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2000
Volume 12, Issue 1
  • ISSN: 2211-7385
  • E-ISSN: 2211-7393

Abstract

Nebivolol HCl is a unique third-generation beta blocker that has less oral bioavailability and exhibits various adverse effects like gastrointestinal disturbance and abdominal pain.

This study aimed to formulate and evaluate nebivolol HCl transferosomal transdermal patches to reduce the problems associated with oral delivery of the drug and enhancement of drug permeation through the skin.

Nebivolol HCl loaded transferosomes were prepared by thin film hydration method. Eight formulations were prepared based on the two independent variables, type of surfactant (Tween 80 and Span 80) and Phospholipid: Edge activator ratio and were evaluated for their vesicle size, PDI, and entrapment efficiency. The optimized formulations were incorporated into transdermal patches, which were evaluated for physicochemical properties, and permeation, skin irritancy, and stability studies.

The vesicle size of the transferosomes ranged from 49 nm to 93 nm, and EE% varied from 39% to 79%. Vesicles formed with Span 80 as an edge activator showed smaller vesicle size and greater EE% as compared to Tween 80. Based on the results, TW4 and SP4 were selected as the optimized formulations for further incorporation into the transdermal patches. and permeation studies showed permeation in the order F2 > F3 > F1, indicating that transferosomal formulations showed superior permeation of the drug compared to plain Nebivolol HCl patches. Span 80 transferosomes showed a slightly better permeation than Tween 80. Stability studies showed that transferosomes and the transdermal patches demonstrated good stability under proper storage conditions.

The study concluded that transferosomal patches of Nebivolol HCl could be used as a potential approach with effective transdermal delivery for the management of hypertension.

