TRANSDERMAL DELIVERY OF CALCIUM CHANNEL BLOCKER: DEVELOPMENT AND CHARACTERIZATION

Surya Teja SP; Manisha Khandelwal; Chitra V; Damodharan N

doi:10.22159/ajpcr.2017.v10i8.15910

Authors

Surya Teja SP Department of Pharmaceutics, SRM College of Pharmacy, SRM University, Kattankulathur, Chennai, Tamil Nadu, India.
Manisha Khandelwal Department of Pharmaceutics, SRM College of Pharmacy, SRM University, Kattankulathur, Chennai, Tamil Nadu, India.
Chitra V Department of Pharmaceutics, SRM College of Pharmacy, SRM University, Kattankulathur, Chennai, Tamil Nadu, India.
Damodharan N Department of Pharmaceutics, SRM College of Pharmacy, SRM University, Kattankulathur, Chennai, Tamil Nadu, India.

DOI:

https://doi.org/10.22159/ajpcr.2017.v10i8.15910

Keywords:

Calcium channel blocker, Felodipine, Transdermal, Permeation

Abstract

Â

Â Objective: Felodipine, a BCS class II calcium channel blocker, is used in the management of hypertension and angina pectoris. Due to the poor solubility and low bioavailability of the drug, there is a necessity to design an alternative route to achieve a constant plasma concentration of felodipine for its maximum therapeutic utility and can be achieved by transdermal route.

Methods: In this study, matrix type transdermal patches were prepared using different combinations of hydrophilic polymer, namely, polyvinylpyrrolidone (PVP) and hydrophobic polymer, namely, ethyl cellulose (EC) by solvent evaporation technique and were subjected for characterization.

Results: The Fourier transform infrared studies confirmed the compatibility between drug and polymers. Hydrophilic nature of the polymers greatly influenced physical characteristics and dissolution rate. Equal percentage of PVP and EC yielded patches with good folding endurance. The concentration of plasticizer present in the patches gave them desired folding endurance, and it increased with the presence of hydrophilic polymer. The formulation with highest PVP concentration, F3, exhibited a maximum drug release of 96.23% for 24 hrs. While the formulation with highest EC concentration, F5, exhibited only 74.45% drug release for 24 hrs.

Conclusion: From the data, formulation F2 (PVP/EC, 2:1) can be concluded as best formulation due to its desired physical characteristics, good initial drug release, sustained release behavior, and good in vitro permeation. This formulation can be further studied in a clinical scenario.

Downloads

Download data is not yet available.

References

Prausnitz MR, Langer R. Transdermal drug delivery. Nat Biotechnol 2008;26(11):1261-8.

Pastore MN, Kalia YN, Horstmann M, Roberts MS. Transdermal patches: History, development and pharmacology. Br J Pharmacol 2015;172(9):2179-209.

Anderson DT, Muto JJ. Duragesic transdermal patch: Postmortem tissue distribution of fentanyl in 25 cases. J Anal Toxicol 2000;24(7):627-34.

Singh VK, Pokhariyal T, Tiwari AK. Transdermal drug delivery system for non-steroidal anti-inflammatory drugs. Indo Am J Pharm Res 2013;3(5):3588-5.

Peter JH, Maisha KF, Terri MW. Appropriate use of transdermal drug delivery systems. J Nurs Educ Pract 2013;3(10):129-38.

Alexandra F, Clementina CI, Angela N. The assay of felodipine by second derivative spectrophotometry. Farmacia 2016;64(1):143-6.

Santhosh K, Boddeda B. Research on felodipine fast dissolving tablets using solid dispersion. Int J Chem Sci Technol 2012;4(1):223-34.

Kumar DS, Reddy A. Formulation and evaluation of mouth dissolving tablets of felodipine. Asian J Pharm Clin Res 2011;4(1):1974-41.

Prabhakar D, Sreekanth J, Jayaveera KN. Development and evaluation of transdermal patches of azelnidipine. Int J Pharm Pharm Sci 2013;5(3):805-10.

Yadav V. Transdermal drug delivery system: Review. Int J Curr Pharm Res 2012;3(2):376-82.

Subramanian S, Rajkapoor B, Vijayaraghavan C. Design and physico-chemical evaluation of cetirizine dihydrochloridetransderml patches. Int J Res Pharm Sci 2011;2(3):518-20.

Kumar De P, Mallick S, Mukherjee B, Sengupta S, Pattnaik S, Chakraborty S. Optimization of In - vitro permeation pattern of ketorolac tromethamine transdermal patches. Iran J Pharm Res 2011;10(2):193-201.

Prabhakar D, Aparna C, Nalini S, Sadanandam M. Development of transdermal patches for bisoprololfumarate. J Pharm Res 2012;5(3):1338-41.

Prajapati ST, Patel CG, Patel CN. Formulation and evaluation of transdermal patch of repaglinide. ISRN Pharm 2011;2011:651909.

Kapoor D, Vyas RB, Lad C, Patel M, Tyagi BL. Formulation development, optimization and characterization of transdermal patches of dihydropyridine based calcium channel blocker. Int J Inst Pharm Life Sci 2014;4(6):98-7.

Sanjoy M, Thimmasetty J, Ratan GN, Kilarimath BH. Formulation and evaluation of carvedilol transdermal patches. Int Res J Pharm 2011;2(1):237-48.

Mamatha T, Jangala VR, Anitha N. Development and physicochemical, in vitro and in vivo evaluation of transdermal patches of Zaleplon. Indian J Pharm Educ Res 2013;47(4):49-58.

Ramkanth S, Alagusundaram M, Gnanaprakash K, Rao KM, Mohammed ST, Paneer K, et al. Design and characterization of matrix type transdermal drug delivery system using metoprolol tartarate. Int J Pharm Res 2010;1(1):1-5.

Deepikareddy H, Rao BB, Shashanka V. Formulation of candesartan cilexetil transdermal patches in-vitro and ex-vivo characterization. Int J Appl Pharm 2016;6(1):17-22.

Priyanka A, Biswajit M. Design, development, physicochemical, and in vitro and in vivo evaluation of transdermal patches containing diclofenac diethylammonium salt. J Pharm Sci 2002;91(9):2076-89.

Damodharan N, Gopa R, Soma G, Mukherjee B. Skin permeation of rosiglitazone from transdermal matrix patches. Pharmtech 2010;34(5):56-72.

Biswajit M, Kousik S, Gurudutta P, Soma G. Preparation, characterization and in-vitro evaluation of sustained release protein-loaded nanoparticles based on biodegradable polymers. Int J Nanomed 2008;3(4):487-96.

Pathan IB, Setty CM. Chemical penetration enhancers for transdermal drug delivery systems. Trop J Pharm Res 2009;8:173-9.