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Pharmaceutical Nanotechnology

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ISSN (Print): 2211-7385
ISSN (Online): 2211-7393

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Research Article

Fabrication, Optimization, and Evaluation of Transdermal Patch: As an Alternative and Effective Transdermal Delivery System for Nebivolol HCl

Author(s): Archana S. Patil*, Shraja Birkodi, Rajashree S. Masareddy and Manisha Rajpurohit

Volume 12, Issue 1, 2024

Published on: 17 July, 2023

Page: [79 - 89] Pages: 11

DOI: 10.2174/2211738511666230601103658

Price: $65

Abstract

Background: 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.

Objectives: 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.

Methods: 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, in-vitro and ex-vivo permeation, skin irritancy, and stability studies.

Results: 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. In-vitro and ex-vivo 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.

Conclusion: 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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[1]
Saju MD, Allagh KP, Scaria L, Joseph S, Thiyagarajan JA. Prevalence, awareness, treatment, and control of hypertension and its associated risk factors: Results from baseline survey of Swades family cohort study. Int J Hypertens 2020; 2020(139): 1-7.
[http://dx.doi.org/10.1155/2020/4964835]
[2]
Al-Dhubiab B, Nair AB, Kumria R, Attimarad MA, Harsha S. Development and evaluation of nebivolol hydrochloride nanocrystals impregnated buccal film. Farmacia 2019; 67(2): 282-9.
[http://dx.doi.org/10.31925/farmacia.2019.2.12]
[3]
Bijani M, Parvizi S, Dehghan A, et al. Investigating the prevalence of hypertension and its associated risk factors in a population-based study: Fasa PERSIAN COHORT data. BMC Cardiovasc Disord 2020; 20(1): 503.
[http://dx.doi.org/10.1186/s12872-020-01797-3]
[4]
Tripati KD. Essential of medical pharmacology. (6th ed.). New Delhi: Jaypee Brothers 2008; pp. 503-4.
[http://dx.doi.org/10.5005/jp/books/10282]
[5]
McEvoy GK, Ed. AHFS drug information American society of health-system pharmacists. 2000; p. 1888.
[6]
Vijayanand P, Patil JS, Reddy MV. Formulation and comparative pharmacokinetic evaluation of orodispersible tablets and films of nebivolol hydrochloride. J Pharm Investig 2015; 45(2): 237-47.
[http://dx.doi.org/10.1007/s40005-014-0169-5]
[7]
Wang SJ, Sander GE. Nebivolol/valsartan combination for the treatment of hypertension: A review. Future Cardiol 2021; 17(4): 573-83.
[http://dx.doi.org/10.2217/fca-2020-0079] [PMID: 33064027]
[8]
Shinde AJ, Waghmare DS, Dalvi RS, More HN. Formulation, design and characterization of muco adhesive buccal film of nebivolol using factorial design. Int J Pharma Sci 2018; 9(5): 1797-805.
[9]
Liu JY, Guo LN, Peng WZ, et al. Efficacy and safety of nebivolol in hypertensive patients: A meta-analysis of randomized controlled trials. J Int Med Res 2020; 48(10)
[http://dx.doi.org/10.1177/0300060520931625] [PMID: 33081551]
[10]
Tanwar H, Sachdeva R. Transdermal drug delivery system: A review. Int J Pharma Sci 2016; 7(6): 2274.
[11]
Shah VP, Tymes NW, Skelly JP. In vitro release profiles of clonidine transdermal therapeutic systems and scopolamine transdermal patches. Pharm Res 1989; 6(4): 346-51.
