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Review

Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches

by
Yanxiong Gan
1,
Jan P. A. Baak
2,3,
Taijun Chen
1,
Hua Ye
1,
Wan Liao
4,
Huixia Lv
5,
Chuanbiao Wen
1,* and
Shichao Zheng
1,*
1
School of Intelligent Medicine, Chengdu University of Traditional Chinese Medicine, Liutai Avenue 1166, Chengdu 611137, China
2
Dr. Med. Jan Baak AS, Risavegen 66, N-4056 Tananger, Norway
3
Department of Pathology, Section of Quantitative Molecular Pathology, Stavanger University Hospital, Gerd Ragna Bloch Thorsens Gate 8, N-4011 Stavanger, Norway
4
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Liutai Avenue 1166, Chengdu 611137, China
5
School of Pharmacy, China Pharmaceutical University, Longmian Avenue 639, Nanjing 211198, China
*
Authors to whom correspondence should be addressed.
Molecules 2023, 28(5), 2212; https://doi.org/10.3390/molecules28052212
Submission received: 30 December 2022 / Revised: 20 February 2023 / Accepted: 24 February 2023 / Published: 27 February 2023
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Abstract

Supersaturation is a promising strategy to improve gastrointestinal absorption of poorly water-soluble drugs. Supersaturation is a metastable state and therefore dissolved drugs often quickly precipitate again. Precipitation inhibitors can prolong the metastable state. Supersaturating drug delivery systems (SDDS) are commonly formulated with precipitation inhibitors, hence the supersaturation is effectively prolonged for absorption, leading to improved bioavailability. This review summarizes the theory of and systemic insight into supersaturation, with the emphasis on biopharmaceutical aspects. Supersaturation research has developed from the generation of supersaturation (pH-shift, prodrug and SDDS) and the inhibition of precipitation (the mechanism of precipitation, the character of precipitation inhibitors and screening precipitation inhibitors). Then, the evaluation approaches to SDDS are discussed, including in vitro, in vivo and in silico studies and in vitro–in vivo correlations. In vitro aspects involve biorelevant medium, biomimetic apparatus and characterization instruments; in vivo aspects involve oral absorption, intestinal perfusion and intestinal content aspiration and in silico aspects involve molecular dynamics simulation and pharmacokinetic simulation. More physiological data of in vitro studies should be taken into account to simulate the in vivo environment. The supersaturation theory should be further completed, especially with regard to physiological conditions.
Keywords: supersaturation; precipitation inhibitors; dissolution; bioavailability; modeling supersaturation; precipitation inhibitors; dissolution; bioavailability; modeling

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MDPI and ACS Style

Gan, Y.; Baak, J.P.A.; Chen, T.; Ye, H.; Liao, W.; Lv, H.; Wen, C.; Zheng, S. Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches. Molecules 2023, 28, 2212. https://doi.org/10.3390/molecules28052212

AMA Style

Gan Y, Baak JPA, Chen T, Ye H, Liao W, Lv H, Wen C, Zheng S. Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches. Molecules. 2023; 28(5):2212. https://doi.org/10.3390/molecules28052212

Chicago/Turabian Style

Gan, Yanxiong, Jan P. A. Baak, Taijun Chen, Hua Ye, Wan Liao, Huixia Lv, Chuanbiao Wen, and Shichao Zheng. 2023. "Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches" Molecules 28, no. 5: 2212. https://doi.org/10.3390/molecules28052212

APA Style

Gan, Y., Baak, J. P. A., Chen, T., Ye, H., Liao, W., Lv, H., Wen, C., & Zheng, S. (2023). Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches. Molecules, 28(5), 2212. https://doi.org/10.3390/molecules28052212

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