Research Journal of Pharmaceutical Dosage Form and Technology

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Formulation Development of Tranexamic Acid loaded Transethosomal Patch for Melasma


Affiliations
1 Department of Pharmaceutics, Prin. K. M. Kundnani College of Pharmacy, Cuffe Parade, Colaba, Mumbai 400005,, India
     

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Nanotechnology based drug delivery systems are employed to overcome the hitches associated with conventional therapies. Melasma is a chronic, acquired, therapeutically challenging, universally relapsing hyperpigmentation disorder that causes greyish-brown spots on the skin, mainly on the face. Tranexamic acid (TXA) is a newer medication used to treat melasma that can be administered topically as well as orally. TXA has an oral bioavailability of 30-50%. The current study aimed to create a transethosomal (TEL) patch, for transdermal delivery of TXA for the treatment of melasma as an alternative to the oral route's hindrance. The cold technique was used to prepare TEL. They are composed of phospholipid (Phospholipon 90G), ethanol, water, and an edge activator (sodium cholate). Drug excipient compatibility study was done using Differential scanning colorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy techniques. TEL batches were further characterized based on particle size (PS) and entrapment efficiency (EE). The optimized batch's PS and EE were found to be 72 nm and 94%, respectively. The average zeta potential was -16 mV, indicating a stable formulation. Vesicular morphology was monitored by Scanning electron microscopy (SEM) analysis. The in vitro and ex vivo release of TXA was evaluated by Franz diffusion study and showed the release of about 93.97% over the period of 24 hrs, which was better than that of a conventional topical cream. All of the above findings showed that TEL may be a good carrier alternative for delivery of TXA into deeper layers, and hence good for treating melasma.

Keywords

Tranexamic acid, Transethosome, Melasma, Transdermal patch, Nanotechnology.
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  • Grimes PE, et al. New oral and topical approaches for the treatment of melasma. International Journal of Women's Dermatology. 2018 Nov 20; 5(1): 30-36. doi:10.1016/j.ijwd.2018.09.004.

  • George A. Tranexamic acid: An emerging depigmenting agent. Pigment Int 2016; 3(2): 66–71.doi: 10.4103/2349-5847.196295.

  • Taraz M, et al. Tranexamic acid in treatment of melasma: A comprehensive review of clinical studies. Dermatol Ther 2017; 30(3): e12465.doi:10.1111/dth.12465

  • Cai J, et al. The many roles of tranexamic acid: An overview of the clinical indications for TXA in medical and surgical patients. European journal of haematology 2020; 104(2): 79- 87.doi:10.1111/ejh.13348.

  • Sheu SL. Treatment of melasma using tranexamic acid: what's known and what's next. Cutis 2018; 101(2):E7–E8.

  • Xu Y, et al. Efficacy of functional microarray of microneedles combined with topical tranexamic acid for melasma: A randomized, self-controlled, split-face study. Medicine (Baltimore) 2017; 96(19): e6897.doi:10.1097%2FMD.0000000000006897

  • Del Rosario, et al. Randomized, placebo-controlled, double-blind study of oral tranexamic acid in the treatment of moderate-to severe melasma. Journal of the American Academy of Dermatology 2018; 78(2): 363-369.doi:10.1016/j.jaad.2017.09.053

  • Kaur A, et al. Tranexamic acid in melasma: a review. Pigment Int 2020; 7(1):12-25.doi: 10.4103/Pigmentinternational.Pigmentinternational_

  • Tan AWM, et al. Oral tranexamic acid lightens refractory melasma. Australas J Dermatol 2017; 58(3):e105- e108.doi:10.1111/ajd.12474.

  • Zhang L, et al. Tranexamic acid for adults with melasma: a systematic review and meta-analysis. BioMed research international 2018; doi:10.1155/2018/1683414.

  • McKesey J, et al. Melasma treatment: an evidence-based review. American journal of clinical dermatology 2020; 21(2):173- 225.doi:10.1007/s40257-019-00488-w.

  • Rodrigues M, Pandya A. Melasma: Clinical diagnosis and management options. Australas J Dermatol 2015; 56(3):151– 63.doi:10.1111/ajd.12290.

