Ethosome: a novel vesicular carrier for transdermal drug delivery
Abstract
Delivery across skin is striking due to its easy convenience. However, drug delivery across skin is still a confront in biomedical sciences. Over the past few decades, various successful narrative devices and techniques have emerged to optimize drug delivery across skin whose barricading behaviour constricts entry of most of the therapeutic agents. Ethosomes are non-invasive delivery transporter that enables drugs to reach the deep skin layers and/or the systemic circulation. Although ethosomal systems are theoretically sophisticated, they are characterized by simplicity in their preparation, efficacy and safety. A combination that can highly inflate their application. Ethosomes are soft, malleable vesicles adapted for enhanced delivery of active agents. This article reviews work carried out method of preparation, application and characterization of ethosomal systems. Because of their exceptional structure, ethosomes are able to encapsulate and deliver through the skin highly lipophilic molecules such as testosterone, cannabinoids and minoxidil as well as cationic drugs such as trihexyphenidil and propranolol. Results obtained in a double-blind two-armed randomized clinical study showed that treatment with the ethosomal acyclovir formulation appreciably improved all the evaluated parameters. In further work, the ethosomal expertise was broadened to introduce agents into cultured cells and microorganisms. Enhanced delivery of bioactive molecules through the skin and cellular membranes by means of an ethosomal transporter opens numerous confronts and prospects for the research and future development of novel improved therapies.
Keywords: Ethosomes, Skin layers, Characterization
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References
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2. Barry WB. Dermatological Formulations: Percutaneous Absorption. New York, Basel: Marcel Dekker, 1983.
3. Flynn GL. Cutaneous and transdermal delivery: processes and systems of delivery. In: Banker GS, Rhodes CT, editors. Modern Pharmaceutics. New York: Marcel Dekker, 1995.
4. Smith EW, Maibach HI. Percutaneous Penetration Enhancers. New York: CRS Press, 1995.
5. Elias PM. Epidermal lipids, barrier function and desquamation. J Invest Dermatol 1983; 80:44-9.
6. Pirot F, Kalia YN, Stinchcomb AL, et al. Characterization of the permeability barrier of human skin in vivo. Proc Natl Acad Sci USA 1997; 94:1562–7.
7. Barry B. Transdermal drug delivery. In: Aulton EM, eds. Pharmaceutics: the science of dosage form design. London: Churchill Livingstone, 2002; 499–528.
8. Barry B. Breaching the skin’s barrier to drugs. Nat Biotechnol 2004; 22:165–7.
9. Honeywell NPL, Bouwstra JA. Vesicles as a tool for transdermal and dermal delivery. Drug Discov Today Technol 2005; 2:67–74.
10. Touitou, E., Godin, B and Weiss, C., Enhanced Delivery of Drug Into and Across The Skin By Ethosomal Carrier, Drug Develop. Res. 2000; 50:406-415.
11. Paolino D, Lucania G, Mardente D, Alhaique F, Fresta M. Ethosome For Skin Delivery of Ammonium Glycyrrhizinate: In Vitro Percutaneous Permeation Through Human Skin And In Vivo Anti Inflammatory Activity on Human Volunteers, J. Cont. Rel, 2005; 106:99- 110.
12. Jun-Bo T , Zhuang-Qun Y, Xi-Jing H, Ying X, Yong S, Zhe X, Tao C. Effect Of Ethosomal Minoxidil on Dermal Delivery, J Dermatol Sci, 2007; 45:135-137.
13. Pandey V, Golhani D, Shukla R. Ethosomes: versatile vesicular carriers for efficient transdermal delivery of therapeutic agents. Drug Delivery, DOI: 10.3109/10717544.2014.889777.
14. Flynn G H. at el. Transdermal delivery of narcotic analgesics, Comparative permeabilities of narcotic analgesics through human cadaver skin, Pharm Res, 1989; 6:825-832.
15. Wertz P W, Downing D T; In Transdermal Drug Delivery, Development Issues and Research Initiatives, Hadgraft, J J, Guy R H. Eds. Marcel Dekker Inc, New York. 1989; 35:1-22.
