Research Article
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Year 2020, Volume: 24 Issue: 4 , 562 - 571 , 27.06.2025
https://doi.org/10.35333/jrp.2020.204
https://izlik.org/JA73CS52DH

Abstract

References

  • [1] Pastore M , Kalia Y, Horstmann M , Roberts M. Transdermal patches : history, development and pharmacology. Br J Pharmacol. 2015; 172(9): 2179–2209. [CrossRef]
  • [2] Al Hanbali O, Khan H, Sarfra M, Arafat M, Ijaz S, Hameed A.Transdermal patches: design and current approaches to painless drug delivery. Acta Pharma. 2019; 69(2): 197–215. [CrossRef]
  • [3] Schechter M. Chemical, pharmacokinetic and pharmacodynamic properties of statins: an update. Fundam Clin Pharmacol. 2005; 19: 117-125. [CrossRef]
  • [4] Puri A, Bhattaccharjee S, Zhang W, Clark M, Singh O, Doncel G, Banga A. Development of a transdermal delivery system for tenofovir alafenamide, a prodrug of tenofovir with potent antiviral activity against HIV and HBV. Pharmaceutics. 2019; 11(173): 1-29. [CrossRef]
  • [5] Regenthal R, Voskanian M, Baumann F ,Teichert J, Brätter C, Aigner A, Abraham G. Pharmacokinetic evaluation of a transdermal anastrozole-in-adhesive formulation. Drug Des Devel Ther. 2018; 12: 3653-3664. [CrossRef]
  • [6] Siafaka P, Barmpalexis P,Lazaridou M ,Papageorgiou G, Koutris E, Karavas E, Kostoglou M, Bikiaris D.Controlled release formulations of risperidone antipsychotic drug in novel aliphatic polyester carriers:data analysis and modelling. Eur J Pharm Biopharm. 2015; 94: 473-484. [CrossRef]
  • [7] Parhi R, Padilam S .In vitro permeation and stability studies on developed drug-in-adhesive transdermal patch of simvastatin. Bulletin of Faculty of Pharmacy, Cairo University. 2018; 56(1): 26-33. [CrossRef]
  • [8] Okur N, Filippousi A, Okur M, Ayla S, Caglar E, Yoltas A, Siafaka P. A novel approach for skin infections: controlled release topical mats of poly(lactic acid)/polyethylene succinate blend containiny voriconazole. J Drug Deliv Sci Technol. 2018; 46: 74-86. [CrossRef]
  • [9] Okur N, Hökenek N, Okur M, Ayla S, Yoltaş A, Siafaka P, Cevher E. An alternative approach to wound healing field; new composite films from natural polymers for mupirocin dermal delivery. Saudi Pharm J. 2019; 27(5): 738-752. [CrossRef]
  • [10] Jafri I, Shoaib M, Yousuf R, Ali F. Effect of permeation enhancers on in vitro release and transdermal delivery of lamotrigine from Eudragit®RS100 polymer matrix-type drug in adhesive patches. Prog Biomater. 2019; 8(2): 91-100. [CrossRef]
  • [11] Hsieh L, Box K, Taylor S. Assessing the Impact of polymers on the pH-induced precipitation behaviour of poorly water soluble compounds using synchrotron wide angle X-ray scattering. J Pharm Sci. 2014; 103: 2724–2735. [CrossRef]
  • [12] Suys J, Chalmers D, Pouton C, Porte C.Polymeric precipitation inhibitors promote fenofibrate supersaturation and enhance drug absorption from a type IV lipid based formulation. Mol Pharm. 2018; 15(6): 2355-2371. [CrossRef]
  • [13] Hadgraft H, Lane M . Drug crystallization – implications for topical and transdermal delivery. Expert Opin Drug Deliv. 2016; 13(6): 817-830. [CrossRef]
  • [14] Weng W, Quan P, Liu C, Zhao H, Fang L. Design of a drug-in-adhesive transdermal patch for risperidone: effect of drug-additive interactions on the crystallization inhibition and in vitro/in vivo correlation study. J Pharm Sci. 2016; 105(10): 3153-3161. [CrossRef]