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2024-02-01
2025-09-24

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References

  1. SajuM.D. AllaghK.P. ScariaL. JosephS. ThiyagarajanJ.A. Prevalence, awareness, treatment, and control of hypertension and its associated risk factors: Results from baseline survey of Swades family cohort study.Int. J. Hypertens.202020201391710.1155/2020/4964835
     [Google Scholar]
  2. Al-DhubiabB. NairA.B. KumriaR. AttimaradM.A. HarshaS. Development and evaluation of nebivolol hydrochloride nanocrystals impregnated buccal film.Farmacia201967228228910.31925/farmacia.2019.2.12
     [Google Scholar]
  3. BijaniM. ParviziS. DehghanA. Investigating the prevalence of hypertension and its associated risk factors in a population-based study: Fasa PERSIAN COHORT data.BMC Cardiovasc. Disord.202020150310.1186/s12872‑020‑01797‑3
     [Google Scholar]
  4. TripatiK.D. Essential of medical pharmacology.6th edNew DelhiJaypee Brothers200850350410.5005/jp/books/10282
     [Google Scholar]
  5. McEvoyGK, Ed AHFS drug information. American society of health-system pharmacists20001888
     [Google Scholar]
  6. VijayanandP. PatilJ.S. ReddyM.V. Formulation and comparative pharmacokinetic evaluation of orodispersible tablets and films of nebivolol hydrochloride.J. Pharm. Investig.201545223724710.1007/s40005‑014‑0169‑5
     [Google Scholar]
  7. WangS.J. SanderG.E. Nebivolol/valsartan combination for the treatment of hypertension: A review.Future Cardiol.202117457358310.2217/fca‑2020‑007933064027
     [Google Scholar]
  8. ShindeA.J. WaghmareD.S. DalviR.S. MoreH.N. Formulation, design and characterization of muco adhesive buccal film of nebivolol using factorial design.Int. J. Pharma Sci.20189517971805
     [Google Scholar]
  9. LiuJ.Y. GuoL.N. PengW.Z. Efficacy and safety of nebivolol in hypertensive patients: A meta-analysis of randomized controlled trials.J. Int. Med. Res.2020481010.1177/030006052093162533081551
     [Google Scholar]
  10. TanwarH. SachdevaR. Transdermal drug delivery system: A review.Int. J. Pharma Sci.2016762274
     [Google Scholar]
  11. ShahV.P. TymesN.W. SkellyJ.P. In vitro release profiles of clonidine transdermal therapeutic systems and scopolamine transdermal patches.Pharm. Res.19896434635110.1023/A:10159629113442748524
     [Google Scholar]
  12. NayakB.S. EllaiahP. PattanayakD. DasS. Formulation design preparation and in vitro characterization of nebivolol transdermal patches.Asian J. Pharm.201453196202
     [Google Scholar]
  13. Al HanbaliO.A. KhanH.M.S. SarfrazM. ArafatM. IjazS. HameedA. Transdermal patches: Design and current approaches to painless drug delivery.Acta Pharm.201969219721510.2478/acph‑2019‑001631259729
     [Google Scholar]
  14. SachanR. ParasharT. SoniyaS.V. Drug carrier transfersomes: A novel tool for transdermal drug delivery system.Int J Res Dev Pharm Life Sci201322309316
     [Google Scholar]
  15. RamadonD. McCruddenM.T. CourtenayA.J. DonnellyR.F. Enhancement strategies for transdermal drug delivery systems: Current trends and applications.Drug Deliv. Transl. Res.202113433474709
     [Google Scholar]
  16. SalemH.F. KharshoumR.M. Abou-TalebH.A. NaguibD.M. Nano sized transferosome-based intranasal in situ gel for brain targeting of resveratrol: formulation, optimization, in vitro evaluation, and in vivo pharmacokinetic study.AAPS PharmSciTech201920518110.1208/s12249‑019‑1353‑831049748
     [Google Scholar]
  17. KumarA. Transferosome: A recent approach for transdermal drug delivery.J. Drug Deliv. Ther.201885-s10010410.22270/jddt.v8i5‑s.1981
     [Google Scholar]
  18. SolankiD. KushwahL. MotiwaleM. ChouhanV. Transferosomes-a review.World J. Pharm. Pharm. Sci.2016125435449
     [Google Scholar]
  19. ThakurN. JainP. JainV. Formulation development and evaluation of transferosomal gel.J. Drug Deliv. Ther.20188516817710.22270/jddt.v8i5.1826
     [Google Scholar]
  20. ParejiyaP.B. PatelR.C. MehtaD.M. ShelatP.K. BarotB.S. Quick dissolving films of nebivolol hydrochloride: Formulation and optimization by a simplex lattice design.J. Pharm. Investig.201343434335110.1007/s40005‑013‑0080‑5
     [Google Scholar]
  21. JatavV. SagguJ. SharmaA. SharmaA. JatR. Design, development and permeation studies of nebivolol hydrochloride from novel matrix type transdermal patches.Adv. Biomed. Res.2013216210.4103/2277‑9175.11581324223377
     [Google Scholar]
  22. SapkotaR. DashA.K. Liposomes and transferosomes: A breakthrough in topical and transdermal delivery.Ther. Deliv.202112214515810.4155/tde‑2020‑012233583219
     [Google Scholar]