16. Nandure HP, Puranik P, Giram P, LoneV. Ethosome: A Novel Drug Carrier. International Journal of Pharmaceutical Research & Allied Sciences 2013; 2(3);18-30.
17. Elsayed Mustafa MA et al. Deformable liposomes and ethosomes: mechanism of enhanced skin delivery. Int J pharm 2006; 322:60-66.
18. Maestrelli F, Capasso G, Gonzalez-Rodriguez ML, Rabasco AM, Ghelardini C, Mura P. Effect of preparation technique on the properties and in vivo efficacy of benzocaine-loaded ethosomes. J Liposome Res. 2009; 19(4):253260.
19. Rani S, David N, Pin CF. Formulation and invitro evaluation of ethosomeas vesicular carrier for enhanced topical delivery of isotretinoin, International Journal of Drug Delivery, 2013; 5:28-34.
20. Song CK, Balakrishnan P, Shim CK, Chung SJ, Chong S, Kim DD. A novel vesicular carrier, transethosome, for enhanced skin delivery of voriconazole: characterization and in vitro/in vivo evaluation. Colloids Surf B Biointerfaces. 2012; 92:299–304.
21. Zhang JP, Wei YH, Zhou Y, Li YQ, Wu XA. Ethosomes, binary ethosomes and transfersomes of terbinafine hydrochloride: a comparative study. Arch Pharm Res. 2012; 35(1):109–117.
22. Dave V, Kumar D, Lewis S, Paliwal S. Ethosome for enhanced transdermal drug delivery of aceclofenac. Int J Drug Deliv. 2010; 2(1):81–92.
23. Gangwar S, Singh S, Garg G. Ethosomes: A Novel Tool for Drug Delivery Through the Skin, Journal of Pharmacy Research 2010; 3(4):688-691.
24. Jain H, Patel J, Joshi K, Patel P, Upadhyay UM. Ethosomes: A Novel Drug Carrier, International Journal of Clinical Practice 2011; 7:1:1-4.
25. Upadhyay N, Mandal S, Bhatia L, Shailesh S, Chauhan P. A Review on Ethosomes: An Emerging Approach for Drug Delivery through the Skin, Recent Research in Science and Technology 2011; 3(7):19-24.
26. Sivakranth M, AnjumaAra P, Krishnaveni C, Venkatesh E. Ethosomes: A Novel Vesicular Drug Delivery System, International Journal of Advances in Pharmaceutical Research 2012; 2(1):16-27.
27. Kumar R, Aslam MD, Tripathi A, Prasad D, Chaudhary V, Jain V, Mishra SK, Singh R. Ethosomes: Novel Vesicular Carriers in Transdermal Drug Delivery, Journal of Global Pharma Technology 2010; 2(6):1-7.
28. Rathore AR, Khambete H, Jain S. Preparation and Characterization of Repaglinide Loaded Ethosomal Gel for the Treatment of NIDDM, International Journal of Pharmaceutical and Biological Archives 2013; 4(2):385-390.
29. Shahwal V, Samnani A, Dubey B, Bhowmick M. Ethosomes: An Overview, International Journal of Biomedical and Advance Research 2011; 2:161-168.
30. Kumar R, Aslam M.D, Tripathi A, Prasad D, Chaudhary V, Jain V, Mishra S K, Singh R. Ethosomes novel vesicular carriers in transdermal drug delivery. J Global Pharma Tech 2010; 2(6):1-7.
31. Heeremans JLM, Gerristen HR, Meusen SP, Mijnheer FW, Gangaram RS, Panday G, Prevost R, Kluft C, Crommelin DJA. The preparation of Tissue Type Plasminogen Activator (T- PA) containing liposomes: Entrapment Efficacy and Ultracentrifugation Damage, Journal of Drug Targeting 1995; 3:301.
