Formulation and Characterization of Efavirenz Nano emulsion Using Grapeseed Oil: A Strategy to Enhance Solubility and Stability

Authors

  • Raushan Kumar
  • Nagesh D R
  • Harish Kumar S
  • Koustav Dutta
  • Vasu Choudhary
  • Archana Singh
  • Sachin Kumar
  • Sonika Prajapati

Keywords:

N\A

Abstract

The purpose of this research was to create and assess a nanoemulsion of grapeseed oil and Efavirenz to improve the drug's solubility in the formulation and, therefore, its bioavailability.Multiple components were tested in sample formulations to choose the best one based on composition, factorial design, clarity, and simplicity of nanoemulsion generation. Transcutol P was chosen as a co-emulsifying agent, tween 80 as the preferable emulsifying agent, and grapeseed oil as the oil.Factorial design was used to find an optimized formulation using the Design Expert software. To make a clear nanoemulsion, the components were combined, efavirenz was added, and a small amount of water was added to the mixture. Particle-size, Zeta-potential, TEM, DSC, TGA, In-vitro drug release and viscosity tests were all examined for the formulation. The normal droplet size of the formulation were found within the 10nm.The zeta-potential of the preparation was originated to be -20.1mV, representing that the formulation is rather stable. Centrifuge method was used to assess the efficiency of the drug entrapment. The In-vitro release studies of liquid formulation showed an increase in drug release profile of 75.38±1.31% in contrast to the marketed formulation (SUSTIVA600) tablet which showed the maximum release of 44.09±0.45%. The kinetics models were applied to the percentage release profile of the NE and it shows that the optimized formulation follows


the zero order showing constant release pattern. The stability studies for the optimized formulation were performed for in total 90 days in and the shelf life for the formulation was found to be 591 days. Nanoemulsions are the great carrier for improving the bioavailability and solubility of the any lipophilic drug which ultimately helps in increasing the potency of any formulation. Nanoemulsions are great choice for vaccine development and can further used in many other applications like in cosmetics, food and nutrition etc.

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References

Powderly, William G., and Kenneth H. Mayer. 2003. “Editorial Commentary: Centers for Disease Control and Prevention Revised Guidelines for Human Immunodeficiency Virus (HIV) Counseling, Testing, and Referral: Targeting HIV Specialists.” Clinical Infectious Diseases 37 (6): 813–19.

Celum, C. L., R. W. Coombs, W. Lafferty, T. S. Inui, P. H. Louie, C. A. Gates, B. J. McCreedy, et al. 1991. “Indeterminate Human Immunodeficiency Virus Type 1 Western Blots: Seroconversion Risk, Specificity of Supplemental Tests, and an Algorithm for Evaluation.” Journal of Infectious Diseases 164 (4): 656–64.

Chou, Roger, Shelley Selph, Tracy Dana, Christina Bougatsos, Bernadette Zakher, Ian Blazina, and P. Todd Korthuis. 2012. “Screening for HIV: Systematic Review to Update the 2005 U.S. Preventive Services Task Force Recommendation.” Annals of Internal Medicine 157 (10): 706.

Haehl, Manfred. 2001. “Nevirapine and Postexposure Prophylaxis for Human Immunodeficiency Virus.” JAMA 285 (7): 883.

Rodari, Anthony, Gilles Darcis, and Carine M. Van Lint. 2021. “The Current Status of Latency Reversing Agents for HIV-1 Remission.” Annual Review of Virology 8 (1): 491–514.

Fauci, Anthony S., and Gregory K. Folkers. 2012. “Toward an AIDS-Free Generation.” JAMA 308 (4): 343.

Deeks, Steven G, Sharon R Lewin, and Diane V Havlir. 2013. “The End of AIDS: HIV Infection as a Chronic Disease.” The Lancet 382 (9903): 1525–33.

Ravi T P U, Padma T (2011) Nanoemulsions for drug delivery through different routes. Res. Biotechnol. 2(3): 1-13.

Kotta S, Khan AW, Pramod K, Ansari S H, Sharma R K, Ali J (2012) Exploring oral nanoemulsions for bioavailability enhancement of poorly water-soluble drugs. Expert Opin. Drug Deliv. 9(5): 585-598.