  • [15] Jain P, Banga AK .Inhibition of crystallization in drug-in-adhesive-type transdermal patches. Int J Pharm. 2010 ; 394 (1-2): 68-74. [CrossRef]
  • [16] Zhao C, Quan P, Liu C, Li Q, Fang L.Effect of isopropyl myristate on the viscoelasticity and drug release of a drugin-adhesive transdermal patch containing blonanserin. Acta Pharm Sin B. 2016; 6(6): 623–628. [CrossRef]
  • [17] Schurr P , Schultz J , Parkinson T . Triton-induced hyperlipidemia in rats as an animal model for screening hypolipidemic drugs. Lipids. 1972; 7(1): 68-74. [CrossRef]
  • [18] Otway S, D. S. Robinson. The use of a non‐ ionic detergent (triton WR 1339) to determine rates of triglyceride entry into the circulation of the rat under different physiological conditions.J Physiol. 1967; 190(2): 321-332. [CrossRef]
  • [19] Li J, Yang M, Xu W. Enhanced oral bioavailability of fluvastatin by using nanosuspensions containing cyclodextrin. Drug Des Devel Ther. 2018; 12: 3491-3499. [CrossRef]
  • [20] Sharma P, Panda A, Pradhan A, Zhang J, Thakkar R, Whang C, Repka M, Murthy S. Solid-state stability issues of drugs in transdermal patch formulations. AAPS PharmSciTech. 2017; 19(1): 27-35. [CrossRef]
  • [21] Geevarghese R, Shirolkar S. RP-HPLC method for estimation of rosuvastatin calcium from bulk and transdermal dosage form. Int J Pharm Sci Res. 2018; 9(11): 4875-4879. [CrossRef]
  • [22] Lal N, Yadav P ,Rastogi V, Verma A, Verma N . Aspects of pressure sensitive adhesives in fabricating drug-in adhesive transdermal therapeutic systems. Drug Deliv Lett. 2017; 7(1): 3-15. [CrossRef]
  • [23] Niharika L, Pragya Y, Vaibhav V, Lalit P, Navneet V, AnuragV. Development and evaluation of transdermal therapeutic system of metoprolol succinate using acrylic polymer. Asian J Pharm. 2016; 10(3): 178-187.
  • [24] Mendes M, Nunes S, Sousa J, Pais A, Vitorino C. Expanding transdermal delivery with lipid nanoparticles: a new drug-in-NLC-in-adhesive design. Mol Pharm. 2017; 14(6): 2099-2115. [CrossRef]
  • [25] Anod H, Gupta V, Gowda D, Manohar M. Preparation and evaluation of simvastatin transdermal film. Int. J. Appl. Pharm. 2018; 10(5): 235-238. [CrossRef]
  • [26] Taghizadeh S, Ardakani A, Mohamadnia F. Statistical experimental design approach to evaluate the influence of various penetration enhancers on transdermal drug delivery of buprenorphine. J Adv Res. 2015; 6: 155–162. [CrossRef]
  • [27] Wang J, Li Z, Sun F, Tang S, Zhang S, Pengyyue L.Evaluation of dermal irritation and skin sensitization due to vitacoxib. Toxicol Rep . 2017; 4: 287–290. [CrossRef]
  • [28] Bautista A, Tan M, Apostol J. Lipid-lowering property of Clausena anisum-olens in hypercholesterolemic rats. Pharm Biol. 2017; 55(1): 833-836. [CrossRef]
  • [29] Surya S, Kurup R, Kumar A, Carla B, Sunil C. Antihyperlipidemic effect of Ficus dalhousiae miq. stem bark on Triton WR-1339 and high fat diet induced hyperlipidemic rats. Bulletin of Faculty of Pharmacy, Cairo University. 2017; 55(1): 73-77. [CrossRef]
  • [30] Murugaiyah V, Ahmed Saeed M, Kuong Y, Murugesu K, Parasuraman S, Asmawi M, Sadikun A. Lipid lowering effect of hydroalcoholic extracts of Gynura procumbens in chemical and high fat diet induced hyperlipidemic rats. Phcog Mag. 2018; 14(55): 184-191. [CrossRef]