32. Jain S, Umamaheshwari RB, Bhadra D, Jain NK. Ethosomes: A Novel Vesicular Carrier for Enhanced Transdermal Delivery of a Anti-HIV Agent, Indian Journal of Pharmaceutical Sciences 2004; 66:72-81.
33. Verma DD, Fahr A, Synergistic Penetration Effect of Ethanol and Phospholipids on the Topical Delivery of Cyclosporin, Journal of Controlled Release 2010; 97:55-66.
34. Touitou E. Composition of Applying Active Substance to or Through the Skin, US patent: 5, 540, 934, 1998.
35. Touitou E, Composition of Applying Active Substance to or Through The Skin, US patent: 5, 716, 638, 1996.
36. Tyagi LK, Kumar S, Maurya SS, Kori ML. Ethosomes novel vesicular carier for enhanced transdermal drug delivery system. Bulletin Pharm Res 2013; 3(1):6-13.
37. Dhurve R, Kashyap N, Mishra A, Pathak AK. A Holistic Review on Ethosome: A Promising Drug Delivery System for Topical Fungal Disease International Journal of Pharmaceutical & Biological Archives 2014; 5(5):13-26
38. Ghule AR, Shinkar DM, Saudagar RB. Ethosomes: Carrier for Enhanced Transdermal Drug Delivery System, J. Adv. Pharm. Edu. & Res. 2014; 4(4):380-387
39. Sudhakar K, Nitish U, Sanjay J R, Narayana C. Ethosomes as non-invasive Loom for transdermal drug delivery. Apple Academic Press Publication. 2012.
40. Maurya SD, Prajapati SK, Gupta AK Saxena GK, Dhakar RC, Formulation Development and Evaluation of Ethosome of Stavudine, Indian J.Pharm. Educ. Res. 2010; 44(1):102-108
41. Gangwar S, Ethosomes: For Drug Delivery, Journal of Pharmacy Research 2010; 3(4):688-691.
42. Kumar KP, Radhika PR, Sivakumar T. Ethosomes: A Priority in Transdermal Drug Delivery, International Journal of Advances in Pharmaceutical Sciences 2010; 1:111-121.
43. Touitou E at al., Composition of Applying Active Substance To or Through The Skin, US Patent: 5716638, 1996.
44. Touitou E at al., Composition of Applying Active Substance To or Through the Skin. US Patent: 5540934, 1998.
45. Mohanty D, Babu MN, Ankitha K, Gunde S, Bakshi V, Jat RM. Ethosome: a recent optimized technology for transdermal drug penetration, European Journal of Biomedical AND Pharmaceutical sciences 2016; 3(12):232-240.
2. Barry WB. Dermatological Formulations: Percutaneous Absorption. New York, Basel: Marcel Dekker, 1983.
3. Flynn GL. Cutaneous and transdermal delivery: processes and systems of delivery. In: Banker GS, Rhodes CT, editors. Modern Pharmaceutics. New York: Marcel Dekker, 1995.
4. Smith EW, Maibach HI. Percutaneous Penetration Enhancers. New York: CRS Press, 1995.
5. Elias PM. Epidermal lipids, barrier function and desquamation. J Invest Dermatol 1983; 80:44-9.
6. Pirot F, Kalia YN, Stinchcomb AL, et al. Characterization of the permeability barrier of human skin in vivo. Proc Natl Acad Sci USA 1997; 94:1562–7.
7. Barry B. Transdermal drug delivery. In: Aulton EM, eds. Pharmaceutics: the science of dosage form design. London: Churchill Livingstone, 2002; 499–528.
8. Barry B. Breaching the skin’s barrier to drugs. Nat Biotechnol 2004; 22:165–7.
9. Honeywell NPL, Bouwstra JA. Vesicles as a tool for transdermal and dermal delivery. Drug Discov Today Technol 2005; 2:67–74.
10. Touitou, E., Godin, B and Weiss, C., Enhanced Delivery of Drug Into and Across The Skin By Ethosomal Carrier, Drug Develop. Res. 2000; 50:406-415.