[http://dx.doi.org/10.1023/A:1015962911344] [PMID: 2748524]
[12]
Nayak BS, Ellaiah P, Pattanayak D, Das S. Formulation design preparation and in vitro characterization of nebivolol transdermal patches. Asian J Pharm 2014; 5(3): 196-202.
[13]
Al Hanbali OA, Khan HMS, Sarfraz M, Arafat M, Ijaz S, Hameed A. Transdermal patches: Design and current approaches to painless drug delivery. Acta Pharm 2019; 69(2): 197-215.
[http://dx.doi.org/10.2478/acph-2019-0016] [PMID: 31259729]
[14]
Sachan R, Parashar T, Soniya SV, et al. Drug carrier transfersomes: A novel tool for transdermal drug delivery system. Int J Res Dev Pharm Life Sci 2013; 2(2): 309-16.
[15]
Ramadon D, McCrudden MT, Courtenay AJ, Donnelly RF. Enhancement strategies for transdermal drug delivery systems: Current trends and applications. Drug Deliv Transl Res 2021; 1-34.
[PMID: 33474709]
[16]
Salem HF, Kharshoum RM, Abou-Taleb HA, Naguib DM. Nano sized transferosome-based intranasal in situ gel for brain targeting of resveratrol: formulation, optimization, in vitro evaluation, and in vivo pharmacokinetic study. AAPS PharmSciTech 2019; 20(5): 181.
[http://dx.doi.org/10.1208/s12249-019-1353-8] [PMID: 31049748]
[17]
Kumar A. Transferosome: A recent approach for transdermal drug delivery. J Drug Deliv Ther 2018; 8(5-s): 100-4.
[http://dx.doi.org/10.22270/jddt.v8i5-s.1981]
[18]
Solanki D, Kushwah L, Motiwale M, Chouhan V. Transferosomes-a review. World J Pharm Pharm Sci 2016; 12(5): 435-49.
[19]
Thakur N, Jain P, Jain V. Formulation development and evaluation of transferosomal gel. J Drug Deliv Ther 2018; 8(5): 168-77.
[http://dx.doi.org/10.22270/jddt.v8i5.1826]
[20]
Parejiya PB, Patel RC, Mehta DM, Shelat PK, Barot BS. Quick dissolving films of nebivolol hydrochloride: Formulation and optimization by a simplex lattice design. J Pharm Investig 2013; 43(4): 343-51.
[http://dx.doi.org/10.1007/s40005-013-0080-5]
[21]
Jatav V, Saggu J, Sharma A, Sharma A, Jat R. Design, development and permeation studies of nebivolol hydrochloride from novel matrix type transdermal patches. Adv Biomed Res 2013; 2(1): 62.
[http://dx.doi.org/10.4103/2277-9175.115813] [PMID: 24223377]
[22]
Sapkota R, Dash AK. Liposomes and transferosomes: A breakthrough in topical and transdermal delivery. Ther Deliv 2021; 12(2): 145-58.
[http://dx.doi.org/10.4155/tde-2020-0122] [PMID: 33583219]
[23]
Dudhipala N, Phasha Mohammed R, Adel Ali Youssef A, Banala N. 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 2020; 46(8): 1334-44.
[http://dx.doi.org/10.1080/03639045.2020.1788069] [PMID: 32598194]
[24]
Balata GF, Faisal MM, Elghamry HA, Sabry SA. Preparation and characterization of ivabradineHCltransfersomes for enhanced transdermal delivery. J Drug Deliv Sci Technol 2020; 60: 101921.
[http://dx.doi.org/10.1016/j.jddst.2020.101921]
[25]
Majukar S, Dandagi PM, Kurangi BK. Design and characterization of transfersomal patch of aceclofenac as a carrier for transdermal delivery. Int J Pharm Biol Sci 2019; 9(1): 1138-47.
[26]
Jagwani S, Jalalpure S, Dhamecha D, Jadhav K, Bohara R. Pharmacokinetic and pharmacodynamic evaluation of resveratrol loaded cationic liposomes for targeting hepatocellular carcinoma. ACS Biomater Sci Eng 2020; 6(9): 4969-84.