Formulation and evaluation of fluvastatin sodium drugin-adhesive transdermal system

Year 2020, Volume: 24 Issue: 4 , 562 - 571 , 27.06.2025
https://doi.org/10.35333/jrp.2020.204
https://izlik.org/JA73CS52DH

Abstract

Current investigation is aimed at designing a fluvastatin sodium loaded drug-in-adhesive patch (DIA Patch ) to overcome the problems associated with the daily oral administration of the drug. The patches were prepared by solvent casting method using acrylate emulsion polymers like covinax 525-78, mowinyl 461 and novacryl PSR32 which served as sustained release matrix polymer and adhesive. Methocel K-15M was added as a solubilizer whereas transcutol, oleic acid and isopropyl myristate were tried as permeation enhancers for the drug-in-adhesive patch. The combination of mowinyl-isopropyl myristate patch was further optimized by 32 factorial design to study the effect of two independent variables i.e. concentration of solubilizer and permeation enhancer on responses i.e.% drug release, tensile strength and peel adhesion strength. The formulation was further evaluated for its lipid lowering activity and skin irritation index. The % cumulative release of drug at the end of 24 h was found to be 87.74%. The formulation shows tensile strength of 12.75 kg/cm2 and peel adhesion strength of 32.44 N/25 mm. The Primary irritation index (PII) for DIA patch was found to be 0.22. The fluvastatin sodium loaded DIA patch significantly inhibits serum cholesterol and triglyceride levels as compared to oral control (p<0.01) in triton WR 1339 induced hyperlipidemic rat. Hence the developed transdermal patch could be acceptable for transdermal use.

