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Encapsulation and physicochemical evaluation of efavirenz in liposomes

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Abstract

Purpose

Antiretroviral therapy remains the most effective means of managing the human immune deficiency virus/acquired immune deficiency syndrome (HIV/AIDS). Application of therapeutics has been hampered by factors including poor bioavailability of most anti-retroviral compounds (ARV), side effects and an alarming emergence of drug resistant strains of the virus.

Methods

Recent developments and use of drug delivery systems (DDS) has shown potential for improving the pharmacological profile of ARV. Amongst these complex DDS, liposomes have been explored for delivery of ARV. In this study, we have aimed at exploring efficient encapsulation of efavirenz (EFV), a potent ARV using different mass ratios of crude soybean lecithin and cholesterol.

Results

The EFV-loaded liposomes (EFL) were prepared using thin film hydration and evaluated for particle size, zeta potential (ZP), encapsulation efficiency (EE%), morphology and drug release studies. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), energy dispersity spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy were used for comprehensive physicochemical characterization of EFL. EFL exhibited high encapsulation (99%) in 1:1 crude lecithin to cholesterol mass ratio. The average particle size and Zeta Potential of EFL were found to be 411.10 ± 7.40 nm and − 53.5.3 ± 0.06 mV, respectively. EFL showed a relatively controlled EFV release behaviour that was similar to the dissolution profile of un-encapsulated EFV.

Conclusion

This suggests that EFL represents a promising vehicle for effective EFV delivery while providing the advantages of a nano-scaled delivery system.

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Acknowledgements

The authors wish to acknowledge the National Research Foundation South Africa through the DST innovation, Rhodes University, and Sundra Cleaning Company for their financial assistance.

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Authors and Affiliations

  1. Department of Chemistry, Faculty of Science, Rhodes University, Grahamstown, 6140, Eastern Cape, South Africa

    Nnamdi Ikemefuna Okafor, Christian Isalomboto Nkanga, Xavier Siwe Noundou & Rui Werner Marçedo Krause

  2. Division of Pharmaceutics, Faculty of Pharmacy, Rhodes University, Grahamstown, 6140, Eastern Cape, South Africa

    Roderick Bryan Walker

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  1. Nnamdi Ikemefuna Okafor
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  2. Christian Isalomboto Nkanga
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  3. Roderick Bryan Walker
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  4. Xavier Siwe Noundou
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  5. Rui Werner Marçedo Krause
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Correspondence to Rui Werner Marçedo Krause.

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Okafor, N.I., Nkanga, C.I., Walker, R.B. et al. Encapsulation and physicochemical evaluation of efavirenz in liposomes. J. Pharm. Investig. 50, 201–208 (2020). https://doi.org/10.1007/s40005-019-00458-8

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  • DOI: https://doi.org/10.1007/s40005-019-00458-8

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