 2013. Alginate coated chitosan core shell nanoparticles for oral delivery of enoxaparin: in vitro and in vivo assessment. Int J Pharm. 456(1):31–40. doi: 10.1016/j.ijpharm.2013.08.037.
  • Biradar SV, Patil AR, Sudarsan GV, Pokharkar VB. 2006. A comparative study of approaches used to improve solubility of roxithromycin. Powder Technol. 169(1):22–32. doi: 10.1016/j.powtec.2006.07.016.
  • De Matteis L, Jary D, Lucía A, García-Embid S, Serrano-Sevilla I, Pérez D, Ainsa JA, Navarro FP, M. de la Fuente J. 2018. New active formulations against M. tuberculosis: bedaquiline encapsulation in lipid nanoparticles and chitosan nanocapsules. Chem Eng J. 340:181–191. doi: 10.1016/j.cej.2017.12.110.
  • De Mohac LM, Raimi-Abraham B, Caruana R, Gaetano G, Licciardi M. 2020. Multicomponent solid dispersion a new generation of solid dispersion produced by spray-drying. J Drug Deliv Sci Technol. 57:101750. doi: 10.1016/j.jddst.2020.101750.
  • De Vito A, Fiore V, Urru V, Bozzi E, Geremia N, Princic E, Canu D, Molicotti P, Are R, Babudieri S, et al. 2022. Use of bedaquiline in spinal osteomyelitis and soft tissue abscess caused by multidrug-resistant Mycobacterium tuberculosis: a case report. Braz J Infect Dis. 26(5):102701. doi: 10.1016/J.BJID.2022.102701.
  • Desai S, Poddar A, Sawant K. 2016. Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability. Mater Sci Eng C Mater Biol Appl. 58:826–834. doi: 10.1016/J.MSEC.2015.09.019.
  • FDA. n.d. Dissolution methods database. [accessed June 8, 2023]. https://www.fda.gov/drugs/drug-approvals-and-databases/dissolution-methods-database.
  • Goddeeris C, Willems T, Houthoofd K, Martens JA, Van den Mooter G. 2008. Dissolution enhancement of the anti-HIV drug UC 781 by formulation in a ternary solid dispersion with TPGS 1000 and Eudragit E100. Eur J Pharm Biopharm. 70(3):861–868. doi: 10.1016/J.EJPB.2008.07.006.
  • Halder S, Ahmed F, Shuma ML, Azad MAK, Kabir ER. 2020. Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization. Heliyon. 6(9):e05026. doi: 10.1016/J.HELIYON.2020.E05026.
  • Jinyi X, Zhang L, Zhang X, Xinzeng W, Jian C. 2021. Crystalline forms of bedaquiline fumarate and preparation methods therefor. [accessed 2023 June 7]. https://patents.google.com/patent/EP3366676B1/lista_geral_produtos_quimicos.pdf
  • Joshi K, Chandra A, Jain K, Talegaonkar S. 2019. Nanocrystalization: an emerging technology to enhance the bioavailability of poorly soluble drugs. Pharm Nanotechnol. 7(4):259–278. doi: 10.2174/2211738507666190405182524.
  • Joshi K, Jain V, Dhankhar K, Popli H, Jain K. 2020. Respiratory tract function and nutraceuticals. In: Bhatt P, Miraghajani MS, Pathak S, Pathak Y, editors. Nutraceuticals for prenatal, maternal and offspring’s nutritional health. Boca Raton, FL: CRC Press. doi: 10.1201/9780429437632-19.
  • Kaushik A, Ammerman NC, Tyagi S, Saini V, Vervoort I, Lachau-Durand S, Nuermberger E, Andries K. 2019. Activity of a long-acting injectable bedaquiline formulation in a paucibacillary mouse model of latent tuberculosis infection. Antimicrob Agents Chemother. 63(4):e00007 doi: 10.1128/AAC.00007-19.
  • Khanfar M, Al-Taani B, Alsmadi M, Zayed A. 2018. Enhancement of the dissolution and bioavailability from freeze-dried powder of a hypocholesterolemic drug in the presence of Soluplus. Powder Technol. 329:25–32. doi: 10.1016/j.powtec.2018.01.068.
  • Khoshnood S, Goudarzi M, Taki E, Darbandi A, Kouhsari E, Heidary M, Motahar M, Moradi M, Bazyar H. 2021. Bedaquiline: current status and future perspectives. J Glob Antimicrob Resist. 25:48–59. doi: 10.1016/J.JGAR.2021.02.017.
  • Lim H, Hoag SW. 2013. Plasticizer effects on physical-mechanical properties of solvent cast Soluplus® films. AAPS PharmSciTech. 14(3):903–910. doi: 10.1208/S12249-013-9971-Z/METRICS.
  • Liu P, Zhou JY, Chang JH, Liu XG, Xue HF, Wang RX, Li ZS, Li CS, Wang J, Liu CZ. 2020. Soluplus-mediated diosgenin amorphous solid dispersion with high solubility and high stability: development, characterization and oral bioavailability. Drug Des Devel Ther. 14:2959–2975. doi: 10.2147/DDDT.S253405.
  • Ma Y, Yang Y, Xie J, Xu J, Yue P, Yang M. 2018. Novel nanocrystal-based solid dispersion with high drug loading, enhanced dissolution, and bioavailability of andrographolide. Int J Nanomedicine. 13:3763–3779. doi: 10.2147/IJN.S164228.
