Elastic liposomes mediated transdermal delivery of verapamil hydrochloride
Abstract
The aim of present investigation was to formulate and characterize elastic liposomes as a delivery system for transdermal delivery of Verapamil hydrochloride, a drug having low oral bioavailability (approx 20%), short biological half-life and extensive first pass metabolism.Verapamil hydrochloride loaded elastic vesicles were prepared by a slightly modified extrusion method using soya phosphatidylcholine and span 80(edge activator). Prepared elastic vesicles were characterized for various parameters such as vesicle shape, vesicle size and size distribution, entrapment efficiency, elasticity measurements, stability studies and in vitro skin permeation studies through excised rat skin (Sprague Dawley) using a locally fabricated Franz diffusion cell. The entrapment efficiency of elastic vesicles was found to be 59.3±3.6%. In vitro skin permeation of verapamil hydrochloride through excised rat skin (Sprague Dawley) revealed that elastic vesicles led to an enhanced transdermal flux (50.2±4.52 mg/cm2/h) of verapamil hydrochloride as compared to liposomes (11.6±2.12mg/cm2/h). Decreased lag time (0.9 h) was also observed in case of elastic liposomes. Our results indicate the feasibility of elastic liposomes for transdermal delivery of verapamil hydrochloride for improved skin permeation.
Keywords: Transdermal delivery, Elastic liposomes, Verapamil hydrochloride.
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References
1. McLafferty E, Hendry C, Alistair F, The integumentary system: anatomy, physiology and fuction of skin, Nurse stand, 2012; 19-25; 27(3):35-42.
2. Kathi C Madison, Barrier function of the skin: “La Raison d’ Etre” of the epidermis, Journal of Investigative Dermatology, 2003; 121(2):231-241.
3. Cevc G, Transfersomes, liposomes and other lipid suspensions on the skin, permeation enhancement, vesicles penetration and transdermal drug delivery, Critical Reviews in Therapeutic Drug Carrier System, 1996; 13:257-388.
4. Ho NFH, Mechanism of topical delivery of liposomally entrapped drugs, Journal of Controlled Release, 1985; 2:61-65.
5. Schreier H, Bouwstra J, Liposomes and niosomes as topical drug carriers: dermal and transdermal drug delivery, Journal of Controlled Release, 1994; 30:1-15.
6. Touitou E, Dayan N, Bergelson L, Godin B and Eliaz M, Ethosomes- novel vesicular carriers: characterization and delivery properties, Journal of Controlled Release, 2000; 65:403-418.
7. Sharma RK, Sharma N, Rana S, Shivkumar HG, Solid lipid nanoparticles as a carrier of metformin for transdermal delivery, International Journal of Drug Delivery, 2013; 5:137-145.
8. Cevc G, Glome G, Lipid vesicles penetrate into intact skin owing to the transdermal osmotic gradients and hydration force, Biochimica et Biophysica Acta, 1992; 1104:226-232.
9. Honeywell-Nguyen PI, Frederik PM, Bomans PHH, Junginger HE, Bouwstra JA, The in vitro transport of pergolide from surfactant based elastic vesicles through human skin: a suggested mechanism of action, Journal of Controlled Release, 2003; 86:145-156.
10. Fitch WP 3rd, Easterling WJ, Talbert RL, Bordovsky MJ, Mosier M, Topical verapamil HCl, topical trifluoperazine, and topical magnesium sulfate for the treatment of Peyronie's disease--a placebo-controlled pilot study, Journal of Sexual Medicine, 2007; 4(2):477-84.
11. Cavalinni G. Maretti C, Hydroelectrophoresis for transdermal administration of verapamil or of hyaluronic acid in peyronie’s disease: a prospective open label multicenter study, Journal of Medical Research and Innovation, 2018; 2(2).
12. Jain GK, Sharma AK, Agrawal SS, Transdermal controlled administration of verapamil- enhancement of skin permeability, International Journal of Pharmaceutics, 1996; 130(2):169-177.