References

  • [1] Pastore M , Kalia Y, Horstmann M , Roberts M. Transdermal patches : history, development and pharmacology. Br J Pharmacol. 2015; 172(9): 2179–2209. [CrossRef]
  • [2] Al Hanbali O, Khan H, Sarfra M, Arafat M, Ijaz S, Hameed A.Transdermal patches: design and current approaches to painless drug delivery. Acta Pharma. 2019; 69(2): 197–215. [CrossRef]
  • [3] Schechter M. Chemical, pharmacokinetic and pharmacodynamic properties of statins: an update. Fundam Clin Pharmacol. 2005; 19: 117-125. [CrossRef]
  • [4] Puri A, Bhattaccharjee S, Zhang W, Clark M, Singh O, Doncel G, Banga A. Development of a transdermal delivery system for tenofovir alafenamide, a prodrug of tenofovir with potent antiviral activity against HIV and HBV. Pharmaceutics. 2019; 11(173): 1-29. [CrossRef]
  • [5] Regenthal R, Voskanian M, Baumann F ,Teichert J, Brätter C, Aigner A, Abraham G. Pharmacokinetic evaluation of a transdermal anastrozole-in-adhesive formulation. Drug Des Devel Ther. 2018; 12: 3653-3664. [CrossRef]
  • [6] Siafaka P, Barmpalexis P,Lazaridou M ,Papageorgiou G, Koutris E, Karavas E, Kostoglou M, Bikiaris D.Controlled release formulations of risperidone antipsychotic drug in novel aliphatic polyester carriers:data analysis and modelling. Eur J Pharm Biopharm. 2015; 94: 473-484. [CrossRef]
  • [7] Parhi R, Padilam S .In vitro permeation and stability studies on developed drug-in-adhesive transdermal patch of simvastatin. Bulletin of Faculty of Pharmacy, Cairo University. 2018; 56(1): 26-33. [CrossRef]
  • [8] Okur N, Filippousi A, Okur M, Ayla S, Caglar E, Yoltas A, Siafaka P. A novel approach for skin infections: controlled release topical mats of poly(lactic acid)/polyethylene succinate blend containiny voriconazole. J Drug Deliv Sci Technol. 2018; 46: 74-86. [CrossRef]
  • [9] Okur N, Hökenek N, Okur M, Ayla S, Yoltaş A, Siafaka P, Cevher E. An alternative approach to wound healing field; new composite films from natural polymers for mupirocin dermal delivery. Saudi Pharm J. 2019; 27(5): 738-752. [CrossRef]
  • [10] Jafri I, Shoaib M, Yousuf R, Ali F. Effect of permeation enhancers on in vitro release and transdermal delivery of lamotrigine from Eudragit®RS100 polymer matrix-type drug in adhesive patches. Prog Biomater. 2019; 8(2): 91-100. [CrossRef]
  • [11] Hsieh L, Box K, Taylor S. Assessing the Impact of polymers on the pH-induced precipitation behaviour of poorly water soluble compounds using synchrotron wide angle X-ray scattering. J Pharm Sci. 2014; 103: 2724–2735. [CrossRef]
  • [12] Suys J, Chalmers D, Pouton C, Porte C.Polymeric precipitation inhibitors promote fenofibrate supersaturation and enhance drug absorption from a type IV lipid based formulation. Mol Pharm. 2018; 15(6): 2355-2371. [CrossRef]
  • [13] Hadgraft H, Lane M . Drug crystallization – implications for topical and transdermal delivery. Expert Opin Drug Deliv. 2016; 13(6): 817-830. [CrossRef]
  • [14] Weng W, Quan P, Liu C, Zhao H, Fang L. Design of a drug-in-adhesive transdermal patch for risperidone: effect of drug-additive interactions on the crystallization inhibition and in vitro/in vivo correlation study. J Pharm Sci. 2016; 105(10): 3153-3161. [CrossRef]
  • [15] Jain P, Banga AK .Inhibition of crystallization in drug-in-adhesive-type transdermal patches. Int J Pharm. 2010 ; 394 (1-2): 68-74. [CrossRef]
  • [16] Zhao C, Quan P, Liu C, Li Q, Fang L.Effect of isopropyl myristate on the viscoelasticity and drug release of a drugin-adhesive transdermal patch containing blonanserin. Acta Pharm Sin B. 2016; 6(6): 623–628. [CrossRef]
  • [17] Schurr P , Schultz J , Parkinson T . Triton-induced hyperlipidemia in rats as an animal model for screening hypolipidemic drugs. Lipids. 1972; 7(1): 68-74. [CrossRef]
  • [18] Otway S, D. S. Robinson. The use of a non‐ ionic detergent (triton WR 1339) to determine rates of triglyceride entry into the circulation of the rat under different physiological conditions.J Physiol. 1967; 190(2): 321-332. [CrossRef]
  • [19] Li J, Yang M, Xu W. Enhanced oral bioavailability of fluvastatin by using nanosuspensions containing cyclodextrin. Drug Des Devel Ther. 2018; 12: 3491-3499. [CrossRef]
  • [20] Sharma P, Panda A, Pradhan A, Zhang J, Thakkar R, Whang C, Repka M, Murthy S. Solid-state stability issues of drugs in transdermal patch formulations. AAPS PharmSciTech. 2017; 19(1): 27-35. [CrossRef]
  • [21] Geevarghese R, Shirolkar S. RP-HPLC method for estimation of rosuvastatin calcium from bulk and transdermal dosage form. Int J Pharm Sci Res. 2018; 9(11): 4875-4879. [CrossRef]
  • [22] Lal N, Yadav P ,Rastogi V, Verma A, Verma N . Aspects of pressure sensitive adhesives in fabricating drug-in adhesive transdermal therapeutic systems. Drug Deliv Lett. 2017; 7(1): 3-15. [CrossRef]
  • [23] Niharika L, Pragya Y, Vaibhav V, Lalit P, Navneet V, AnuragV. Development and evaluation of transdermal therapeutic system of metoprolol succinate using acrylic polymer. Asian J Pharm. 2016; 10(3): 178-187.
  • [24] Mendes M, Nunes S, Sousa J, Pais A, Vitorino C. Expanding transdermal delivery with lipid nanoparticles: a new drug-in-NLC-in-adhesive design. Mol Pharm. 2017; 14(6): 2099-2115. [CrossRef]
  • [25] Anod H, Gupta V, Gowda D, Manohar M. Preparation and evaluation of simvastatin transdermal film. Int. J. Appl. Pharm. 2018; 10(5): 235-238. [CrossRef]
  • [26] Taghizadeh S, Ardakani A, Mohamadnia F. Statistical experimental design approach to evaluate the influence of various penetration enhancers on transdermal drug delivery of buprenorphine. J Adv Res. 2015; 6: 155–162. [CrossRef]
  • [27] Wang J, Li Z, Sun F, Tang S, Zhang S, Pengyyue L.Evaluation of dermal irritation and skin sensitization due to vitacoxib. Toxicol Rep . 2017; 4: 287–290. [CrossRef]
  • [28] Bautista A, Tan M, Apostol J. Lipid-lowering property of Clausena anisum-olens in hypercholesterolemic rats. Pharm Biol. 2017; 55(1): 833-836. [CrossRef]
  • [29] Surya S, Kurup R, Kumar A, Carla B, Sunil C. Antihyperlipidemic effect of Ficus dalhousiae miq. stem bark on Triton WR-1339 and high fat diet induced hyperlipidemic rats. Bulletin of Faculty of Pharmacy, Cairo University. 2017; 55(1): 73-77. [CrossRef]
  • [30] Murugaiyah V, Ahmed Saeed M, Kuong Y, Murugesu K, Parasuraman S, Asmawi M, Sadikun A. Lipid lowering effect of hydroalcoholic extracts of Gynura procumbens in chemical and high fat diet induced hyperlipidemic rats. Phcog Mag. 2018; 14(55): 184-191. [CrossRef]
There are 30 citations in total.

