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In vitro–in vivo correlation of microsphere formulations: recent advances and challenges

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Abstract

Background

Microsphere formulations prepared using biodegradable polymers are among the most common strategies used for controlled-release drug delivery. These formulations can be loaded with a wide array of drugs, including chemicals and peptides, enabling prolonged release periods. However, establishing a standardized release profile for microsphere formulations is challenging because of their complexity and diversity. For this reason, there is no official method for in vitro–in vivo correlation (IVIVC) of microspheres.

Area covered

This review outlines a method for developing IVIVC of microsphere formulations based on the United States Food and Drug Administration guidance for extended-release oral dosage forms. It briefly provides definitions and summarizes each stage of the method. In addition, we discuss the findings of recent studies on obstacles and influencing factors in developing IVIVC of microspheres.

Expert opinion

IVIVC is an effective model for quality control during manufacturing and an indicator of in vivo performance. Ultimately, it can serve as a surrogate for costly and time-consuming human bioequivalence studies. The IVIVC of microspheres has become an important concern as the microsphere drug market grows. This review provides a plethora of examples for microsphere IVIVC to enhance predictability.

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Acknowledgements

This work was supported by a grant (22183MFDS366) from Ministry of Food and Drug Safety of South Korea in 2022–2025.

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Author notes

  1. Sung Soo Kim and Si Won Ro have contributed equally to this work.

Authors and Affiliations

  1. College of Pharmacy, Chung-Ang University, 84 Heukseok-ro, Dongjak-gu, Seoul, 06974, Republic of Korea

    Sung Soo Kim, Si Won Ro & Dong Hee Na

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  1. Sung Soo Kim
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  2. Si Won Ro
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Correspondence to Dong Hee Na.

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Kim, S.S., Ro, S.W. & Na, D.H. In vitro–in vivo correlation of microsphere formulations: recent advances and challenges. J. Pharm. Investig. 54, 37–49 (2024). https://doi.org/10.1007/s40005-023-00655-6

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