13. Devi VK, Saisivam S, Maria GR, Deepti PU, Design and evaluation of matrix diffusion controlled transdermal patches of verapamil hydrochloride, Drug Development and Industrial Pharmacy, 2003; 29(5):495-503.
14. Gungor S, Bektas A, Alp FI, Uydes Dogan BS, Ozdemir O, Araman A, Ozsoy Y, Matrix-type transdermal patches of verapamil hydrochloride: in vitro permeation studies through excised rat skin and pharmacodynamic evaluation in rats, 2008; 13(4):283-9.
15. Sood J, Kaur V, Pawar P, Transdermal delivery of verapamil HCl: effect of penetration agent on in vitro penetration through rat skin, Journal of Applied Pharmaceutical Science, 2013; 3(03):44-51.
16. Thirupathi A, Vancha AR, Sunitha S, Preparation and evaluation of transdermal films of verapamil, International Journal of Biopharmaceutics, 2014; 5(2):83-89.
17. Kaur M, Ita KB, Popova IE, Parikh SJ, Bair DA, Microneedle assisted delivery of verapamil hydrochloride and amlodipine besylate, European Journal of Pharmaceutics and Biopharmaceutics, 2014; (86):284-291.
18. El Maghraby GM, Williams AC, Barry BW, Oestradiol skin delivery from ultradeformable liposomes: refinement of surfactant concentration, International Journal of Pharmaceutics, 2000; 196:63–74.
19. Fry DW, White JC, Goldman ID, Rapid Separation of low molecular weight solutes from liposomes without dilution, Analytical Biochemistry, 1978; 90:809-815.
20. Sorensen EN, Weisman G, Vidaver GA, A sephadex column for measuring uptake and loss of low molecular solutes from small vesicles, Analytical Biochemistry, 1977; 82:376-84.
21. Bangham D, Horn TN. Negative staining of phospholipids and their structural modification by surface-active agents as observed in the electron microscope. Journal of Molecular Biology, 1964; 8:660.
22. Jaiswal P, Kesharwani S, Kesharwani R, Patel D. Ethosome: a new technology used as topical and transdermal delivery system. Journal of Drug Delivery and Therapeutics, 2016; 6(3)7-17.
23. Jain S, Sapre R, Tiwari AK, Jain NK, Proultraflexible lipid vesiciles for effective transdermal delivery of levonorgestrel: development, characterization andperformance evaluation, AAPS PharmSciTech, 2005; 6(3):513-522.
24. Vanden Bergh BAI, Wertz PW, Junginger HE, Bouwstra JA, Elasticity of vesicles assessed by electron spin resonance, electron microscopy and extrusion measurement, International Journal of Pharmaceutics, 2001; 217:13-24.
2. Kathi C Madison, Barrier function of the skin: “La Raison d’ Etre” of the epidermis, Journal of Investigative Dermatology, 2003; 121(2):231-241.
3. Cevc G, Transfersomes, liposomes and other lipid suspensions on the skin, permeation enhancement, vesicles penetration and transdermal drug delivery, Critical Reviews in Therapeutic Drug Carrier System, 1996; 13:257-388.
4. Ho NFH, Mechanism of topical delivery of liposomally entrapped drugs, Journal of Controlled Release, 1985; 2:61-65.
5. Schreier H, Bouwstra J, Liposomes and niosomes as topical drug carriers: dermal and transdermal drug delivery, Journal of Controlled Release, 1994; 30:1-15.
6. Touitou E, Dayan N, Bergelson L, Godin B and Eliaz M, Ethosomes- novel vesicular carriers: characterization and delivery properties, Journal of Controlled Release, 2000; 65:403-418.
7. Sharma RK, Sharma N, Rana S, Shivkumar HG, Solid lipid nanoparticles as a carrier of metformin for transdermal delivery, International Journal of Drug Delivery, 2013; 5:137-145.
8. Cevc G, Glome G, Lipid vesicles penetrate into intact skin owing to the transdermal osmotic gradients and hydration force, Biochimica et Biophysica Acta, 1992; 1104:226-232.
