OPTIMIZING TRANSDERMAL PATCH FORMULATION FOR ENHANCED DELIVERY OF RIVAROXABAN: A COMPREHENSIVE DESIGN OF EXPERIMENTS APPROACH

RAMA RAO NADENDLA; P. V. L. N. PRIYANKA

doi:10.22159/ijpps.2024v16i12.51075

Authors

RAMA RAO NADENDLA Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Chalapathi Nagar, Lam, Guntur-522034, Andhra Pradesh, India
P. V. L. N. PRIYANKA Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Chalapathi Nagar, Lam, Guntur-522034, Andhra Pradesh, India https://orcid.org/0000-0002-7387-5225

DOI:

https://doi.org/10.22159/ijpps.2024v16i12.51075

Keywords:

Rivaroxaban, Transdermal patches, Factorial design, In vitro drug release, Hydroxypropyl methylcellulose

Abstract

Objective: To optimize Trans Dermal Patches (TDPs) of rivaroxaban using Poly Vinyl Pyrrolidone (PVP K30) and Hydroxypropyl Methyl Cellulose E50(HPMC E50) as hydrophilic polymers, Propylene Glycol(PG) as a plasticizer, and permeation enhancer.

Methods: TDPs were crafted using a solvent casting technique with a 2-level, 3-factor factorial design. These patches were assessed for thickness, folding endurance, in vitro drug release, drug content, and moisture uptake and loss. An 8-stage diffusion cell apparatus facilitated in vitro drug release testing. The independent variables were HPMC E50, PVP K30, and PG. The change in the concentration of these independent variables resulted in the optimization of the transdermal patch. The dependent variables were the thickness, folding endurance, and in vitro diffusion.

Results: The patch thickness ranged from 0.311±0.3 to 0.334±0.6. Folding endurance ranged from 58±0.7 92±6. The in vitro drug release ranged from 52.36% to 95.58%. The percentage drug content ranged from 83.58±0.4 to 95.26±0.5. The percentage of moisture content absorbed ranged from 21.36±0.13% to 25.54±0.26%. The percentage of moisture lost ranged from 1.01% to 2.31%.

Conclusion: PG increased the release of rivaroxaban because it permeated the membrane. HPMC E50 is highly soluble. Thus, rivaroxaban patches are potentially suitable transdermal drug delivery systems.

Downloads

Download data is not yet available.

References

John L, Kumar A. Comparison of amlodipine transdermal patches using hydroxypropyl methylcellulose and chitosan. Asian J Pharm Clin Res. 2014 Jan 1;7(1):86-90.

Das A, Ahmed AB. Formulation and evaluation of transdermal patch of indomethacin containing patchouli oil as a natural penetration enhancer. Asian J Pharm Clin Res. 2017 Aug;10(11):320-5. doi: 10.22159/ajpcr.2017.v10i11.20926.

Evans VJ, Lawrence M, Whitley J, Johns C, Pillai S, Hawkins K. The treatment effect of rivaroxaban on clot characteristics in patients who present acutely with first-time deep vein thrombosis. Clin Hemorheol Microcirc. 2022 Jan 1;80(2):139-51. doi: 10.3233/CH-201030, PMID 33682699.

Nadendla RR, Rao KS, Kanna S, Satyanarayana J, Mrudhvani C. Preparation and evaluation of spray dried powder of Trigonella foenum graecum seeds as suspending agents to develop RXB nanosuspension. Indian J Biochem Biophys. 2024 Jan 29;61(2):105-17. doi: 10.56042/ijbb.v61i2.6922.

Kanna S, Nadendla RR, Satyanarayana J, Karthikeya V, Sonu MV, Bhargavi PN. Formulation and evaluation of fast-dissolving oral film of rivaroxaban. J Young Pharm. 2023 Dec 7;15(4):687-95. doi: 10.5530/jyp.2023.15.94.

Patel RP, Patel G, Baria A. Formulation and evaluation of transdermal patch of aceclofenac. Int J Drug Del. 2009 Jul;1(1):41-51. doi: 10.5138/ijdd.2009.0975.0215.01005.

Cherukuri S, Batchu UR, Mandava K, Cherukuri V, Ganapuram KR. Formulation and evaluation of transdermal drug delivery of topiramate. Int J Pharm Investig. 2017 Jan;7(1):10-7. doi: 10.4103/jphi.JPHI_35_16, PMID 28405574.

Alam MI, Alam N, Singh V, Alam MS, Ali MS, Anwer T. Type preparation and evaluation of transdermal patch: a review. World J Pharm Pharm Sci. 2013 May 21;2(4):2199-233.

Kumar SS, Behury B, Sachinkumar P. Formulation and evaluation of transdermal patch of stavudine. Dhaka Univ J Pharm Sci. 2013 Sep 2;12(1):63-9. doi: 10.3329/dujps.v12i1.16302.

Satturwar PM, Fulzele SV, Dorle AK. Evaluation of polymerized rosin for the formulation and development of transdermal drug delivery system: a technical note. AAPS Pharm Sci Tech. 2005;6(4):E649-54. doi: 10.1208/pt060481, PMID 16408867.

Zakir S, Banu SK, Fatima SN, Jahan T, Wajida F, Sireesha P. Formulation and evaluation of transdermal patches of ketoprofin by using different polymers. Asian J Pharm Res Dev. 2015 Nov-Dec;3(6):1-11.

Budhathoki U, Gartoulla K, Shakya S. Formulation and evaluation of transdermal patches of atenolol. Indonesian J Pharm. 2016 Dec;27(4):27(4):196. doi: 10.14499/indonesianjpharm27iss4pp196.

Yadav AV, Urade MN. Formulation and evaluation of chitosan-based transdermal patches of lornoxicam for prolonged drug release and to study the effect of permeation enhancer. Indian J Pharm Educ Res. 2019 Jan;53(1):88-96. doi: 10.5530/ijper.53.1.12.

Kriplani P. Formulation and evaluation of transdermal patch of diclofenac sodium. Glob J Pharm Pharm Sci. 2018;4(5):1-4. doi: 10.19080/GJPPS.2018.04.555647.

Shivalingam MR, Balasubramanian AR, Ramalingam KO. Formulation and evaluation of transdermal patches of pantoprazole sodium. Int J App Pharm. 2021 Sep 7;13(5):287-91. doi: 10.22159/ijap.2021v13i5.42175.

Ananthalakshmi D, Sravya E, Rakesh K, Aishwarya P, Sivaparvathi S, Prasanna VK. Formulation and evaluation of transdermal patches of metoprolol succinate. World J Pharm Res. 2023;12(4):1503-14. doi: 10.20959/wjpr20234-27368.

https://www.businessresearchinsights.com/market-reports.market-108902:RXB#:~:text=The%20global%20RXB%20market%20size.p.10.19%25%20during%20the%20forecast%20period. [Last accessed on 05 May 2024].

Nadendla R Andjuluri, Satyanarayana and Doppalapudi, Sai and Pyda, Venkata and Tadiboina, Avinash and Addanki, Vishnuvarddhaan and Kalluri, Sriharshavardhan. Physicochemical characterization of RXB and compatibility studies with its pharmaceutical excipients: life sciences pharma. International Journal of Life Science and Pharma Research. 2021;11(3):25-32. doi: 10.22376/ijpbs/lpr.2021.11.3:25-P32.