PREPARATION AND CHARACTERIZATION OF TRIFLUOPERAZINE LOADED TRANSDERMAL PATCHES FOR SUSTAINED RELEASE

Authors

  • ANJU PARAMBIL College of Pharmaceutical Sciences, Government Medical College, Kozhikode 673008, Kerala
  • SEENIVASAN PALANICHAMY Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education & Research, Porur, Chennai 600116, Tamil Nadu, India
  • ARUL KUTTALINGAM College of Pharmaceutical Sciences, Government Medical College, Kottayam 686008, Kerala
  • VELLAPANDIAN CHITRA SRM College of Pharmacy, SRM University, Kattankulathur 603203, Tamilnadu

DOI:

https://doi.org/10.22159/ijap.2021v13i6.42413

Keywords:

Trifluoperazine, Transdermal patches, Psychiatric disorders, Solvent casting, Sustained release

Abstract

Objective: The purpose of the present study was to formulate and evaluate the polymeric transdermal delivery system of antipsychotic drug Trifluoperazine (TFP) for sustained drug release.

Methods: A transdermal patch loaded with (TFP) was formulated by solvent casting technique. Polyvinyl pyrrolidone (PVP) K-30 and ethyl cellulose (EC) was used as a polymeric matrix with different ratios. Di n-butyl phthalate was used as a plasticizer. The parameters such as thickness, folding endurance and weight variation of the prepared patches were studied. The interaction study by attenuated total reflectance-infrared (ATR-IR) spectroscopy, X-ray diffraction and thermal analysis by differential scanning calorimetry (DSC) were performed. In vitro drug release study was performed by modified paddle over-disc technique.

Results: The infrared spectroscopic study confirmed the absence of any chemical interaction between TFP and selected polymers. All the prepared formulations showed folding endurance values ranging from 130-162 and a satisfactory drug loading of 90-95%. In in vitro drug release study, formulations PE-3 and PE-4 exhibited a sustained and stable cumulative release of 54 % and 48% respectively, at the end of 24 h. The DSC and XRD analysis proved the partial conversion of the drug from crystalline to amorphous form when integrated into the polymeric matrix.

Conclusion: The prepared transdermal formulations using polymers PVP and ethyl cellulose demonstrated their ability to sustain the release of TFP. The developed formulation could be exploited for multiday therapy of TFP for the effective treatment of schizophrenia with a simplified dosing regimen and enhanced patient compliance.

Downloads

Download data is not yet available.

References

Koch K, Mansi K, Haynes E, Adams CE, Sampson S, Furtado VA. Trifluoperazine versus placebo for schizophrenia. Cochrane Database Syst Rev. 2014;(1):CD010226. doi: 10.1002/14651858.CD010226.pub2, PMID 24414883.

Joint formulary committee. British National Formulary. BMJ 2008;56:191-5.

Isaac M, Holvey C. Transdermal patches: the emerging mode of drug delivery system in psychiatry. Ther Adv Psychopharmacol. 2012;2(6):255-63. doi: 10.1177/2045125312458311, PMID 23983984.

Siafaka PI, Barmpalexis P, Lazaridou M, Papageorgiou GZ, Koutris E, Karavas E, et al. Controlled release formulations of risperidone antipsychotic drug in novel aliphatic polyester carriers: data analysis and modelling. Eur J Pharm Biopharm. 2015;94:473-84. doi: 10.1016/j.ejpb.2015.06.027, PMID 26159838. ejpb.2015.06.027.

Mazzitelli S, Pagano C, Giusepponi D, Nastruzzi C, Perioli L. Hydrogel blends with adjustable properties as patches for transdermal delivery. Int J Pharm. 2013;454(1):47-57. doi: 10.1016/j.ijpharm.2013.06.081, PMID 23856160.

Jalhan S, Kaur K, Kaur P, K Jain U. Formulation and in vitro evaluation of transdermal matrix patches of doxophylline. Asian J Pharm Clin Res. 2016;9(5):140-5. doi: 10.22159/ajpcr.2016.v9i5.12774.

Citrome L, Zeni CM, Correll CU. Patches: established and emerging transdermal treatments in psychiatry. J Clin Psychiatry. 2019;80(4). doi: 10.4088/JCP.18nr12554, PMID 31318185.

Jung E, Lee EY, Choi HK, Ban SJ, Choi SH, Kim JS, Yoon IS, Kim DD. Development of drug-in-adhesive patch formulations for transdermal delivery of fluoxetine: in vitro and in vivo evaluations. Int J Pharm. 2015;487(1-2):49-55. doi: 10.1016/j.ijpharm.2015.04.012, PMID 25863117.

Hardainiyan SW, Kumar KR, Nandy BC, Saxena RI. Design, Formulation and in vitro drug release from transdermal patches containing imipramine hydrochloride as model drug. Int J Pharm Pharm Sci. 2017;9(6):220-5. doi: 10.22159/ijpps.2017v9i6.16851.

Das PS, Saha P. Design and characterisation of transdermal patches of phenformin hydrochloride. Int J Curr Pharm Sci. 2017;9(6):90-3. doi: 10.22159/ijcpr.2017v9i6.23437.