9. Honeywell-Nguyen PI, Frederik PM, Bomans PHH, Junginger HE, Bouwstra JA, The in vitro transport of pergolide from surfactant based elastic vesicles through human skin: a suggested mechanism of action, Journal of Controlled Release, 2003; 86:145-156.
10. Fitch WP 3rd, Easterling WJ, Talbert RL, Bordovsky MJ, Mosier M, Topical verapamil HCl, topical trifluoperazine, and topical magnesium sulfate for the treatment of Peyronie's disease--a placebo-controlled pilot study, Journal of Sexual Medicine, 2007; 4(2):477-84.
11. Cavalinni G. Maretti C, Hydroelectrophoresis for transdermal administration of verapamil or of hyaluronic acid in peyronie’s disease: a prospective open label multicenter study, Journal of Medical Research and Innovation, 2018; 2(2).
12. Jain GK, Sharma AK, Agrawal SS, Transdermal controlled administration of verapamil- enhancement of skin permeability, International Journal of Pharmaceutics, 1996; 130(2):169-177.
13. Devi VK, Saisivam S, Maria GR, Deepti PU, Design and evaluation of matrix diffusion controlled transdermal patches of verapamil hydrochloride, Drug Development and Industrial Pharmacy, 2003; 29(5):495-503.
14. Gungor S, Bektas A, Alp FI, Uydes Dogan BS, Ozdemir O, Araman A, Ozsoy Y, Matrix-type transdermal patches of verapamil hydrochloride: in vitro permeation studies through excised rat skin and pharmacodynamic evaluation in rats, 2008; 13(4):283-9.
15. Sood J, Kaur V, Pawar P, Transdermal delivery of verapamil HCl: effect of penetration agent on in vitro penetration through rat skin, Journal of Applied Pharmaceutical Science, 2013; 3(03):44-51.
16. Thirupathi A, Vancha AR, Sunitha S, Preparation and evaluation of transdermal films of verapamil, International Journal of Biopharmaceutics, 2014; 5(2):83-89.
17. Kaur M, Ita KB, Popova IE, Parikh SJ, Bair DA, Microneedle assisted delivery of verapamil hydrochloride and amlodipine besylate, European Journal of Pharmaceutics and Biopharmaceutics, 2014; (86):284-291.
18. El Maghraby GM, Williams AC, Barry BW, Oestradiol skin delivery from ultradeformable liposomes: refinement of surfactant concentration, International Journal of Pharmaceutics, 2000; 196:63–74.
19. Fry DW, White JC, Goldman ID, Rapid Separation of low molecular weight solutes from liposomes without dilution, Analytical Biochemistry, 1978; 90:809-815.
20. Sorensen EN, Weisman G, Vidaver GA, A sephadex column for measuring uptake and loss of low molecular solutes from small vesicles, Analytical Biochemistry, 1977; 82:376-84.
21. Bangham D, Horn TN. Negative staining of phospholipids and their structural modification by surface-active agents as observed in the electron microscope. Journal of Molecular Biology, 1964; 8:660.
22. Jaiswal P, Kesharwani S, Kesharwani R, Patel D. Ethosome: a new technology used as topical and transdermal delivery system. Journal of Drug Delivery and Therapeutics, 2016; 6(3)7-17.
23. Jain S, Sapre R, Tiwari AK, Jain NK, Proultraflexible lipid vesiciles for effective transdermal delivery of levonorgestrel: development, characterization andperformance evaluation, AAPS PharmSciTech, 2005; 6(3):513-522.
24. Vanden Bergh BAI, Wertz PW, Junginger HE, Bouwstra JA, Elasticity of vesicles assessed by electron spin resonance, electron microscopy and extrusion measurement, International Journal of Pharmaceutics, 2001; 217:13-24.
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JAIN N, Argal A, Gautam G. Elastic liposomes mediated transdermal delivery of verapamil hydrochloride. JDDT [Internet]. 15Nov.2018 [cited 2Mar.2021];8(6):16-1. Available from: http://jddtonline.info/index.php/jddt/article/view/2073
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