  • Sarkar R., et al. Melasma in men: A review of clinical, etiological, and management issues. The Journal of clinical and aesthetic dermatology 2018 11(2), p.53-59.

  • Ikino JK, et al. Melasma and assessment of the quality of life in Brazilian women. An Bras Dermatol 2015; 90(2):196– 200.doi:10.1590/abd1806-4841.20152771

  • Aishwarya K, et al. Current concepts in melasma - A review article. J Skin Sex Transm Dis 2020; 2(1):13-17.doi: 10.25259/JSSTD_34_2019

  • Beedha. S. et al. Formulation and Characterization of Tramadol HCl Transdermal Patch. Asian J. Pharm. Tech. 2018; 8 (1):23-28. doi: 10.5958/2231-5713.2018.00004.1

  • Shaji J, Bajaj R. Formulation Development of 5-Fluorouracil Transethosomes for Skin Cancer Therapy. Ijppr. Human 2017; Vol. 11 (1): 453-464.

  • Borkar S, et al. Tamoxifen Citrate Loaded Solid Lipid Nanoparticles- A Novel Approach In The Treatment of ER+ Breast Cancer. Research J. Pharma. Dosage Forms and Tech. 2009; 1(2): 143-149.

  • Duan XD, et al. Formulation and Development of DendrimerBased Transdermal Patches of Meloxicam for the Management of Arthritis, Trop J Pharm Res 2015; 14(4): 583-590.doi: https://doi.org/10.4314/tjpr.v14i4.4.

  • Talib S., et al. Chitosan-chondroitin based artemether loaded nanoparticles for transdermal drug delivery system. Journal of Drug Delivery Science and Technology 2021; 61:102281.doi: 10.1016/j.jddst.2020.102281

  • Attama, A. A., Momoh, M.A., Builders, P.F. Lipid nanoparticulate drug delivery system: a revolution in dosage form design and development. Recent adv. Novel drug carrier Syst. 2012; 5:107- 140.

  • Gavini, MV, et al. Formulation and Invitro Evaluation of Nanoparticulate Drug Delivery System Loaded With 5- Fluorouracil. Res. J. Pharm. Dosage Form. and Tech. 2014; 6(4): 243-248.

  • Jessy Shaji, Monika Kumbhar. Linezolid Loaded Biodegradable Polymeric Nanoparticles Formulation and Characterization. Res. J. Pharm. Dosage Form. and Tech. 2018; 10(4): 272-278. doi: 10.5958/0975-4377. 2018.00040.X

  • Panigrahi L., Ghosal S. K. Formulation and evaluation of pseudo latex transdermal drug delivery system of terbutaline sulphate, Indian J Pharm Sci. 2002; 64(1): 79.

  • Patel R, et al. Formulation and Evaluation of Transdermal Patch of Aceclofenac. Research J. Pharma. Dosage Forms and Tech. 2009; 1(2): 108-115.doi: 10.5958/0975-4377.

  • Salve P, et al. Formulation and Evaluation of Solid Lipid Nanoparticle Based Transdermal Drug Delivery System for Alzheimer’s Disease. Res. J. Pharm. Dosage Form. and Tech. 2016; 8(2):73-80. doi: 10.5958/0975-4377.2016.00011.2

  • Tipre DN, Vavia PR. Formulation optimization and stability study of transdermal therapeutic system of nicorandil. Pharm. Dev. Technol. 2002; 7:325–32.doi:10.1081/PDT-120005729.

  • Singh V, et al. Formulation and Evaluation of Transdermal Patches of Nebivolol Hydrochloride. Research J. Pharma. Dosage Forms and Tech. 2012; 4(5): 272-277.

  • Wu IY, et al. Interpreting non-linear drug diffusion data: Utilizing Korsmeyer-Peppas model to study drug release from liposomes. Eur J Pharm Sci. 2019 October 1; 138: 105026.doi: 10.1016/j.ejps.2019.105026.

