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

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...

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Autores principales: Gan, Yanxiong, Baak, Jan P. A., Chen, Taijun, Ye, Hua, Liao, Wan, Lv, Huixia, Wen, Chuanbiao, Zheng, Shichao
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10005129/
https://www.ncbi.nlm.nih.gov/pubmed/36903470
http://dx.doi.org/10.3390/molecules28052212
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author Gan, Yanxiong
Baak, Jan P. A.
Chen, Taijun
Ye, Hua
Liao, Wan
Lv, Huixia
Wen, Chuanbiao
Zheng, Shichao
author_facet Gan, Yanxiong
Baak, Jan P. A.
Chen, Taijun
Ye, Hua
Liao, Wan
Lv, Huixia
Wen, Chuanbiao
Zheng, Shichao
author_sort Gan, Yanxiong
collection PubMed
description 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.
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spelling pubmed-100051292023-03-11 Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches Gan, Yanxiong Baak, Jan P. A. Chen, Taijun Ye, Hua Liao, Wan Lv, Huixia Wen, Chuanbiao Zheng, Shichao Molecules Review 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. MDPI 2023-02-27 /pmc/articles/PMC10005129/ /pubmed/36903470 http://dx.doi.org/10.3390/molecules28052212 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Gan, Yanxiong
Baak, Jan P. A.
Chen, Taijun
Ye, Hua
Liao, Wan
Lv, Huixia
Wen, Chuanbiao
Zheng, Shichao
Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches
title Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches
title_full Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches
title_fullStr Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches
title_full_unstemmed Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches
title_short Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches
title_sort supersaturation and precipitation applicated in drug delivery systems: development strategies and evaluation approaches
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10005129/
https://www.ncbi.nlm.nih.gov/pubmed/36903470
http://dx.doi.org/10.3390/molecules28052212
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