Formulation and Evaluation of Invasomal and Ethosomal Gel for Curcumin and Determination of Anti- Fungal Activity


Cite item

Full Text

Abstract

Background:Despite exhibiting anti-inflammatory, antiseptic, and anti-cancer properties, curcumin is not exhibiting the same efficacy as that other non-steroidal anti-inflammatory agents and anti-cancer drugs. The main reason is its poor solubility and poor permeability. To improve the solubility the particle size has to be reduced to the nano level and to improve the permeability vesicular drug delivery approaches have to be adapted. By developing invasomal and ethosomal gels the bioavailability of curcumin can be enhanced.

Aim and Objective:The main aim of the study is to develop Invasomal and Ethosomal drug delivery systems for curcumin by various techniques.

Methods:Curcumin loaded invasomes were prepared by using a thin film hydration method. Six formulations were prepared by varying drug to lipid ratios (INV1 to INV6). Soya lecithin was used as a phospholipid, span60 was used as a surfactant, limonene was used as terpene, ethanol and chloroform were used as solvents. Curcumin-loaded ethosomes were prepared by using a hot method. Five formulations were prepared by increasing lipid concentration (E1 to E5). Soya lecithin as lipid, propylene glycol, and ethanol as solvent. The prepared formulations were evaluated for particle size, zeta potential, drug content, entrapment efficiency. and in vitro drug release studies.

Results:Among all the formulations of Invasomes, INV3 formulation containing a 1:5 ratio of the drug (40 mg) to lipid (200 mg) was considered as best formulation because of its particle size of 327. A total of 1nm, zeta potential of -32.6 mV, highest drug content of 97.5%, entrapment efficiency of 96%, and in vitro drug release of 95% in a time period of 12 hrs. Among all the formulations of ethosomes, the E3 formulation was considered as best formulation due to its particle size of 697.5 nm, zeta potential of - 28.0 Mv, highest drug content of 97.3%, entrapment efficiency of 90%, and in vitro drug release of 94.6% in a time period of 12 hrs.

Conclusion:The best invasomal and ethosomal formulations were incorporated into gel and evaluated for pH, viscosity, Spreadability, drug content, in vitro drug release studies, and ex vivo studies. INV3 and E3 were incorporated into gel and comparative studies were made with plain gel. Among the three gels (PG, INV3G, E3G), invasomal gel (INV3) exhibited the highest content drug content of 81%, pH of 6.6, spreadability 14.8g cm/sec, in vitro drug release of 90.6%, ,and ex vivo drug release of 97% in a time period of 12 hrs with the release rate of 32.53 microgram/cm2/hr-1/2, the flux of 0.346 μg/cm2/hr and permeation coefficient of 42.71 cm/hr.

About the authors

Abbaraju Sailaja

Department of Pharmaceutic, RBVRR Women’s College of Pharmacy,, Affiliated to Osmania University

Author for correspondence.
Email: info@benthamscience.net

Thoudaboina Meghana

Department of Pharmaceutic, RBVRR Women’s College of Pharmacy, Affiliated to Osmania University