Details

Primary Language English
Subjects Pharmacology and Pharmaceutical Sciences (Other)
Journal Section Research Article
Authors

Rachel Geevarghese This is me

Satish Shirolkar This is me

Publication Date June 27, 2025
DOI https://doi.org/10.35333/jrp.2020.204
IZ https://izlik.org/JA73CS52DH
Published in Issue Year 2020 Volume: 24 Issue: 4

Cite

APA Geevarghese, R., & Shirolkar, S. (2025). Formulation and evaluation of fluvastatin sodium drugin-adhesive transdermal system. Journal of Research in Pharmacy, 24(4), 562-571. https://doi.org/10.35333/jrp.2020.204
AMA 1.Geevarghese R, Shirolkar S. Formulation and evaluation of fluvastatin sodium drugin-adhesive transdermal system. J. Res. Pharm. 2025;24(4):562-571. doi:10.35333/jrp.2020.204
Chicago Geevarghese, Rachel, and Satish Shirolkar. 2025. “Formulation and Evaluation of Fluvastatin Sodium Drugin-Adhesive Transdermal System”. Journal of Research in Pharmacy 24 (4): 562-71. https://doi.org/10.35333/jrp.2020.204.
EndNote Geevarghese R, Shirolkar S (June 1, 2025) Formulation and evaluation of fluvastatin sodium drugin-adhesive transdermal system. Journal of Research in Pharmacy 24 4 562–571.
IEEE [1]R. Geevarghese and S. Shirolkar, “Formulation and evaluation of fluvastatin sodium drugin-adhesive transdermal system”, J. Res. Pharm., vol. 24, no. 4, pp. 562–571, June 2025, doi: 10.35333/jrp.2020.204.
ISNAD Geevarghese, Rachel - Shirolkar, Satish. “Formulation and Evaluation of Fluvastatin Sodium Drugin-Adhesive Transdermal System”. Journal of Research in Pharmacy 24/4 (June 1, 2025): 562-571. https://doi.org/10.35333/jrp.2020.204.
JAMA 1.Geevarghese R, Shirolkar S. Formulation and evaluation of fluvastatin sodium drugin-adhesive transdermal system. J. Res. Pharm. 2025;24:562–571.
MLA Geevarghese, Rachel, and Satish Shirolkar. “Formulation and Evaluation of Fluvastatin Sodium Drugin-Adhesive Transdermal System”. Journal of Research in Pharmacy, vol. 24, no. 4, June 2025, pp. 562-71, doi:10.35333/jrp.2020.204.
Vancouver 1.Rachel Geevarghese, Satish Shirolkar. Formulation and evaluation of fluvastatin sodium drugin-adhesive transdermal system. J. Res. Pharm. 2025 Jun. 1;24(4):562-71. doi:10.35333/jrp.2020.204