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Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes

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Abstract

Near-infrared (NIR) approaches is considered one of the most well-studied process analyzers evolving from the process analytical technology initiatives. The objective of this study was to evaluate NIR spectroscopy and imaging to assess individual components within a novel tenofovir liposomal formulation. By varying stearylamine, as a positive charge imparting agent, five batches were prepared by the thin film method. Each formulation was characterized in terms of drug entrapment efficiency, release characteristics, particle sizing, and zeta potential. Drug excipients compatibility was tested using Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The obtained results showed an increase in drug entrapment and a slower drug release by increasing the incorporated percentage of stearylamine. The compatibility testing revealed a significant interaction between the drug and some of the investigated excipients. The developed NIR calibration model was able to assess drug, phospholipid, and stearylamine levels along the batches. The calibration and prediction plots were linear with correlation coefficients of more than 0.9. The root square standard errors of calibration and prediction did not attain 5% of the measured values confirming the accuracy of the model. In contrast, NIR spectral imaging was capable of clearly distinguishing the different batches, both qualitatively and quantitatively. A linear relationship was obtained correlating the actual drug entrapped and the predicted values obtained from the partial least squares images.

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Authors and Affiliations

  1. Division of Product Quality Research, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, Maryland, USA

    Ahmed S. Zidan, Crystal Spinks & Mansoor A. Khan

  2. School of Pharmacy, Department of Pharmaceutical Sciences, Howard University, Washington, District of Columbia, USA

    Crystal Spinks, Joseph Fortunak & Muhammad Habib

  3. Faculty of Pharmacy, Department of pharmaceutics, Zagazig University, Zagazig, Egypt

    Ahmed S. Zidan

Authors
  1. Ahmed S. Zidan
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  2. Crystal Spinks
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  3. Joseph Fortunak
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  4. Muhammad Habib
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  5. Mansoor A. Khan
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Correspondence to Mansoor A. Khan.

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This scientific contribution is intended to support regulatory policy development. The views presented in this article have not been adopted as regulatory policies by the Food and Drug Administration at this time.

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Zidan, A.S., Spinks, C., Fortunak, J. et al. Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes. AAPS J 12, 202–214 (2010). https://doi.org/10.1208/s12248-010-9177-1

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  • DOI: https://doi.org/10.1208/s12248-010-9177-1

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