11. Paolino D, Lucania G, Mardente D, Alhaique F, Fresta M. Ethosome For Skin Delivery of Ammonium Glycyrrhizinate: In Vitro Percutaneous Permeation Through Human Skin And In Vivo Anti Inflammatory Activity on Human Volunteers, J. Cont. Rel, 2005; 106:99- 110.
12. Jun-Bo T , Zhuang-Qun Y, Xi-Jing H, Ying X, Yong S, Zhe X, Tao C. Effect Of Ethosomal Minoxidil on Dermal Delivery, J Dermatol Sci, 2007; 45:135-137.
13. Pandey V, Golhani D, Shukla R. Ethosomes: versatile vesicular carriers for efficient transdermal delivery of therapeutic agents. Drug Delivery, DOI: 10.3109/10717544.2014.889777.
14. Flynn G H. at el. Transdermal delivery of narcotic analgesics, Comparative permeabilities of narcotic analgesics through human cadaver skin, Pharm Res, 1989; 6:825-832.
15. Wertz P W, Downing D T; In Transdermal Drug Delivery, Development Issues and Research Initiatives, Hadgraft, J J, Guy R H. Eds. Marcel Dekker Inc, New York. 1989; 35:1-22.
16. Nandure HP, Puranik P, Giram P, LoneV. Ethosome: A Novel Drug Carrier. International Journal of Pharmaceutical Research & Allied Sciences 2013; 2(3);18-30.
17. Elsayed Mustafa MA et al. Deformable liposomes and ethosomes: mechanism of enhanced skin delivery. Int J pharm 2006; 322:60-66.
18. Maestrelli F, Capasso G, Gonzalez-Rodriguez ML, Rabasco AM, Ghelardini C, Mura P. Effect of preparation technique on the properties and in vivo efficacy of benzocaine-loaded ethosomes. J Liposome Res. 2009; 19(4):253260.
19. Rani S, David N, Pin CF. Formulation and invitro evaluation of ethosomeas vesicular carrier for enhanced topical delivery of isotretinoin, International Journal of Drug Delivery, 2013; 5:28-34.
20. Song CK, Balakrishnan P, Shim CK, Chung SJ, Chong S, Kim DD. A novel vesicular carrier, transethosome, for enhanced skin delivery of voriconazole: characterization and in vitro/in vivo evaluation. Colloids Surf B Biointerfaces. 2012; 92:299–304.
21. Zhang JP, Wei YH, Zhou Y, Li YQ, Wu XA. Ethosomes, binary ethosomes and transfersomes of terbinafine hydrochloride: a comparative study. Arch Pharm Res. 2012; 35(1):109–117.
22. Dave V, Kumar D, Lewis S, Paliwal S. Ethosome for enhanced transdermal drug delivery of aceclofenac. Int J Drug Deliv. 2010; 2(1):81–92.
23. Gangwar S, Singh S, Garg G. Ethosomes: A Novel Tool for Drug Delivery Through the Skin, Journal of Pharmacy Research 2010; 3(4):688-691.
24. Jain H, Patel J, Joshi K, Patel P, Upadhyay UM. Ethosomes: A Novel Drug Carrier, International Journal of Clinical Practice 2011; 7:1:1-4.
25. Upadhyay N, Mandal S, Bhatia L, Shailesh S, Chauhan P. A Review on Ethosomes: An Emerging Approach for Drug Delivery through the Skin, Recent Research in Science and Technology 2011; 3(7):19-24.
26. Sivakranth M, AnjumaAra P, Krishnaveni C, Venkatesh E. Ethosomes: A Novel Vesicular Drug Delivery System, International Journal of Advances in Pharmaceutical Research 2012; 2(1):16-27.
27. Kumar R, Aslam MD, Tripathi A, Prasad D, Chaudhary V, Jain V, Mishra SK, Singh R. Ethosomes: Novel Vesicular Carriers in Transdermal Drug Delivery, Journal of Global Pharma Technology 2010; 2(6):1-7.
