Development and characterization of miconazole nitrate transfersomal gel

  • Shaik Sajid Ali Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur-34, Andhra Pradesh, India.
  • Madhu Gudipati Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur-34, Andhra Pradesh, India.
  • Ramarao Nadendla Department of Pharmaceutics, Chalapathi Institute of Pharmaceutical Sciences, Lam, Guntur-34, Andhra Pradesh, India.
Keywords: Antifungal activity, Carbapol 934, Entrapment efficiency, Miconazole nitrate, Transfersomes

Abstract

Miconazole nitrate (MIC) is an antifungal drug used for the treatment of superficial fungal infections. However, it has low skin permeability. Hence, the basic idea behind the development of such a system, transfersomes is to maintain a sustain release of drug from the dosage form and for target delivery. Miconazole nitrate was formulated as transfersomes, half-life can be increased and the desired effect can be obtained. MIC transfersomes were prepared using a thin lipid film hydration technique. The prepared transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of MIC transfersomes was incorporated into a Carbapol 934 gel base which was for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro activity. The prepared MIC transfersomes had a high EE% ranging from 65.45% to 80.11%, with small particle sizes ranging from 368 nm to 931 nm. The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. In 24 hrs the drug release was observed ranging from 79.08% to 88.72%. The kinetic analysis of all release profiles was found to follow Higuchi’s diffusion model. All independent variables had a significant effect on the dependent variables (p-values < 0.05). Therefore, Miconazole nitrate in the form of transfersomes has the ability to penetrate the skin, overcoming the stratum corneum barrier. When the data subjected to zero order and first order kinetics model, a linear relationship was observed with high R2 values for zero order model as compared to first order model and suggested that the formulations followed zero order sustained release.

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References

Qushawy, M., Nasr, A., Abd-Alhaseeb, M., & Swidan, S. (2018). Design, optimization and characterization of a transfersomal gel using miconazole nitrate for the treatment of candida skin infections. Pharmaceutics, 10(1), 26. DOI: 10.3390/pharmaceutics10010026. DOI: https://doi.org/10.3390/pharmaceutics10010026

Premchandani, L. A., Bakliwal, S. R., Rane, B. R., Gujarathi, N. A., Patil, V. B., & Pawar, S. P. (2016). Protransfersome: ultraflexible vesicular approach for transdermal drug delivery system. Indian Journal of Drugs, 4(2), 28-41.

Vinod, K. R., Kumar, M. S., Anbazhagan, S., Sandhya, S., Saikumar, P., Rohit, R. T., & Banji, D. (2012). Critical issues related to transfersomes-novel vesicular system. ACTA Scientiarum Polonorum Technologia Alimentaria, 11(1), 67-82.

Sangwan, S., & Dureja, H. (2009). Pharmacosomes: A potential alternative to conventional vesicular systems.

Wf, L. (1990). Schaumburg-Lever G. Histopathology of the skin. J.B. Lippincott Company, 7th edition, Philadelphia.

Chaurasia, L., Singh, S., Arora, K., & Saxena, C. (2019). Transferosome: A Suitable Delivery System for Percutaneous Administration. Current Research in Pharmaceutical Sciences, 1-11. DOI: https://doi.org/10.24092/CRPS.2019.090101

Fartasch, M., Bassukas, I. D., & Diepgkn, T. L. (1993). Structural relationship between epidermal lipid lamellae, lamellar bodies and desmosomes in human epidermis: an ultrastructural study. British Journal of Dermatology, 128(1), 1-9. DOI: https://doi.org/10.1111/j.1365-2133.1993.tb00138.x

Ford, J. L., Rubinstein, M. H., & Hogan, J. E. (1985). Propranolol hydrochloride and aminophylline re-lease from matrix tablets containing hydroxypro-pylmethylcellulose. International journal of pharmaceutics, 24(2-3), 339-350. DOI: https://doi.org/10.1016/0378-5173(85)90032-8

Remuñán-López, C., Portero, A., Vila-Jato, J. L., & Alonso, M. J. (1998). Design and evaluation of chitosan/ethylcellulose mucoadhesive bilayered de-vices for buccal drug delivery. Journal of controlled release, 55(2-3), 143-152. DOI: https://doi.org/10.1016/S0168-3659(98)00044-3

Benson, H. A. (2005). Transdermal drug delivery: penetration enhancement techniques. Current drug delivery, 2(1), 23-33. DOI: https://doi.org/10.2174/1567201052772915

Mezei, M., & Gulasekharam, V. (1980). Liposomes-a selective drug delivery system for the topical route of administration I. Lotion dosage form. Life Sciences, 26(18), 1473-1477. DOI: https://doi.org/10.1016/0024-3205(80)90268-4

Thakur, N., Jain, P., & Jain, V. (2018). Formulation Development and Evaluation of transferosomal gel. Journal of Drug Delivery and Therapeutics, 8(5), 168-177. DOI: https://doi.org/10.22270/jddt.v8i5.1826

Salman, B. S., & Baig, M. A. H. (2019). Formulation and evaluation of nanoparticulate ofloxacin ophthalmic gel using ionic gelation method. International Journal of Research in Pharmaceutical Sciences and Technology, 1(2), 73-78. DOI: https://doi.org/10.33974/ijrpst.v1i2.148

US Food and Drug Administration. (1995). Code of Federal register.

Sathe, S., Bagade, M., Nandgude, T., Kore, K., & Shete, R. (2015). Formulation and evaluation of thermoreversible in-situ nasal gel of terbutaline sulphate. Indo Am J Pharm Res, 5, 3680-7.

Patel, R., Singh, S. K., Singh, S., Sheth, N. R., & Gen-dle, R. (2009). Development and characterization of curcumin loaded transfersome for transdermal delivery. Journal of pharmaceutical sciences and research, 1(4), 71.

Purushottam, S. S., Bhaskarrao, G. S., & Bhanudas, S. R. (2013). Gelified emulsion: a newborn formulation for topical delivery of hydrophobic drugs. World journal of pharmacy and pharmaceutical sciences, 3, 233-251.

Masmoudi, H., Piccerelle, P., Le Dréau, Y., & Kister, J. (2006). A rheological method to evaluate the physical stability of highly viscous pharmaceutical oil-in-water emulsions. Pharmaceutical Research, 23(8), 1937-1947. DOI: https://doi.org/10.1007/s11095-006-9038-x

Prajapati, S. T., Patel, C. G., & Patel, C. N. (2011). Transfersomes: a vesicular carrier system for transdermal drug delivery. Asian Journal of Bio-chemical and Pharmaceutical Research, 2(1), 507-524.

Bargir, T. N., Aj, A., & Sa, P. (2016). Composition of terbinafine HCL polymeric gel for mucosal drug delivery.

Sanjay, Jain, B. D., Padsalg, A., Patel, K., & Mokale, V. (2007). Formulation development and evaluation of fluconazole gel in various polymer bases-formulation development and evaluation of fluconazole gel in various polymer bases. Asian Journal of Pharmaceutics, 1(1), 63-68.

Published
23-06-2020
How to Cite
Shaik Sajid Ali, Madhu Gudipati, & Ramarao Nadendla. (2020). Development and characterization of miconazole nitrate transfersomal gel. International Journal of Research in Pharmaceutical Sciences and Technology, 1(4), 109-116. https://doi.org/10.33974/ijrpst.v1i4.200
Section
Research Article