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Volume 20, Issue 2
  • ISSN: 1574-8855
  • E-ISSN: 2212-3903

Abstract

Aims

The aim of this research work was to investigate the potential ability of cilnidipine-loaded-Self-Emulsifying Drug Delivery System (SEDDS) to improve the solubility and oral bioavailability of cilnidipine.

Background

The therapeutic value of drugs is constrained by the low oral bioavailability of BCS class II drugs. In order to improve the solubility and oral bioavailability of poorly water-soluble drugs, SEDDS are frequently utilised.

Methods

To develop the cilnidipine-loaded-SEDDS formulation, Canola oil as the oil phase, tween 80 as the surfactant, and PEG 300 as the co-surfactant were used. The SEDDS formulation was evaluated based on stability study per ICH guidelines, drug precipitation during lipolysis study under fasted and fed state, and pharmacodynamic study in Wistar rats. The content of the drug was determined by assay of SEDDS formulation using the official method of cilnidipine.

Results

The pharmacodynamic study demonstrated that cilnidipine-loaded SEDDS formulation significantly produced a rapid antihypertensive effect (within 2 h) that lasted for 24 h in comparison to drug suspension. During the lipolysis study, the concentration of the drug recovered from the aqueous phase under both fasted and fed state was more than 90% after 10 minutes, with a minute amount of drug involved in precipitation. At stability conditions of 30 ± 2°C/65 ± 5%RH for a duration of six months, the SEDDS formulation was found to be stable. The content of cilnidipine in the SEDDS formulation was found to be 98.4%.

Conclusion

A BCS class-II drug's oral bioavailability and dissolution might be improved using the self-emulsifying drug delivery method.

© 2025 Bentham Science Publishers
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/content/journals/cdth/10.2174/0115748855257230230919111500
2024-04-03
2024-12-28