28. Rathore AR, Khambete H, Jain S. Preparation and Characterization of Repaglinide Loaded Ethosomal Gel for the Treatment of NIDDM, International Journal of Pharmaceutical and Biological Archives 2013; 4(2):385-390.
29. Shahwal V, Samnani A, Dubey B, Bhowmick M. Ethosomes: An Overview, International Journal of Biomedical and Advance Research 2011; 2:161-168.
30. Kumar R, Aslam M.D, Tripathi A, Prasad D, Chaudhary V, Jain V, Mishra S K, Singh R. Ethosomes novel vesicular carriers in transdermal drug delivery. J Global Pharma Tech 2010; 2(6):1-7.
31. Heeremans JLM, Gerristen HR, Meusen SP, Mijnheer FW, Gangaram RS, Panday G, Prevost R, Kluft C, Crommelin DJA. The preparation of Tissue Type Plasminogen Activator (T- PA) containing liposomes: Entrapment Efficacy and Ultracentrifugation Damage, Journal of Drug Targeting 1995; 3:301.
32. Jain S, Umamaheshwari RB, Bhadra D, Jain NK. Ethosomes: A Novel Vesicular Carrier for Enhanced Transdermal Delivery of a Anti-HIV Agent, Indian Journal of Pharmaceutical Sciences 2004; 66:72-81.
33. Verma DD, Fahr A, Synergistic Penetration Effect of Ethanol and Phospholipids on the Topical Delivery of Cyclosporin, Journal of Controlled Release 2010; 97:55-66.
34. Touitou E. Composition of Applying Active Substance to or Through the Skin, US patent: 5, 540, 934, 1998.
35. Touitou E, Composition of Applying Active Substance to or Through The Skin, US patent: 5, 716, 638, 1996.
36. Tyagi LK, Kumar S, Maurya SS, Kori ML. Ethosomes novel vesicular carier for enhanced transdermal drug delivery system. Bulletin Pharm Res 2013; 3(1):6-13.
37. Dhurve R, Kashyap N, Mishra A, Pathak AK. A Holistic Review on Ethosome: A Promising Drug Delivery System for Topical Fungal Disease International Journal of Pharmaceutical & Biological Archives 2014; 5(5):13-26
38. Ghule AR, Shinkar DM, Saudagar RB. Ethosomes: Carrier for Enhanced Transdermal Drug Delivery System, J. Adv. Pharm. Edu. & Res. 2014; 4(4):380-387
39. Sudhakar K, Nitish U, Sanjay J R, Narayana C. Ethosomes as non-invasive Loom for transdermal drug delivery. Apple Academic Press Publication. 2012.
40. Maurya SD, Prajapati SK, Gupta AK Saxena GK, Dhakar RC, Formulation Development and Evaluation of Ethosome of Stavudine, Indian J.Pharm. Educ. Res. 2010; 44(1):102-108
41. Gangwar S, Ethosomes: For Drug Delivery, Journal of Pharmacy Research 2010; 3(4):688-691.
42. Kumar KP, Radhika PR, Sivakumar T. Ethosomes: A Priority in Transdermal Drug Delivery, International Journal of Advances in Pharmaceutical Sciences 2010; 1:111-121.
43. Touitou E at al., Composition of Applying Active Substance To or Through The Skin, US Patent: 5716638, 1996.
44. Touitou E at al., Composition of Applying Active Substance To or Through the Skin. US Patent: 5540934, 1998.
45. Mohanty D, Babu MN, Ankitha K, Gunde S, Bakshi V, Jat RM. Ethosome: a recent optimized technology for transdermal drug penetration, European Journal of Biomedical AND Pharmaceutical sciences 2016; 3(12):232-240.
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Zahid SR, Upmanyu N, Dangi S, Ray SK, Jain P, Parkhe G. Ethosome: a novel vesicular carrier for transdermal drug delivery. JDDT [Internet]. 15Nov.2018 [cited 30Apr.2024];8(6):318-26. Available from: https://jddtonline.info/index.php/jddt/article/view/2028
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