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Sustainable Alternatives to Petroleum-Derived Excipients in Pharmaceutical Oil-in-Water Creams

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Abstract

Recently, vast efforts towards sustainability have been made in the pharmaceutical industry. In conventional oil-in-water (O/W) cream formulations, various petroleum-based excipients, namely mineral oil and petrolatum, are commonly used. Natural or synthetic excipients, derived from vegetable sources, were explored as alternatives to petroleum-based excipients in prototype topical creams, with 1% (w/w) lidocaine. A conventional cream comprised of petroleum-derived excipients was compared to creams containing sustainable excipients in terms of key quality and performance attributes, physicochemical properties, and formulation performance. The petrolatum-based control formulation had the highest viscosity of 248.0 Pa·s, a melting point of 42.7°C, a low separation index at 25°C of 0.031, and an IVRT flux of 52.9 µg/cm2/h. Formulation SUS-4 was the least viscous formulation at 86.9 Pa·s, had the lowest melting point of 33.6°C, the highest separation index of 0.120, and the highest IVRT flux of 139.4 µg/cm2/h. Alternatively, SUS-5 had a higher viscosity of 131.3 Pa·s, a melting point of 43.6°C, a low separation index of 0.046, and the lowest IVRT flux of 25.2 µg/cm2/h. The cumulative drug permeation after 12 h from SUS-4, SUS-5, and the control were 126.2 µg/cm2, 113.8 µg/cm2, and 108.1 µg/cm2, respectively. The composition of the oil-in-water creams had influence on physicochemical properties and drug release; however, skin permeation was not impacted. Sustainable natural or synthetic excipients in topical cream formulations were found to be suitable alternatives to petroleum-based excipients with comparable key quality attributes and performance attributes and should be considered during formulation development.

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Acknowledgements

The authors would like to acknowledge David Nieto, a former Pfizer Summer Student worker 2021, that established correlations between sensorial attributes and instrumental measurements for topical cream formulations.

Funding

This work was funded by Pfizer Inc.

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Authors and Affiliations

  1. Drug Product Design, Worldwide Research, Development and Medical, Pfizer Inc., Groton, Connecticut, 06340, USA

    Dana Gates, Abu Zayed Md Badruddoza, Thean Yeoh & Jaymin Shah

  2. Department of Pharmaceutical Sciences, School of Pharmacy, The University of Texas at El Paso, 500 West University Ave, El Paso, Texas, 79902, USA

    Md Ikhtiar Zahid & Md Nurunnabi

  3. Eurofins Lancaster Laboratories Professional Scientific Services, 2425 New Holland Pike, Lancaster, Pennsylvania, 17601, USA

    Taylor Walsh

  4. Biomedical Engineering Program, College of Engineering, University of Texas at El Paso, El Paso, Texas, 79968, USA

    Md Nurunnabi

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  1. Dana Gates
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Contributions

Conceptualization: Gates and Badruddoza; data curation: Gates, Zahid, and Walsh; formal analysis: Gates and Badruddoza; funding acquisition: Gates and Badruddoza; investigation: Gates and Badruddoza; methodology: Gates, Badruddoza, Yeoh, and Zahid; project administration: Gates and Badruddoza; resources and supervision: Nurunnabi, Shah, Yeoh; visualization: Gates and Walsh; roles/writing original draft: Gates and Zahid; and writing—review and editing: Gates, Badruddoza, and Shah

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Correspondence to Dana Gates.

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Gates, D., Badruddoza, A.Z.M., Zahid, M.I. et al. Sustainable Alternatives to Petroleum-Derived Excipients in Pharmaceutical Oil-in-Water Creams. AAPS PharmSciTech 25, 68 (2024). https://doi.org/10.1208/s12249-024-02784-z

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