Chemical Permeation Enhancers for Transdermal Delivery of Thiocolchicoside: Assessment of Ex-vivo Skin Flux and In-vivo Pharmacokinetics
DOI:
https://doi.org/10.37285/ijpsn.2017.10.5.3Abstract
Present investigation comprises the study of ex-vivo skin flux and in-vivo pharmacokinetics of Thiocolchicoside (THC) from transdermal films. The films were fabricated by solvent casting technique employing combination of hydrophilic and hydrophobic polymers. A flux of 18.08 µg/cm2h and 13.37µg/cm2h was achieved for optimized formulations containing 1, 8-cineole and oleic acid respectively as permeation enhancers. The observed flux values were higher when compared to passive control (8.66 µg/cm2h). Highest skin permeation was observed when 1,8-cineole was used as chemical permeation enhancer and it considerably (2-2.5 fold) improved the THC transport across the rat skin. In vivo studies were performed in rabbits and samples were analysed by LC-MS-MS. The mean area under the curve (AUC) values of transdermal film showed about 2.35 times statistically significant (p<0.05) improvement in bioavailability when compared with the oral administration of THC solution. The developed transdermal therapeutic systems using chemical permeation enhancers were suitable for drugs like THC in effective management of muscular pain.
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Keywords:
Thiocolchicoside, 1,8-cineole, Oleic acid, Skin flux, Passive control, Bioavailability.
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Published
2017-09-30
How to Cite
1.
Rao YM, P G, M A, Kumar PP, kumar K. Chemical Permeation Enhancers for Transdermal Delivery of Thiocolchicoside: Assessment of Ex-vivo Skin Flux and In-vivo Pharmacokinetics. Scopus Indexed [Internet]. 2017 Sep. 30 [cited 2024 Nov. 19];10(5):3827-35. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/861
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Research Articles
References
Aarti N, Louk ARMP, Potts RO and Guy RH (1995). Mechanism of Oleic acid-induced skin penetration enhancement in vivo in humans. J Control Release 37: 299-306.
Artusi M, Nicoli S, Colomb P, Bettini R, Sacchi A and Santi P (2004). Effect of Chemical Enhancers and Iontophoresis on Thiocolchicoside permeation across rabbit and Human Skin In Vitro. J Pharm Sci 93(10).
Artusi M, Santi P, Colombo P and Junginger H.E (2003). Buccal delivery of thiocolchicoside: in vitro and in vivo permeation studies. Int J Pharm 250: 203-213.
Aulton ME, Abdul-Razzak MH and Hogan JE (1981). The mechanical properties of hydroxypropyl methylcellulose films derived from aqueous systems: the influence of plasticizers. Drug Dev Ind Pharm 7(6): 649-668.
Barry BW (1987). Mode of action of penetration enhancers in human skin. J Control Release 6: 85-97.
Barry BW (1988). Action of skin penetration enhancers- The Lipid Protein Partitioning theory. Int J Cosmet Sci 10: 281-293.
Bos JD and Meinardi MMHM (2000). The 500 dalton rule for skin penetration of chemical compounds and drugs. Exp Dermatol 9: 165-169.
Bouwstra JA (1997). The Skin barrier, a well –organized membrane. Colloids Surf A Physicochem Eng Asp 123-124: 403-413.
Devi VK, Saisivam S, Maria GR and Deepti PU (2003). Design and Evaluation of Matrix Diffusion Controlled Transdermal Patches of Verapamil Hydrochloride. Drug Dev Ind Pharm 29(5): 495-503.
Gannu R, Devandla A, Burra M and Madhusudan Rao Y (2011). Development of Matrix Type Transdermal Patches of Lacidipine: Evaluation of Physicochemical, in vitro, ex vivo and Mechanical Properties. Curr Trends Biotechnol Pharm 5(2): 1173-1182.
Gannu R, Palem CR, Vamshi VY, Shravan Kumar Y and Madhusudan Rao Y (2010). Enhanced bioavailability of lacidipine via micoemulsion based transdermal gels: Formulation optimization, ex vivo and in vivo characterization. Int J Pharm 388: 231-241.
Gayatri. P, Ajita M, Pavan Kumar P and Madhusudan Rao Y (2016). Development and Characterization of Nisoldipine Matrix type transdermal films; in vitro-ex vivo Evaluation. American Scientific Research Journal for Engineering, Technology and Sciences 23(1): 1-14.
Green PG, Guy RH and Hadgraft J (1988). In vitro and in vivo enhancement of skin permeation with oleic and lauric acids. Int J Pharm 48: 103-111.
Levang AK, Zhao K and Singh J (1999). Effect of ethanol/propylene glycol on the in vitro percutaneous absorption of asprin, biophysical changes and macroscopic barrier properties of the skin. Int J Pharm 181: 255-263.
Niazy EM (1991). Influence of oleic acid and other permeation promoters on transdermal delivery of dihydroergotamine through rabbit skin. Int J Pharm 67: 97-100.
Pankaj K and Samir M (2009). Enhancement of transdermal drug delivery via synergistic action of chemicals. Biochim Biophys Acta 1788: 2362-2373.
Perucca E, Poitou EP and Pifferi G (1995). Comparative pharmacokinetics and bioavailability of two oral formulations of thiocolchicoside a GABA-mimetic muscle relaxant drug in normal volunteers. Eur J Drug Metab Pharmacokinet 20(4): 301-305.