Walter JR, Xu S. Therapeutic transdermal drug innovation from 2000 to 2014: current status and outlook. Drug Discovery Today. 2015;20(11):1293-9. doi: 10.1016/j.drudis.2015.06.007, PMID 26116094.

Sachdeva V, Bai Y, Kydonieus A, Banga AK. Formulation and optimization of desogestrel transdermal contraceptive patch using crystallization studies. Int J Pharm. 2013;441(1-2):9-18. doi: 10.1016/j.ijpharm.2012.12.014, PMID 23262424. ijpharm.2012.12.014.

Mukherjee B, Mahapatra S, Gupta R, Patra B, Tiwari A, Arora P. A comparison between povidone-ethylcellulose and povidone-eudragit transdermal dexamethasone matrix patches based on in vitro skin permeation. Eur J Pharm Biopharm. 2005;59(3):475-83. doi: 10.1016/j.ejpb.2004.09.009, PMID 15760728.

Rajabalaya R, Rani S, David N, Khanam J, Nanda A. Effect of plasticizers on in vitro release and ex vivo permeation of chlorpheniramine maleate from ethyl cellulose polyvinyl pyrrolidone based matrix patches. Farmacia. 2013;61:975-90.

Koradia H, Butani S, Gohel M. Studies in oxcarbazepine microspheres employing plackett and burman design. Int J Pharm Pharm Sci. 2014;6:305-10.

Karki S, Kim H, Na SJ, Shin D, Jo K, Lee J. Thin films as an emerging platform for drug delivery. Asian J Pharm Sci. 2016;11(5):559-74. doi: 10.1016/j.ajps.2016.05.004.

Jaipakdee N, Pongjanyakul TH, Limpongsa EK. Preparation and characterization of poly (vinyl alcohol)-poly (vinyl pyrrolidone) mucoadhesive buccal patches for delivery of lidocaine HCL. Int J App Pharm. 2018;10(1):115-23. doi: 10.22159/ijap.2018v10i1.23208.

Kandavilli S, Nair V, Panchagnula R. Polymers in transdermal drug delivery systems. Pharm Technol. 2002;26:62-81.

Suksaeree J, Siripornpinyo P, Chaiprasit S. Formulation, characterization, and in vitro evaluation of transdermal patches for inhibiting crystallization of mefenamic acid. J Drug Delivery. 2017;2017:7358042. doi: 10.1155/2017/7358042, PMID 29259828.

Vieira MGA, Da Silva MA, Dos Santos LO, Beppu MM. Natural-based plasticizers and biopolymer films: a review. Eur Polym J. 2011;47(3):254-63. doi: 10.1016/j.eurpolymj.2010.12.011.

Arora P, Mukherjee B. 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. doi: 10.1002/jps.10200, PMID 12210054.

Veras KS, Fachel FNS, Pittol V, Garcia KR, Bassani VL, dos Santos V, et al. Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques. Saudi Pharm J. 2019;27(8):1138-45. doi: 10.1016/j.jsps.2019.09.010, PMID 31885473. jsps.2019.09.010.

Moffat AC, Osselton MD, Widdop B, Watts J. Clarke’s analysis of drugs and poisons. Vol. II. London: Pharmaceutical Press; 2011. p. 2193-4.

Nair RS, Ling TN, Abdul Shukkoor MS, Manickam B. Matrix type transdermal patches of captopril: Ex vivo permeation studies through excised rat skin. J Pharm Res. 2013;6(7):774-9. doi: 10.1016/j.jopr.2013.07.003.

Bhatt DC, Dhake AS, Khar RK, Mishra DN. Development and in vitro evaluation of transdermal matrix films of metoprolol tartrate. Yakugaku Zasshi. 2008;128(9):1325-31. doi: 10.1248/yakushi.128.1325, PMID 18758147.

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. doi: 10.1016/j.jare.2015.09.001. PMID 27222758.

Rajesh P, Gunasekaran S, Gnanasambandan T, Seshadri S. Molecular structure and vibrational analysis of trifluoperazine by FT-IR, FT-Raman and UV–vis spectroscopies combined with DFT calculations. Spectrochim Acta A Mol Biomol Spectrosc. 2015;137:1184-93. doi: 10.1016/j.saa.2014.08.100, PMID 25305610.

British Pharmacopoeia. Commission. Vol. II. British Pharmacopoeia. London; 2016.

Post A, Warren RJ, Zarembo JE. Trifluoperazine hydrochloride. Anal Profiles Drug Substances. 1981;9:543-81. doi: 10.1016/S0099-5428(08)60153-7.

Published

07-11-2021

How to Cite

PARAMBIL, A., PALANICHAMY, S., KUTTALINGAM, A., & CHITRA, V. (2021). PREPARATION AND CHARACTERIZATION OF TRIFLUOPERAZINE LOADED TRANSDERMAL PATCHES FOR SUSTAINED RELEASE. International Journal of Applied Pharmaceutics, 13(6), 186–191. https://doi.org/10.22159/ijap.2021v13i6.42413

Issue

Section

Original Article(s)

Most read articles by the same author(s)