FORMULATION, OPTIMIZATION, AND CHARACTERIZATION OF TRANSDERMAL DRUG DELIVERY SYSTEMS CONTAINING EPLERENONE

Authors

  • RAMESH SHINDE Department of Pharmaceutical Sciences, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies, Chennai, Tamil Nadu, India, Chennai, Tamilnadu, India
  • MALARKODI VELRAJ Department of Pharmaceutical Sciences, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies, Chennai, Tamil Nadu, India, Chennai, Tamilnadu, India

DOI:

https://doi.org/10.22159/ijap.2022v14i1.42827

Keywords:

TDDS, Eplerenone, ERS 100, in-vivo skin irritation study

Abstract

Objective: The proposed work was aimed at optimization, formulation, and characterization of transdermal patches of eplerenone for efficient transdermal delivery of the drug.

Methods: The log p estimation of eplerenone is 1.34, it was closer to standard worth. Log P value in a range of 1 to 4 indicates higher permeation through the skin. FTIIR study was carried out individually for drug, each polymer, and finished product (Patches) compared eplerenone and FTIR spectra of pure drug and polymer. The calibration curve of eplerenone in Phosphate buffer pH 6.8 was analyzed.

Results: The selected range of eplerenone was found to be linear. A regression coefficient (R2) at 245 nm was found to be 0.994. Drug content outcomes additionally discovered uniform in all clusters in a range of 97 % to 98 %, that batches arranged with ERS 100 show great mechanical properties contrast with different polymers however helpless glue properties. The flatness of 4 cm2 patches ranges from 348 ± 0.087 mg to 387 ± 0.527 mg. skin irritation it was produced irritation with negligible erythema following 10 days and unequivocal erythema, promptly obvious edema was produced following 12 days.

Conclusion: These after effects of the in-vivo skin irritation study recommended that advanced batch S9 doesn't show any kind of significant disturbance on rodent skin for as long as 14 days and it was securely utilized around 24 hrs. the optimized batch S9 drug was constantly discharged through the Wistar rodent skin up to 16 hr and the delivery design was like an in-vitro dissolution profile of the market product.

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References

Oza NA, Sahu AR, Patel DM, Patel PU, Patel LD, Koshia HG. Studies on optimization of the reservoir-type transdermal patch using carvedilol using 32 full factorial designs. International Journal of Research in Medicine. 2013 Sep;2(4):84Ǧ89.

Brajesh M, Naina K, Shashank S. Quantitative determination of Eplerenone in bulk drug and tablet dosage form by TLC/densitometry. Int J Pharm Life Sci 2011 June; 2: 502-5.

Charles T, Stier Jr. Eplerenone: a selective aldosterone blocker. Cardiovasc Drug Rev 2003 Feb; 21: 169-84.

Naresh Chandra Reddy M, Chandra Sekhar KB. Development and validation of gradient RP-HPLC for estimation of impurities in Eplerenone tablet dosage form. Int Res J Pharm ApplSci 2012 Aug; 2: 58-75.

Weinberger MH, Roniker B, Krause SL, Weiss RJ. Eplerenone, a selective Aldosterone blocker in mild-to-moderate hypertension. Am J Hypertens 2002 July; 15: 709-16.

White WB, Duprez D, St Hillaire R, Krause S, Roniker B, Kuse- Hamilton J, et al. Effects of the selective aldosterone blocker Eplerenone versus the calcium antagonist Amlodipine in systolic hypertension. Hypertension 2003 Dec; 41: 1021-6.

Moore TD, Nawarskas JJ, Anderson JR. Eplerenone: a selective aldosterone Receptor antagonist for hypertension and heart failure. Heart Dis 2003 May; 5: 354-63.

Patel RP, Patel G, Patel H, Baria A. Formulation and evaluation of transdermal patch of aceclofenac. Research Journal of Pharmaceutical Dosage Forms and Technology. 2009 Feb; 1(2): 108-15.

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;10(11):320-5.

Mishra AD, Khunt DM, Ghayal AH, Patel CN, Shah DR. Formulation and optimization of ethosomes for transdermal delivery of felodipine. Research Journal of Pharmacy and Technology. 2012 May; 5(12): 1509-17.

D Mishra A, N Patel C, R Shah D. Formulation and optimization of ethosomes for transdermal delivery of ropinirole hydrochloride. Current drug delivery. 2013 Oct 1; 10(5): 500-16.

Rao MR, Sonavane V, Kulkarni S, Magar M, Zope A, Karanjkar P. Design of transdermal patch of ketoprofen by full factorial design for the treatment of rheumatoid arthritis. Journal of Drug Delivery and Therapeutics. 2019 Mar 15; 9(2): 197-205.