Sutherland FCW, Smith MJ, Herbst L, Els J, Hundt HKL, Swart KJ and Hundt AF (2002). Highly specific and liquid chromatography- tandem mass spectrometry method for the determination of 3-desmethylthiocolchicine in human plasma as analyte for the assessment of bioequivalence after oral administration of thiocolchicoside. J Chromatogra A 949: 71-77.
Williams AC and Barry BW (2012). Penetration Enhancers. Adv Drug Deliv Rev 56(5): 603-618.
Williams AC and Barry BW(1991). Terpenes and the Lipid-Protein-Partitioning theory of skin Penetration Enhancement. Pharm Res 8(1): 17-24.
Yamane MA, Williams AC and Barry BW (1995(a)). Effect of Terpenes and oleic acid as skin penetration enhancers towards 5-fluorouracil as assessed with time; permeation, partitioning and differential scanning calorimetry. Int J Pharm 116: 237-251.
Yamane MA, Williams AC and Barry BW (1995(b)). Terpene Penetration Enhancers in Propylene glycol/water Co-solvent systems: Effectiveness and Mechanism of Action. J Pharm Pharmacol 47: 978-989.
Artusi M, Nicoli S, Colomb P, Bettini R, Sacchi A and Santi P (2004). Effect of Chemical Enhancers and Iontophoresis on Thiocolchicoside permeation across rabbit and Human Skin In Vitro. J Pharm Sci 93(10).
Artusi M, Santi P, Colombo P and Junginger H.E (2003). Buccal delivery of thiocolchicoside: in vitro and in vivo permeation studies. Int J Pharm 250: 203-213.
Aulton ME, Abdul-Razzak MH and Hogan JE (1981). The mechanical properties of hydroxypropyl methylcellulose films derived from aqueous systems: the influence of plasticizers. Drug Dev Ind Pharm 7(6): 649-668.
Barry BW (1987). Mode of action of penetration enhancers in human skin. J Control Release 6: 85-97.
Barry BW (1988). Action of skin penetration enhancers- The Lipid Protein Partitioning theory. Int J Cosmet Sci 10: 281-293.
Bos JD and Meinardi MMHM (2000). The 500 dalton rule for skin penetration of chemical compounds and drugs. Exp Dermatol 9: 165-169.
Bouwstra JA (1997). The Skin barrier, a well –organized membrane. Colloids Surf A Physicochem Eng Asp 123-124: 403-413.
Devi VK, Saisivam S, Maria GR and Deepti PU (2003). Design and Evaluation of Matrix Diffusion Controlled Transdermal Patches of Verapamil Hydrochloride. Drug Dev Ind Pharm 29(5): 495-503.
Gannu R, Devandla A, Burra M and Madhusudan Rao Y (2011). Development of Matrix Type Transdermal Patches of Lacidipine: Evaluation of Physicochemical, in vitro, ex vivo and Mechanical Properties. Curr Trends Biotechnol Pharm 5(2): 1173-1182.
Gannu R, Palem CR, Vamshi VY, Shravan Kumar Y and Madhusudan Rao Y (2010). Enhanced bioavailability of lacidipine via micoemulsion based transdermal gels: Formulation optimization, ex vivo and in vivo characterization. Int J Pharm 388: 231-241.
Gayatri. P, Ajita M, Pavan Kumar P and Madhusudan Rao Y (2016). Development and Characterization of Nisoldipine Matrix type transdermal films; in vitro-ex vivo Evaluation. American Scientific Research Journal for Engineering, Technology and Sciences 23(1): 1-14.
Green PG, Guy RH and Hadgraft J (1988). In vitro and in vivo enhancement of skin permeation with oleic and lauric acids. Int J Pharm 48: 103-111.
Levang AK, Zhao K and Singh J (1999). Effect of ethanol/propylene glycol on the in vitro percutaneous absorption of asprin, biophysical changes and macroscopic barrier properties of the skin. Int J Pharm 181: 255-263.
Niazy EM (1991). Influence of oleic acid and other permeation promoters on transdermal delivery of dihydroergotamine through rabbit skin. Int J Pharm 67: 97-100.
Pankaj K and Samir M (2009). Enhancement of transdermal drug delivery via synergistic action of chemicals. Biochim Biophys Acta 1788: 2362-2373.
Perucca E, Poitou EP and Pifferi G (1995). Comparative pharmacokinetics and bioavailability of two oral formulations of thiocolchicoside a GABA-mimetic muscle relaxant drug in normal volunteers. Eur J Drug Metab Pharmacokinet 20(4): 301-305.
Sutherland FCW, Smith MJ, Herbst L, Els J, Hundt HKL, Swart KJ and Hundt AF (2002). Highly specific and liquid chromatography- tandem mass spectrometry method for the determination of 3-desmethylthiocolchicine in human plasma as analyte for the assessment of bioequivalence after oral administration of thiocolchicoside. J Chromatogra A 949: 71-77.
Williams AC and Barry BW (2012). Penetration Enhancers. Adv Drug Deliv Rev 56(5): 603-618.
Williams AC and Barry BW(1991). Terpenes and the Lipid-Protein-Partitioning theory of skin Penetration Enhancement. Pharm Res 8(1): 17-24.
Yamane MA, Williams AC and Barry BW (1995(a)). Effect of Terpenes and oleic acid as skin penetration enhancers towards 5-fluorouracil as assessed with time; permeation, partitioning and differential scanning calorimetry. Int J Pharm 116: 237-251.
Yamane MA, Williams AC and Barry BW (1995(b)). Terpene Penetration Enhancers in Propylene glycol/water Co-solvent systems: Effectiveness and Mechanism of Action. J Pharm Pharmacol 47: 978-989.