  • S. B. Gondkar, et al. Formulation Development and Characterization of Etodolac Loaded Transethosomes for Transdermal Delivery. Research J. Pharm. and Tech. 2017; 10(9): 3049-3057. doi: 10.5958/0974-360X.2017.00541.8

  • Rehman Q, et al. Role of Kinetic Models in Drug Stability. In: Akash M.S.H., Rehman K. (eds). Drug Stability and Chemical Kinetics. Springer, Singapore.2020 Nov 02; 155- 165.doi:10.1007/978-981-15-6426-0_11.

  • Singhvi G, Singh M. In-vitro drug release characterization models. Int J Pharm Stud Res. 2011; 2:77-84.

  • Rathore S, Pathak B. Formulation and Evaluation of Aceclofenacloaded Nanoparticles by Solvent Evaporation Method. Res. J. Pharma. Dosage Forms and Tech.2020; 12(4):237-244. doi: 10.5958/0975-4377.2020.00039.7

  • I.H.T. Guideline, Stability testing of new drug substances and products, Q1A (R2) 2003; current step. 4:1-24.

  • Arayne, M. S., et al. Spectrophotometric techniques to determine tranexamic acid: Kinetic studies using ninhydrin and direct measuring using ferric chloride. Journal of Molecular Structure 2008; 891(1-3), 475–480.doi:10.1016/j.molstruc.2008.04.026

  • Sinico, C, et al. Liposomes as carriers for dermal delivery of tretinoin: in vitro evaluation of drug permeation and vesicle–skin interaction. Journal of Controlled Release 2005; 103(1):123– 136.doi:10.1016/j.jconrel.2004.11.020.

  • T. Venkateswara Rao, Owku Ravi Kiran. Review: Transdermal patch. Research J. Pharma. Dosage Forms and Tech. 2013; 5(1): 12-16.

  • Shaji, J., and S. Garude. “Transethosomes and ethosomes for enhanced transdermal delivery of ketorolac tromethamine: a comparative assessment”. International Journal of Current Pharmaceutical Research 2014; 6(4):88-93.

  • J. Charles, Pouchert. The Aldrich library of infrared spectra. 2nd ed. ACS publication; 1972.

  • Silverstien R, Webster F, Kiemle D. Spectrometric identification of organic compounds.1st ed. New York Wiley; 2004.


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  • Formulation Development of Tranexamic Acid loaded Transethosomal Patch for Melasma

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Authors

Jessy Shaji
Department of Pharmaceutics, Prin. K. M. Kundnani College of Pharmacy, Cuffe Parade, Colaba, Mumbai 400005,, India
Shamika S. Parab Parab
Department of Pharmaceutics, Prin. K. M. Kundnani College of Pharmacy, Cuffe Parade, Colaba, Mumbai 400005,, India

Abstract


Nanotechnology based drug delivery systems are employed to overcome the hitches associated with conventional therapies. Melasma is a chronic, acquired, therapeutically challenging, universally relapsing hyperpigmentation disorder that causes greyish-brown spots on the skin, mainly on the face. Tranexamic acid (TXA) is a newer medication used to treat melasma that can be administered topically as well as orally. TXA has an oral bioavailability of 30-50%. The current study aimed to create a transethosomal (TEL) patch, for transdermal delivery of TXA for the treatment of melasma as an alternative to the oral route's hindrance. The cold technique was used to prepare TEL. They are composed of phospholipid (Phospholipon 90G), ethanol, water, and an edge activator (sodium cholate). Drug excipient compatibility study was done using Differential scanning colorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy techniques. TEL batches were further characterized based on particle size (PS) and entrapment efficiency (EE). The optimized batch's PS and EE were found to be 72 nm and 94%, respectively. The average zeta potential was -16 mV, indicating a stable formulation. Vesicular morphology was monitored by Scanning electron microscopy (SEM) analysis. The in vitro and ex vivo release of TXA was evaluated by Franz diffusion study and showed the release of about 93.97% over the period of 24 hrs, which was better than that of a conventional topical cream. All of the above findings showed that TEL may be a good carrier alternative for delivery of TXA into deeper layers, and hence good for treating melasma.

Keywords


Tranexamic acid, Transethosome, Melasma, Transdermal patch, Nanotechnology.

References