[http://dx.doi.org/10.1021/acsbiomaterials.0c00429] [PMID: 33455290]
[27]
Marwah H, Garg T, Rath G, Goyal AK. Development of transferosomal gel for trans-dermal delivery of insulin using iodine complex. Drug Deliv 2016; 23(5): 1636-44.
[http://dx.doi.org/10.3109/10717544.2016.1155243] [PMID: 27187718]
[28]
Surti N, Parmar N, Bhadsavle S, Patel V. Transfersomes loaded transdermal drug delivery system of methotrexate for rheumatoid arthritis. World J Pharm Pharm Sci 2015; 4(12): 958-68.
[29]
Yadav PK, Mishra S. transdermal patch of an antihypertensive drug: Its development and evaluation. World J Pharm Res 2017; 6(4): 1355-74.
[http://dx.doi.org/10.20959/wjpr20174-8214]
[30]
Parhi R, Suresh P. Transdermal delivery of Diltiazem HCl from matrix film: Effect of penetration enhancers and study of antihypertensive activity in rabbit model. J Adv Res 2016; 7(3): 539-50.
[http://dx.doi.org/10.1016/j.jare.2015.09.001] [PMID: 27222758]
[31]
Ansari K, Singhai AK, Saraogi GK, Patil S. Transdermal drug delivery of salbutamol sulphate with different concentration of polymers. Int J Pharma Sci 2011; 1(3)
[32]
Bhatia C, Sachdeva M, Bajpai M. Formulation and evaluation of transdermal patch of pregabalin. Int J Pharma Sci 2012; 3(2): 569.
[33]
El-Nabarawi MA, Shaker DS, Attia DA, Hamed SA. In vitro skin permeation and biological evaluation of lornoxicam monolithic transdermal patches. Int J Pharm Pharm Sci 2013; 5(2): 242-8.
[34]
Mandava K, Cherukuri S, Batchu UR, Cherukuri V, Ganapuram K. Formulation and evaluation of transdermal drug delivery of topiramate. Int J Pharm Investig 2017; 7(1): 10-7.
[http://dx.doi.org/10.4103/jphi.JPHI_35_16] [PMID: 28405574]
[35]
Joshi A, Kaur J, Kulkarni R, Chaudhari R. In-vitro and ex-vivo evaluation of raloxifene hydrochloride delivery using nano-transferosome based formulations. Int J Pharm Investig 2018; 45: 151.
[36]
Sharma V, Yusuf M, Pathak K. Nanovesicles for transdermal delivery of felodipine: Development, characterization, and pharmacokinetics. Int J Pharm Investig 2014; 4(3): 119-30.
[http://dx.doi.org/10.4103/2230-973X.138342] [PMID: 25126525]
[37]
Anggraini W, Sagita E, Iskandarsyah I. Effect of hydrophilicity surfactants toward characterization and in vitro transfersomes penetration in gels using Franz diffusion test. Int J Appl Pharm 2017; 9: 112-5.
[http://dx.doi.org/10.22159/ijap.2017.v9s1.67_74]
[38]
Singh A, Bali A. Formulation and characterization of transdermal patches for controlled delivery of duloxetine hydrochloride. J Anal Sci Technol 2016; 7(1): 25.
[http://dx.doi.org/10.1186/s40543-016-0105-6]
[39]
Prajapati ST, Patel CG, Patel CN. Formulation and evaluation of transdermal patch of repaglinide. IntSch Res Notices 2011; 2011.
[http://dx.doi.org/10.5402/2011/651909]
[40]
Qushawy M, Nasr A, Abd-Alhaseeb M, Swidan S. Design, optimization and characterization of a transfersomal gel using miconazole nitrate for the treatment of candida skin infections. Pharmaceutics 2018; 10(1): 26.
[http://dx.doi.org/10.3390/pharmaceutics10010026] [PMID: 29473897]
[41]
Shah S, Prabhu P, Gundad S. Formulation development and investigation of domperidone transdermal patches. Int J Pharm Investig 2011; 1(4): 240-6.
[http://dx.doi.org/10.4103/2230-973X.93008] [PMID: 23071950]

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