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Co-amorphous Drug Delivery Systems: a Review of Physical Stability, In Vitro and In Vivo Performance

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Abstract

Over the past few decades, co-amorphous solids have been used as a promising approach for delivering poorly water-soluble drugs. Co-amorphous solids, comprising pharmacologically relevant drug substances or excipients, improve physical stability, solubility, dissolution, and bioavailability compared with single amorphous ingredients. In this review, we have summarized recent advances in physical stability and in vitro and in vivo performances of co-amorphous solids. We have highlighted the role of molar ratio, molecular interaction, and mobility that affects the physical stability of co-amorphous solids. This review delves deep as to how co-amorphous solids affect the physicochemical properties in vitro and in vivo. We also described the challenges to the formulation of co-amorphous solids. A better understanding of the mechanisms of the physical stability, in vitro and in vivo performance of co-amorphous solids, and proper selection of the co-former is likely to expedite the development of robust co-amorphous-based pharmaceutical formulations and can address the challenges associated with the delivery of poorly soluble drugs.

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Copyright © 2015 American Chemical Society)

Fig. 2

Copyright © 2021 Elsevier)

Fig. 3

Copyright © 2018 American Chemical Society)

Fig. 4

(Adapted from Ref. 51 with the permission of the American Chemical Society)

Fig. 5

(Copyright © 2019 Elsevier)

Fig. 6

(Copyright © 2020 Elsevier)

Fig. 7

(Copyright © 2022 American Chemical Society))

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Funding

The authors are grateful for financial support of this work by the National Natural Science Foundation of China (No. 81803452), the Natural Science Foundation of Jiangsu Province (No. BK20211114), Natural Science Foundation in Colleges of Jiangsu Province (No. 21KJB350016), and the National Subject Cultivation Project of Jiangsu Vocational College of Medicine (No. 20204304).

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Authors and Affiliations

  1. School of Pharmacy, Jiangsu Vocational College of Medicine, Yancheng, 224005, China

    Qin Shi & Yanan Wang

  2. College of Pharmacy, California Northstate University, 9700 West Taron Drive, Elk Grove, California, 95757, USA

    Sakib M. Moinuddin, Xiaodong Feng & Fakhrul Ahsan

  3. East Bay Institute For Research & Education (EBIRE), 10535 Hospital Way, Mather, California, 95655, USA

    Sakib M. Moinuddin & Fakhrul Ahsan

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  1. Qin Shi
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Qin Shi: conceptualization, investigation, writing—original draft, writing—review and editing, funding acquisition; Yanan Wang: conceptualization, writing—original draft, writing—review and editing; Sakib M. Moinuddin: conceptualization, writing—review and editing; Xiaodong Feng: writing—review and editing; Fakhrul Ahsan: conceptualization, writing—original draft, writing—review and editing.

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Shi, Q., Wang, Y., Moinuddin, S.M. et al. Co-amorphous Drug Delivery Systems: a Review of Physical Stability, In Vitro and In Vivo Performance. AAPS PharmSciTech 23, 259 (2022). https://doi.org/10.1208/s12249-022-02421-7

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