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Pharmaceutical Product Characterization and Manufacturability of Surfactant-Enriched Oil Marbles with Abiraterone Acetate

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Abstract

The present study investigates the physicochemical properties and stability of a novel lipid-based formulation—surfactant-enriched oil marbles containing abiraterone acetate. While the biopharmaceutical performance of this formulation has been reported recently, this study aims to fill the gap between a promising in vivo performance and industrial applicability. A series of techniques were employed to assess the solid-state characteristics of oil marble cores along with their physicochemical properties upon stability testing. The chemical stability of abiraterone acetate in the formulation was also investigated. The core of the formulation was found to be stable both physically and chemically over 12 months of storage. The in vitro performance of stressed samples was evaluated using a dissolution experiment. The formulation has successfully self-emulsified upon incubation in bio-relevant media, resulting in a fast and complete API release. An important issue connected with the excipient used as a covering material of oil marbles has been identified. The seemingly insignificant water sorption caused agglomeration of the oil marbles and consequently compromised the dissolution rate in some of the stressed samples. Replacing HPMC with lactose as a covering material resulted in more favorable properties upon storage. Overall, it has been shown that oil marbles are an industrially applicable concept of the solidified lipid-based formulation.

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Acknowledgements

The authors would like to thank The Pharmaceutical Applied Research Centre (The PARC) and Zentiva k.s for supporting this work.

Funding

F.S. would like to acknowledge support by the Czech Science Foundation (project 19-26127X).

Author information

Authors and Affiliations

  1. Zentiva, k.s. U Kabelovny 130, 102 37, Prague, Czech Republic

    Jakub Petřík, Ondřej Rychecký, Tereza Krejčí, Dan Trunov, Ondřej Navrátil, Pavel Žvátora, Lukáš Krejčík, Ondřej Dammer, Josef Beránek & Jakub Heřt

  2. Department of Chemical Engineering, University of Chemistry and Technology, Prague, Technická 5, 166 28, Prague, Czech Republic

    Ondřej Rychecký, Tereza Krejčí, Dan Trunov, Maximilián Prachár, Ondřej Navrátil, Miroslav Šoóš & František Štěpánek

  3. Department of Analytical Chemistry, University of Chemistry and Technology, Prague, Technická 5, 166 28, Prague, Czech Republic

    Jakub Petřík & Lucia Becherová

  4. Department of Analytical Chemistry, Faculty of Science, Charles University, Prague, Czech Republic

    Petr Kozlík & Tomáš Křížek

  5. DottBonapace &C srl, Via A.Merli 10/A, Cusano Milanino (MI), Italy

    Samuele Bissola & Simone Berto

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  1. Jakub Petřík
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Contributions

J. Petřík: degradation products analysis, manuscript writing.

O. Rychecký: liquid marble formulation and processing, mechanical properties testing, flow properties testing, manuscript writing.

T. Boleslavská: dissolution tests, manuscript writing.

L. Becherová: spectroscopic analysis, manuscript writing.

D. Trunov: emulsion characterization, manuscript writing.

M. Prachár: liquid marble processing, mechanical properties testing, manuscript writing.

O. Navrátil: micro-CT analysis, manuscript writing.

P. Žvátora: liquid marble formulation, manuscript writing.

L. Krejčík: analytical method development, manuscript writing.

O. Dammer: DSC and XPRD analysis, manuscript writing.

J. Beránek: dissolution testing, manuscript writing.

P. Kozlík: analytical method development, manuscript writing.

T. Křížek: analytical method development, manuscript writing.

M. Šoóš: dynamic light scattering data interpretation, manuscript writing.

J. Heřt: analytical method development, manuscript writing.

S. Bissola: capsule filling experiments, manuscript writing.

S. Berto: capsule filling experiments, manuscript writing.

F. Štěpánek: conceptualization, supervision, funding acquisition, manuscript writing.

Corresponding author

Correspondence to František Štěpánek.

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Conflict of Interest

O. Rychecky is the owner of a start-up company MarbleMat, s.r.o., which develops liquid marble formulations. Other authors declare no competing financial interests.

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Petřík, J., Rychecký, O., Krejčí, T. et al. Pharmaceutical Product Characterization and Manufacturability of Surfactant-Enriched Oil Marbles with Abiraterone Acetate. AAPS PharmSciTech 23, 274 (2022). https://doi.org/10.1208/s12249-022-02430-6

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