Lankaranian D, Reis R, Henderer JD, Choe S, Moster MR. Comparison of single thickness and double thickness processed pericardium patch graft in glaucoma drainage device surgery: a single surgeon comparison of outcome. Journal of glaucoma. 2008 Jan 1; 17(1): 48-51.

Leo A, Hansch C, Elkins D. Partition Coefficients And Their Uses. Chemical Reviews 1971; 71(6): 525-554.

Nichols L. Step- By- Step Procedures For Melting Point Determination. Chemistry LibreText2021. https://chem.libretexts.org/Bookshelves/Organic_Chemistry/Book%3A_Organic_Chemistry_Lab_Techniques_(Nichols)/06%3A_Miscellaneous_Techniques/6.01%3A_Melting_Point/6.1D%3A__Step-by-Step_Procedures_for_Melting_Point_Determination

Jamakandi VG, Mulla JS, Vinay BL, Shivakumar HN. Formulation, characterization, and evaluation of matrix-type transdermal patches of a model antihypertensive drug. Asian Journal of Pharmaceutics (AJP): Free full-text articles from Asian J Pharm. 2014 Aug 28; 3(1).

Guyot M, Fawaz F. Design and in vitro evaluation of adhesive matrix for transdermal delivery of propranolol. International Journal of Pharmaceutics. 2000 Jun 20; 204(1-2): 171-82.

Wang J, Ruan J, Zhang C, Ye Y, Cai Y, Wu Y. Development and evaluation of the Sinomenine transdermal patch. Pakistan journal of pharmaceutical sciences. 2008 Oct 1; 21(4).

Aggarwal G, Dhawan S, Harikumar SL. Formulation, in vitro, and in vivo evaluation of matrix-type transdermal patches containing olanzapine. Pharmaceutical development and technology. 2013 Aug 1; 18(4): 916-25.

Parivesh S, Sumeet D, Abhishek D. Design, evaluation, parameters and marketed products of transdermal patches: A review. J. Pharm. Res. 2010 Feb; 3(2): 235-40.

Gaikwad KA. Transdermal drug delivery system: Formulation aspects and evaluation. International Journal of PharmTech Research 2013 Mar; 3(4): 2140-2148.

Darwhekar G, Jain DK, Patidar VK. Formulation and Evaluation of Transdermal Drug Delivery System of Clopidogrel Bisulfate, Asian Journal of Pharmacy and Life Science 2011 Jan; 1(3): 14-20.

Latheeshjlal L P. Phanitejaswini, Soujanya Y, Swapna U, Sarika V, Moulika G. Transdermal Drug Delivery Systems: An Overview. Int.J. Pharmatech Res 2011 Mar; 3(4): 1-8.

Kumar SR, Jain A, Nayak S. Development and Evaluation of Transdermal Patches of Colchicine. Der Pharmacia Lettre 2012 Apr; 4(1): 330-343.

Mutalik S, Udupa N. Glibenclamide Transdermal Patches, Physicochemical, Pharmacodynamic and Pharmacokinetic Evaluations. Journal of Pharmaceutical Sciences 2004 June; 93 (6): 1557-1594.

Mali AD, Bathe R, Patil M. An updated review on transdermal drug delivery systems. International Journal of Advances in Scientific Research 2015 Jan; 1(06): 244-254.

Bagchi A, Dey BK. Formulation, In- vitro Evaluations and Skin Irritation study of Losartan Potassium Transdermal Patches. Iranian Journal of Pharmaceutical Sciences 2010 June; 6(3): 163-170.

Keleb E, Sharma R, Mosa EB, Zaljahwi AZ. Transdermal drug delivery system- design and evaluation. International Journal of Advances in Pharmaceutical Sciences 2010 Feb; 1: 201–211.

Prajapati ST, Patel CG, Patel CN. Formulation and Evaluation of Transdermal Patch of Repaglinide. International Scholarly Notices 2011 Mar; https://doi.org/10.5402/2011/651909.

Kavitha K, Rajendra MM. Design and evaluation of transdermal films of lornoxicam. International Journal of Pharma and Bio Sciences. 2011 Jun 30; 2(2): 54-62.

Furuishi T, Io T, Fukami T, Suzuki T, Tomono K. Formulation and in vitro evaluation of pentazocine transdermal delivery system. Biological and Pharmaceutical Bulletin. 2008 Jul 1; 31(7): 1439-43.

Gutschke E, Bracht S, Nagel S, Weitschies W. Adhesion testing of transdermal matrix patches with a probe tack test–In vitro and in vivo evaluation. European journal of pharmaceutics and biopharmaceutics. 2010 Aug 1; 75(3): 399-404.

Saroha K, Yadav B, Sharma B. Transdermal patch: A discrete dosage form. Int J Curr Pharm Res. 2011 Apr; 3(3): 98-108.