  23. DudhipalaN. Phasha MohammedR. Adel Ali YoussefA. BanalaN. Effect of lipid and edge activator concentration on development of aceclofenac-loaded transfersomes gel for transdermal application: In vitro and ex vivo skin permeation.Drug Dev. Ind. Pharm.20204681334134410.1080/03639045.2020.178806932598194
     [Google Scholar]
  24. BalataG.F. FaisalM.M. ElghamryH.A. SabryS.A. Preparation and characterization of ivabradineHCltransfersomes for enhanced transdermal delivery.J. Drug Deliv. Sci. Technol.20206010192110.1016/j.jddst.2020.101921
     [Google Scholar]
  25. MajukarS. DandagiP.M. KurangiB.K. Design and characterization of transfersomal patch of aceclofenac as a carrier for transdermal delivery.Int. J. Pharm. Biol. Sci.20199111381147
     [Google Scholar]
  26. JagwaniS. JalalpureS. DhamechaD. JadhavK. BoharaR. Pharmacokinetic and pharmacodynamic evaluation of resveratrol loaded cationic liposomes for targeting hepatocellular carcinoma.ACS Biomater. Sci. Eng.2020694969498410.1021/acsbiomaterials.0c0042933455290
     [Google Scholar]
  27. MarwahH. GargT. RathG. GoyalA.K. Development of transferosomal gel for trans-dermal delivery of insulin using iodine complex.Drug Deliv.20162351636164410.3109/10717544.2016.115524327187718
     [Google Scholar]
  28. SurtiN. ParmarN. BhadsavleS. PatelV. Transfersomes loaded transdermal drug delivery system of methotrexate for rheumatoid arthritis.World J. Pharm. Pharm. Sci.2015412958968
     [Google Scholar]
  29. YadavP.K. MishraS. transdermal patch of an antihypertensive drug: Its development and evaluation.World J. Pharm. Res.2017641355137410.20959/wjpr20174‑8214
     [Google Scholar]
  30. ParhiR. SureshP. Transdermal delivery of Diltiazem HCl from matrix film: Effect of penetration enhancers and study of antihypertensive activity in rabbit model.J. Adv. Res.20167353955010.1016/j.jare.2015.09.00127222758
     [Google Scholar]
  31. AnsariK. SinghaiA.K. SaraogiG.K. PatilS. Transdermal drug delivery of salbutamol sulphate with different concentration of polymers.Int. J. Pharma Sci.201113
     [Google Scholar]
  32. BhatiaC. SachdevaM. BajpaiM. Formulation and evaluation of transdermal patch of pregabalin.Int. J. Pharma Sci.201232569
     [Google Scholar]
  33. El-NabarawiM.A. ShakerD.S. AttiaD.A. HamedS.A. In vitro skin permeation and biological evaluation of lornoxicam monolithic transdermal patches.Int. J. Pharm. Pharm. Sci.201352242248
     [Google Scholar]
  34. MandavaK. CherukuriS. BatchuU.R. CherukuriV. GanapuramK. Formulation and evaluation of transdermal drug delivery of topiramate.Int. J. Pharm. Investig.201771101710.4103/jphi.JPHI_35_1628405574
     [Google Scholar]
  35. JoshiA. KaurJ. KulkarniR. ChaudhariR. In-vitro and ex-vivo evaluation of raloxifene hydrochloride delivery using nano-transferosome based formulations.Int. J. Pharm. Investig.201845151
     [Google Scholar]
  36. SharmaV. YusufM. PathakK. Nanovesicles for transdermal delivery of felodipine: Development, characterization, and pharmacokinetics.Int. J. Pharm. Investig.20144311913010.4103/2230‑973X.13834225126525
     [Google Scholar]
  37. AnggrainiW. SagitaE. IskandarsyahI. Effect of hydrophilicity surfactants toward characterization and in vitro transfersomes penetration in gels using Franz diffusion test.Int J Appl Pharm2017911211510.22159/ijap.2017.v9s1.67_74
     [Google Scholar]
  38. SinghA. BaliA. Formulation and characterization of transdermal patches for controlled delivery of duloxetine hydrochloride.J. Anal. Sci. Technol.2016712510.1186/s40543‑016‑0105‑6
     [Google Scholar]
  39. PrajapatiST PatelCG PatelCN Formulation and evaluation of transdermal patch of repaglinide.IntSch Res Notices2011201110.5402/2011/651909
     [Google Scholar]
  40. QushawyM. NasrA. Abd-AlhaseebM. SwidanS. Design, optimization and characterization of a transfersomal gel using miconazole nitrate for the treatment of candida skin infections.Pharmaceutics20181012610.3390/pharmaceutics1001002629473897
     [Google Scholar]
  41. ShahS. PrabhuP. GundadS. Formulation development and investigation of domperidone transdermal patches.Int. J. Pharm. Investig.20111424024610.4103/2230‑973X.9300823071950
     [Google Scholar]
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Fabrication, Optimization, and Evaluation of Transdermal Patch: As an Alternative and Effective Transdermal Delivery System for Nebivolol HCl
Pharm. Nanotechnol. 12, 79 (2024); https://doi.org/10.2174/2211738511666230601103658
/content/journals/pnt/10.2174/2211738511666230601103658
/content/journals/pnt/10.2174/2211738511666230601103658
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  • Article Type:     Research Article
Keyword(s): hypertension; Nebivolol HCl; optimization; transdermal delivery; transferosomal patches; transferosomes

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