  • Momin MAM, Rangnekar B, Sinha S, Cheung CY, Cook GM, Das SC. 2019. Inhalable dry powder of bedaquiline for pulmonary tuberculosis: in vitro physicochemical characterization, antimicrobial activity and safety studies. Pharmaceutics. 11(10):502. doi: 10.3390/PHARMACEUTICS11100502.
  • Pardhi VP, Jain K. 2021. Impact of binary/ternary solid dispersion utilizing poloxamer 188 and TPGS to improve pharmaceutical attributes of bedaquiline fumarate. J Drug Deliv Sci Technol. 62:102349. doi: 10.1016/j.jddst.2021.102349.
  • Pardhi VP, Patel P, Vaish A, Jain K. 2024a. Inclusion complexes of bedaquiline fumarate with β-cyclodextrin and its derivatives: in silico, in vitro and in vivo evaluation. J Drug Deliv Sci Technol. 91:105253. doi: 10.1016/j.jddst.2023.105253.
  • Pardhi VP, Pathak A, Jain K. 2024b. Solid dispersions of bedaquiline fumarate to improve its pharmaceutical attributes: a comparative study between PEG and PVP. J Drug Deliv Sci Technol. 94(105461):1–15. doi: 10.1016/j.jddst.2024.105461.
  • Pardhi VP, Suthar T, Sharma A, Jain K. 2022. Bedaquiline fumarate microemulsion: formulation optimization, rheological characterization and in vitro studies. Nanomedicine (Lond). 17(21):1529–1546. doi: 10.2217/NNM-2022-0132.
  • Patil SM, Sawant SS, Kunda NK. 2021. Inhalable bedaquiline-loaded cubosomes for the treatment of non-small cell lung cancer (NSCLC). Int J Pharm. 607:121046. doi: 10.1016/J.IJPHARM.2021.121046.
  • Pignatello R, Corsaro R, Bonaccorso A, Zingale E, Carbone C, Musumeci T. 2022. Soluplus® polymeric nanomicelles improve solubility of BCS-class II drugs. Drug Deliv Transl Res. 12(8):1991–2006. doi: 10.1007/S13346-022-01182-X/FIGURES/11.
  • Rao M, Mandage Y, Thanki K, Bhise S. 2010. Dissolution improvement of simvastatin by surface solid dispersion technology. Dissolution Technol. 17(2):27–34. doi: 10.14227/DT170210P27.
  • Shamma RN, Basha M. 2013. Soluplus®: a novel polymeric solubilizer for optimization of Carvedilol solid dispersions: formulation design and effect of method of preparation. Powder Technol. 237:406–414. doi: 10.1016/j.powtec.2012.12.038.
  • Sharma A, Jain K, Flora SJS. 2018. Vitamins based novel target pathways/molecules as possible emerging drug targets for the management of tuberculosis. Med Chem. 14(3):212–224. doi: 10.2174/1573406413666171103093235.
  • Solanki NG, Lam K, Tahsin M, Gumaste SG, Shah AV, Serajuddin ATM. 2019. Effects of surfactants on itraconazole-HPMCAS solid dispersion prepared by hot-melt extrusion I: miscibility and drug release. J Pharm Sci. 108(4):1453–1465. doi: 10.1016/J.XPHS.2018.10.058.
  • Soria-Carrera H, Lucía A, De Matteis L, Aínsa JA, Martín-Rapún R, de la Fuente JM. 2019. Polypeptidic micelles stabilized with sodium alginate enhance the activity of encapsulated bedaquiline. Macromol Biosci. 19:e1800397. doi: 10.1002/MABI.201800397.
  • Svensson EM, Du Bois J, Kitshoff R, de Jager VR, Wiesner L, Norman J, Nachman S, Smith B, Diacon AH, Hesseling AC, et al. 2018. Relative bioavailability of bedaquiline tablets suspended in water: implications for dosing in children. Br J Clin Pharmacol. 84(10):2384–2392. doi: 10.1111/BCP.13696.
  • Tambe A, Mokashi P, Pandita N. 2019. Ex-vivo intestinal absorption study of boswellic acid, cyclodextrin complexes and poloxamer solid dispersions using everted gut sac technique. J Pharm Biomed Anal. 167:66–73. doi: 10.1016/J.JPBA.2018.12.018.
  • Tian Y, Jacobs E, Jones DS, McCoy CP, Wu H, Andrews GP. 2020. The design and development of high drug loading amorphous solid dispersion for hot-melt extrusion platform. Int J Pharm. 586:119545. doi: 10.1016/J.IJPHARM.2020.119545.
  • Van Hemelryck S, Dewulf J, Niekus H, van Heerden M, Ingelse B, Holm R, Mannaert E, Langguth P. 2019. In vitro evaluation of poloxamer in situ forming gels for bedaquiline fumarate salt and pharmacokinetics following intramuscular injection in rats. Int J Pharm X. 1:100016. doi: 10.1016/J.IJPX.2019.100016.
  • Zheng Y, Chen H, Zeng X, Liu Z, Xiao X, Zhu Y, Gu D, Mei L. 2013. Surface modification of TPGS-b-(PCL-ran-PGA) nanoparticles with polyethyleneimine as a co-delivery system of TRAIL and endostatin for cervical cancer gene therapy. Nanoscale Res Lett. 8(1):161. doi: 10.1186/1556-276X-8-161.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.