Ravikumar R, Ganesh M, Senthil V, Ramesh YV, Jakki SL, Choi EY. Tetrahydro curcumin loaded PCL-PEG electrospun transdermal nanofiber patch: Preparation, characterization, and in vitro diffusion evaluations. Journal of Drug Delivery Science and Technology. 2018 Apr 1; 44: 342-8.

Pongjanyakul T, Prakongpan S, Priprem A. Acrylic matrix type nicotine transdermal patches: in vitro evaluations and batch-to-batch uniformity. Drug development and industrial pharmacy. 2003 Jan 1; 29(8): 843-53.

Jayakumar C, Kumar KD, Nesakumar D, Gandhi NN. International Journal of Pharmacy and Pharmaceutical Sciences. Int J Pharmacy and Pharm Sci.;2(3):124-5.

Sharma S, Aggarwal G, Dhawan S. Design and evaluation of Olanzapine transdermal patches containing vegetable oils as permeation enhancers. Scholars Research Library. 2010 Feb; 2(6): 84-98.

Gannon R, Vamshi Vishnu Y, Kishan V, Madhusudan Rao Y. Development of nitrendipine transdermal patches: in vitro and ex vivo characterization. Current Drug Delivery. 2007 Jan 1; 4(1): 69-76.

Pathan BI, Setty CM, Gupta VRM. Comparison of the effect of essential oils on the permeation of diclofenac diethylamine through various barriers. ActaPharmaceuticaSciencia 2008 Aug; 50(3): 219-228.

Marwah H, Garg T, Goyal AK, Rath G. Permeation enhancer strategies in transdermal drug delivery. Drug delivery 2014 Oct; 23(2): 564-578.

Kunta JR, Goskonda VR, Brotherton HO, Khan MA, Reddy IK. Effect of menthol and related terpenes on the percutaneous absorption of propranolol across excised hairless mouse skin. Journal of Pharmaceutical Sciences 1997 Nov; 86(12): 1369-1373.

Pfister WR, Hsieh DS. Permeation enhancers are compatible with transdermal drug delivery systems. Part I: selection and formulation considerations. Med Device Technol. 1990 Dec; 1(5): 48-55.

Pfister WR, Hsieh DS. Permeation enhancers are compatible with transdermal drug delivery systems. Part II: system dsignconsideations. Med Device Technol. 1990 July; 1(6): 28-33.

Norton BJ, Strube M. Guide for the Interpretation of Two-way Analysis of Variance. Physical Therapy 1986 Apr; 66(3): 402-412.

Kim HY. Statistical notes for clinical researchers: Two-way analysis of variance (ANOVA)- exploring possible interaction between factors. Restorative Dentistry & Endodontics 2014 Feb; 39(2): 143-147.

Banerjee S, Chattopadhyay P, Ghosh A, Pathak MP, Singh S, Veer V. Sensitization, and Acute Toxicity Studies of a Transdermal Patch for Prophylaxis Against (±) Anatoxin- A Poisoning. International Journal in Toxicology 2013 Apr; 32(4): 308-313.

Kawahara K, Tojo K. Skin irritation in Transdermal drug delivery systems: a strategy for its reduction. Pharm Res 2007; 24(2): 399-408.

Vishwakarma AK, Panda P, Verma NK, Vishwakarma DK, Mishra JN. An Overview of Transdermal Patches. International Journal of Pharmacy Review & Research 2017; 7(1): 17-23.

Shinde AJ, Shinde AL, More HN. Design and evaluation of transdermal drug delivery system of gliclazide. Asian Journal of Pharmaceutics 2010 Feb; 4(2): 121-129.

Trivedi D, Goyal A. Formulation and evaluation of transdermal patches containing dexketoprofen trometamol. International Journal of Pharmaceutical Chemistry and Analysis 2020 Oct; 7(2): 87-97.

Deepika B, Juveria T, Kandukoori NR, Sarojini S, Sowmya S. Dissolution: A Predictive Tool for conventional and novel dosage forms. Journal of Pharma Research 2018 Nov; 7(6): 113-119.

Khan R, Irchhaiya R. In vitro in vivo evaluation of niosomal formulation of famotidine. International Journal of Pharmacy and Pharmaceutical Sciences. 2020 Jan 10:15-22.

Published

02-11-2021

How to Cite

SHINDE, R., & VELRAJ, M. (2021). FORMULATION, OPTIMIZATION, AND CHARACTERIZATION OF TRANSDERMAL DRUG DELIVERY SYSTEMS CONTAINING EPLERENONE. International Journal of Applied Pharmaceutics, 14(1). https://doi.org/10.22159/ijap.2022v14i1.42827

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