Email: info@benthamscience.net

References

  1. Sammeta SM, Repka MA, Narasimha Murthy S. Magnetophoresis in combination with chemical enhancers for transdermal drug delivery. Drug Dev Ind Pharm 2011; 37(9): 1076-82. doi: 10.3109/03639045.2011.559659 PMID: 21449699
  2. Patel M, Joshi A, Hassanzadeth H, Juluru R, Stagni G. Quantification of dermal and transdermal delivery of meloxicam gels in rabbits. Drug Dev Ind Pharm 2011; 37(5): 613-7. doi: 10.3109/03639045.2010.534098 PMID: 21469950
  3. Din Fakhar ud, Zeb A. Effective use of nanocarriers as drug delivery systems for the treatment of selected tumors. International journal of nanomedicine 2017; 12: 7291-309.
  4. Yang Z, Teng Y, Wang H, Hou H. Enhancement of skin permeation of bufalin by limonene via reservoir type transdermal patch: Formu-lation design and biopharmaceutical evaluation. Int J Pharm 2013; 447(1-2): 231-40. doi: 10.1016/j.ijpharm.2013.02.048 PMID: 23467076
  5. Ahad A, Aqil M, Ali A. Investigation of antihypertensive activity of carbopol valsartan transdermal gel containing 1,8-cineole. Int J Biol Macromol 2014; 64: 144-9. doi: 10.1016/j.ijbiomac.2013.11.018 PMID: 24296403
  6. Zhou W, He S, Yang Y, Jian D, Chen X, Ding J. Formulation, characterization and clinical evaluation of propranolol hydrochloride gel for transdermal treatment of superficial infantile hemangioma. Drug Dev Ind Pharm 2015; 41(7): 1109-19. doi: 10.3109/03639045.2014.931968 PMID: 25151873
  7. Ainbinder D, Touitou E. Testosterone ethosomes for enhanced transdermal delivery. Drug Deliv 2005; 12(5): 297-303. doi: 10.1080/10717540500176910 PMID: 16188729
  8. Paolino D, Lucania G, Mardente D, Alhaique F, Fresta M. Ethosomes for skin delivery of ammonium glycyrrhizinate: In vitro percutane-ous permeation through human skin and in vivo anti-inflammatory activity on human volunteers. J Control Release 2005; 106(1-2): 99-110. doi: 10.1016/j.jconrel.2005.04.007 PMID: 15935505
  9. Touitou E, Dayan N, Bergelson L, Godin B, Eliaz M. Ethosomes-novel vesicular carriers for enhanced delivery: Characterization and skin penetration properties. J Control Release 2000; 65(3): 403-18. doi: 10.1016/S0168-3659(99)00222-9 PMID: 10699298
  10. Dragicevic-Curic N, Scheglmann D, Albrecht V, Fahr A. Temoporfin-loaded invasomes: Development, characterization and in vitro skin penetration studies. J Control Release 2008; 127(1): 59-69. doi: 10.1016/j.jconrel.2007.12.013 PMID: 18281119
  11. Barel AO, Paye M, Maibach HI. Handbook of cosmetic science and technology. CRC press 2009; p. 802. doi: 10.1201/b15273
  12. Dragicevic-Curic N, Scheglmann D, Albrecht V, Fahr A. Development of different temoporfin-loaded invasomes-novel nanocarriers of temoporfin: Characterization, stability and in vitro skin penetration studies. Colloids Surf B Biointerfaces 2009; 70(2): 198-206. doi: 10.1016/j.colsurfb.2008.12.030 PMID: 19188048
  13. Shah SM, Ashtikar M, Jain AS, et al. LeciPlex, invasomes, and liposomes: A skin penetration study. Int J Pharm 2015; 490(1-2): 391-403. doi: 10.1016/j.ijpharm.2015.05.042 PMID: 26002568
  14. Sapra B, Jain S, Tiwary AK. Percutaneous permeation enhancement by terpenes: Mechanistic view. AAPS J 2008; 10(1): 120-32. doi: 10.1208/s12248-008-9012-0 PMID: 18446512
  15. Lakshmi PK, Kalpana B, Prasanthi D. Invasomes-novel vesicular carriers for enhanced skin permeation. Syst Rev Pharmacy 2014; 4(1): 26-30.
  16. Rizvi SAA, Saleh AM. Applications of nanoparticle systems in drug delivery technology. Saudi Pharm J 2018; 26(1): 64-70. doi: 10.1016/j.jsps.2017.10.012 PMID: 29379334