Dixit RP, Nagarsenker MS (2008) Self-nanoemulsifying granules of ezetimibe: design, optimization and evaluation. Eur. J. Pharm. Sci. 35: 3183-3192.

Shafiq S, Shakeel F, Talegaonkar S (2007) Development and bioavailability assessment of ramipril nanoemulsion formulation. Eur. J. Pharm. Biopharm. 66: 2227-2243

Gasco MR, Gallarate M, Pattarino F (1991) In vitro permeation of azelaic acid from viscosized microemulsions. Int J Pharm 69:193–196

Kriwet K, Muller-Goymann C (1995) Diclofenac release from phospholipid drug systems and permeation through excised human stratum corneum. Int J Pharm 125:231–242

“Fiz. Khim. Mekh. Mater.” 1993. Metal Powder Report 48 (2): 37.

Mohr, K.-H. 1987. “High-Pressure Homogenization. Part II. The Influence of Cavitation on Liquid-Liquid Dispersion in Turbulence Fields of High Energy Density.” Journal of Food Engineering 6 (4): 311–24.

Stone, H. A., B. J. Bentley, and L. G. Leal. 1986. “An Experimental Study of Transient Effects in the Breakup of Viscous Drops.” Journal of Fluid Mechanics 173 (December): 131–58.

Abismaı̈l. B, J.P Canselier, A.M Wilhelm, H Delmas, and C Gourdon. 1999. “Emulsification by Ultrasound: Drop Size Distribution and Stability.” Ultrasonics Sonochemistry 6 (1-2): 75–83.

Alegria, Antonio E., Yves Lion, Takashi Kondo, and Peter Riesz. 1989. “Sonolysis of Aqueous Surfactant Solutions: Probing the Interfacial Region of Cavitation Bubbles by Spin Trapping.” The Journal of Physical Chemistry 93 (12): 4908–13.

Stone, H.A., A.D. Stroock, and A. Ajdari. 2004. “ENGINEERING FLOWS in SMALL DEVICES.” Annual Review of Fluid Mechanics 36 (1): 381–411.

Paquin, Paul. 1999. “Technological Properties of High Pressure Homogenizers: The Effect of Fat Globules, Milk Proteins, and Polysaccharides.” International Dairy Journal 9 (3-6): 329–35.

Utada, A. S., L.-Y. Chu, A. Fernandez-Nieves, D. R. Link, C. Holtze, and D. A. Weitz. 2007. “Dripping, Jetting, Drops, and Wetting: The Magic of Microfluidics.” MRS Bulletin 32 (9): 702–8.

Shinoda, K, and H Saito. 1968. “The Effect of Temperature on the Phase Equilibria and the Types of Dispersions of the Ternary System Composed of Water, Cyclohexane, and Nonionic Surfactant.” Journal of Colloid and Interface Science 26 (1): 70–74.

Shinoda, Kōzō, and Hiroshi Saito. 1969. “The Stability of O/W Type Emulsions as Functions of Temperature and the HLB of Emulsifiers: The Emulsification by PIT-Method.” Journal of Colloid and Interface Science 30 (2): 258–63.

Shinoda, K., M. Hanrin, H. Kunieda, and H. Saito. 1981. “Principles of Attaining Ultra-Low Interfacial Tension: The Role of Hydrophile—Lipophile-Balance of Surfactant at Oil/Water Interface.” Colloids and Surfaces 2 (4): 301–14.

Warson, H. 1987. “Emulsions and Solubilization: K. Shinoda and S. Friberg, Wiley-Interscience, New York, 1986. Pp. Xiii + 174, Price £43.25. ISBN 0-471-03646-3.” British Polymer Journal 19 (6): 544–45.

Taisne, L., and B. Cabane. 1998. “Emulsification and Ripening Following a Temperature Quench†.” Langmuir 14 (17): 4744–52.

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Published

2025-06-21

How to Cite

1.
Kumar R, D R N, Kumar S H, Dutta K, Choudhary V, Singh A, Kumar S, Prajapati S. Formulation and Characterization of Efavirenz Nano emulsion Using Grapeseed Oil: A Strategy to Enhance Solubility and Stability. J Neonatal Surg [Internet]. 2025Jun.21 [cited 2025Jul.15];14(32S):1473-85. Available from: https://jneonatalsurg.com/index.php/jns/article/view/7591