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References

  1. ZhouB. PerelP. MensahG.A. EzzatiM. Global epidemiology, health burden and effective interventions for elevated blood pressure and hypertension.Nat. Rev. Cardiol.2021181178580210.1038/s41569‑021‑00559‑834050340
     [Google Scholar]
  2. HeadGA MihailidouAS DugganKA Definition of ambulatory blood pressure targets for diagnosis and treatment of hypertension in relation to clinic blood pressure: prospective cohort study.BMJ2010340apr14 3c110410.1136/bmj.c110420392760
     [Google Scholar]
  3. TakaharaA. Cilnidipine: a new generation Ca channel blocker with inhibitory action on sympathetic neurotransmitter release.Cardiovasc. Ther.200927212413910.1111/j.1755‑5922.2009.00079.x19426250
     [Google Scholar]
  4. UneyamaH. UchidaH. KondaT. YoshimotoR. Cilnidipine: preclinical profile and clinical evaluation.Cardiovasc. Drug Rev.199917434135710.1111/j.1527‑3466.1999.tb00024.x
     [Google Scholar]
  5. Cilnidipine, Drug bankAvailable from: https://go.drugbank.com/drugs/DB09232 (Accessed on: 8 January 2023).
  6. KohliK. ChopraS. DharD. AroraS. KharR.K. Self-emulsifying drug delivery systems: an approach to enhance oral bioavailability.Drug Discov. Today20101521-2295896510.1016/j.drudis.2010.08.00720727418
     [Google Scholar]
  7. ShresthaH. BalaR. AroraS. Lipid-based drug delivery systems.J. Pharm. (Cairo)2014201411010.1155/2014/80182026556202
     [Google Scholar]
  8. KadianR. NandaA. A comprehensive insight on self emulsifying drug delivery systems.Recent Advances in Drug Delivery and Formulation2022161164410.2174/266738781566621120711280334875995
     [Google Scholar]
  9. XiaoL. YiT. LiuY. ZhouH. The in vitro lipolysis of lipid-based drug delivery systems: A newly identified relationship between drug release and liquid crystalline phase.BioMed Res. Int.201620161910.1155/2016/236431727294110
     [Google Scholar]
  10. Government of IndiaMinistry of Health & Family Welfare.GhaziabadThe Indian Pharmacopoeia Commission2018
     [Google Scholar]
  11. LiaoH. GaoY. LianC. Oral absorption and lymphatic transport of baicalein following drug–phospholipid complex incorporation in self-microemulsifying drug delivery systems.Int. J. Nanomedicine2019147291730610.2147/IJN.S21488331564878
     [Google Scholar]
  12. FatourosD. NielsenF. DouroumisD. HadjileontiadisL. MullertzA. In vitro–in vivo correlations of self-emulsifying drug delivery systems combining the dynamic lipolysis model and neuro-fuzzy networks.Eur. J. Pharm. Biopharm.200869388789810.1016/j.ejpb.2008.01.02218367386
     [Google Scholar]
  13. AlayoubiA. AqueelM.S. CruzC.N. AshrafM. ZidanA.S. Application of in vitro lipolysis for the development of oral self-emulsified delivery system of nimodipine.Int. J. Pharm.20185531-244145310.1016/j.ijpharm.2018.10.06630385374
     [Google Scholar]
  14. ICH harmonised tripartite guidelines, Stability testing of new drug substances and products, Link.Available from: https://database.ich.org/sites/default/files/Q1A%28R2%29%20Guideline.pdf (Accessed on: 13 June, 2022).
  15. DudhipalaN. VeerabrahmaK. Pharmacokinetic and pharmacodynamic studies of nisoldipine-loaded solid lipid nanoparticles developed by central composite design.Drug Dev. Ind. Pharm.201541121968197710.3109/03639045.2015.102468525830370
     [Google Scholar]
  16. DiwanR. RaviP.R. PathareN.S. AggarwalV. Pharmacodynamic, pharmacokinetic and physical characterization of cilnidipine loaded solid lipid nanoparticles for oral delivery optimized using the principles of design of experiments.Colloids Surf. B Biointerfaces202019311107310.1016/j.colsurfb.2020.11107332388122
     [Google Scholar]
  17. KadianR. NandaA. Formulation, optimization, and in vitro characterization of cilnidipine-loaded self-emulsifying drug delivery system.Drug Delivery Letters202313322524210.2174/2210303113666230502104226
     [Google Scholar]
  18. BuyaA.B. UcakarB. BeloquiA. MemvangaP.B. PréatV. Design and evaluation of self-nanoemulsifying drug delivery systems (SNEDDSs) for senicapoc.Int. J. Pharm.202058011918010.1016/j.ijpharm.2020.11918032135227
     [Google Scholar]
  19. FatourosD.G. DeenG.R. ArlethL. Structural development of self nano emulsifying drug delivery systems (SNEDDS) during in vitro lipid digestion monitored by small-angle X-ray scattering.Pharm. Res.200724101844185310.1007/s11095‑007‑9304‑617458683
     [Google Scholar]
  20. ElgartA. CherniakovI. AldoubyY. DombA.J. HoffmanA. Improved oral bioavailability of BCS class 2 compounds by self nanoemulsifying drug delivery systems (SNEDDS): The underlying mechanisms for amiodarone and talinolol.Pharm. Res.201330123029304410.1007/s11095‑013‑1063‑y23686373
     [Google Scholar]
/content/journals/cdth/10.2174/0115748855257230230919111500
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In-vitro Lipolysis, Stability and Pharmacodynamic Study of Cilnidipine Loaded Self-emulsifying Drug Delivery System
Curr Drug Ther 20, 210 (2025); https://doi.org/10.2174/0115748855257230230919111500
/content/journals/cdth/10.2174/0115748855257230230919111500
/content/journals/cdth/10.2174/0115748855257230230919111500
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  • Article Type:     Research Article
Keyword(s): Cilnidipine; ICH guidelines; in vitro lipolysis; pharmacodynamic; self-emulsifying drug delivery system; stability

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