  17. Williams AC, Barry BW. Penetration enhancers. Adv Drug Deliv Rev 2004; 56(5): 603-18. doi: 10.1016/j.addr.2003.10.025 PMID: 15019749
  18. Lahora D. Terpenes: Natural skin penetration enhancers in transdermal drug delivery system. Int J Pharma Res Dev 2011; 2: 39-45.
  19. Pfister WR, Hsieh DS, Hsieh S. Permeation enhancers compatible with transdermal drug delivery systems. Part I: selection and formula-tion considerations. Med Device Technol 1990; 1(5): 48-55. PMID: 10171148
  20. Obata Y, Takayama K, Machida Y, Nagai T. Combined effect of cyclic monoterpenes and ethanol on percutaneous absorption of diclo-fenac sodium. Drug Des Discov 1991; 8(2): 137-44. PMID: 1793775
  21. Dayan N, Touitou E. Carriers for skin delivery of trihexyphenidyl HCl: ethosomes vs. liposomes. Biomaterials 2000; 21(18): 1879-85. doi: 10.1016/S0142-9612(00)00063-6 PMID: 10919691
  22. Verma P, Pathak K. Nanosized ethanolic vesicles loaded with econazole nitrate for the treatment of deep fungal infections through topical gel formulation. Nanomedicine 2012; 8(4): 489-96. doi: 10.1016/j.nano.2011.07.004 PMID: 21839053
  23. Valenta C, Janisch M. Permeation of cyproterone acetate through pig skin from different vehicles with phospholipids. Int J Pharm 2003; 258(1-2): 133-9. doi: 10.1016/S0378-5173(03)00180-7 PMID: 12753760
  24. Kumar L, Verma S, Singh K, Prasad DN, Jain AK. Ethanol based vesicular carriers in transdermal drug delivery: Nanoethosomes and transethosomes in focus. NanoWorld J 2016; 2(3): 41-51. doi: 10.17756/nwj.2016-030
  25. Barel AO, Paye M, Maibach HI. Handbook of Cosmetic Science and Technology. (4th ed.), Boca Raton, FL, USA: CRC Press 2014. doi: 10.1201/b16716
  26. Cornwell PA, Barry BW, Bouwstra JA, Gooris GS. Modes of action of terpene penetration enhancers in human skin; Differential scan-ning calorimetry, small-angle X-ray diffraction and enhancer uptake studies. Int J Pharm 1996; 127(1): 9-26. doi: 10.1016/0378-5173(95)04108-7
  27. Kamran M, Ahad A, Aqil M, Imam SS, Sultana Y, Ali A. Design, formulation and optimization of novel soft nano-carriers for transder-mal olmesartan medoxomil delivery: In vitro characterization and in vivo pharmacokinetic assessment. Int J Pharm 2016; 505(1-2): 147-58. doi: 10.1016/j.ijpharm.2016.03.030 PMID: 27005906
  28. Cui Y, Li L, Zhang L, et al. Enhancement and mechanism of transdermal absorption of terpene-induced propranolol hydrochloride. Arch Pharm Res 2011; 34(9): 1477-85. doi: 10.1007/s12272-011-0909-2 PMID: 21975809
  29. Prasanthi D, Lakshmi PK. Iontophoretic transdermal delivery of finasteride in vesicular invasomal carriers. Pharm Nanotechnol 2013; 1: 136-50. doi: 10.2174/2211738511301020009
  30. Badran M, Shazly G, El-Badry M. Effect of terpene liposomes on the transdermal delivery of hydrophobic model drug, nimesulide: Characterization, stability and in vitro skin permeation. Afr J Pharm Pharmacol 2012; 6(43): 3018-26. doi: 10.5897/AJPP12.552
  31. Lakshmi P, Mounica V, Manoj KY, Prasanthi D. Preparation and evaluation of curcumin invasomes. Int J Drug Deliv 2014; 6: 113-20.
  32. Bibisara. Formulaton and evaluation of curcumin loaded ethosomes by hot and cold method. PhD Thesis, Osmania University, October 2019.
  33. Inayat Bashir Pathan et al Curcumin loaded ethosomes for transdermal application: Formulation, optimization, in-vitro and in-vivo study. Journal of Drug Delivery Science and Technology 2018; 44: 49-57.

Supplementary files

Supplementary Files
Action
1. JATS XML
Download

Copyright (c) 2024 Bentham Science Publishers