Solubilisation of salicylate in F127 micelles: Effect of pH and temperature on morphology and interactions with cyclodextrin

Margarita Valero; Wenjing Hu; Judith E. Houston; Cécile A. Dreiss

doi:10.1016/j.molliq.2020.114892

Solubilisation of salicylate in F127 micelles: Effect of pH and temperature on morphology and interactions with cyclodextrin

Margarita Valero, Wenjing Hu, Judith E. Houston, Cécile A. Dreiss

Institute of Pharmaceutical Science

Research output: Contribution to journal › Article › peer-review

11 Citations (Scopus)

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Abstract

The present work examines the behavior of salicylic acid (SAL)-loaded F127 micelles as drug nanocarriers for controlled release by means of interaction with 2,6-dimethyl-β-cyclodextrin (DIMEB) in the intestine at basic pH = 7–8, both important excipients, of pharmaceutical formulations.

The results show that acidic pH (pH = 1) strongly increases the partitioning of SAL in F127 micelles compared to neutral pH, due to the drug being in its molecular form. Fluorescence spectroscopy and small-angle neutron scattering show that free and SAL-loaded F127 micelles transition to cylindrical micelles at pH = 1 and high temperatures (37 °C). Micelles loaded with SAL are disrupted by DIMEB to a higher extent than at pH = 7 at physiological temperature. This study reveals that F127 could be a valuable nanocarrier for intestine controlled release of SAL. Taken together, our results highlight the importance of water in the structure of the micelles and their interaction with DIMEB, and bring precious insights into the mechanisms that regulate drug loading and release in complex formulations.

Original language	English
Article number	114892
Journal	JOURNAL OF MOLECULAR LIQUIDS
Volume	322
Early online date	3 Dec 2020
DOIs	https://doi.org/10.1016/j.molliq.2020.114892
Publication status	Published - 15 Jan 2021

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Solubilisation of salicylate in_VALERO_Acc25Nov2020Epub3Dec2020_GREEN AAMAccepted author manuscript, 836 KB

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title = "Solubilisation of salicylate in F127 micelles: Effect of pH and temperature on morphology and interactions with cyclodextrin",

abstract = "The present work examines the behavior of salicylic acid (SAL)-loaded F127 micelles as drug nanocarriers for controlled release by means of interaction with 2,6-dimethyl-β-cyclodextrin (DIMEB) in the intestine at basic pH = 7–8, both important excipients, of pharmaceutical formulations.The results show that acidic pH (pH = 1) strongly increases the partitioning of SAL in F127 micelles compared to neutral pH, due to the drug being in its molecular form. Fluorescence spectroscopy and small-angle neutron scattering show that free and SAL-loaded F127 micelles transition to cylindrical micelles at pH = 1 and high temperatures (37 °C). Micelles loaded with SAL are disrupted by DIMEB to a higher extent than at pH = 7 at physiological temperature. This study reveals that F127 could be a valuable nanocarrier for intestine controlled release of SAL. Taken together, our results highlight the importance of water in the structure of the micelles and their interaction with DIMEB, and bring precious insights into the mechanisms that regulate drug loading and release in complex formulations.",

author = "Margarita Valero and Wenjing Hu and Houston, {Judith E.} and Dreiss, {C{\'e}cile A.}",

note = "Funding Information: This work is based upon experiments performed at the KWS-2 instrument operated by JCNS at the Heinz Maier-Leibnitz Zentrum (MLZ), Garching, Germany. This work benefited from the use of the SasView application, originally developed under NSF Award DMR- 0520547. SasView also contains code developed with funding from the EU Horizon 2020 programme under the SINE2020 project. Grant No 654000. Funding Information: This work is based upon experiments performed at the KWS-2 instrument operated by JCNS at the Heinz Maier-Leibnitz Zentrum (MLZ) , Garching, Germany. This work benefited from the use of the SasView application, originally developed under NSF Award DMR- 0520547 . SasView also contains code developed with funding from the EU Horizon 2020 programme under the SINE2020 project . Grant No 654000 . Publisher Copyright: {\textcopyright} 2020 Copyright: Copyright 2020 Elsevier B.V., All rights reserved.",

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AU - Dreiss, Cécile A.

N1 - Funding Information: This work is based upon experiments performed at the KWS-2 instrument operated by JCNS at the Heinz Maier-Leibnitz Zentrum (MLZ), Garching, Germany. This work benefited from the use of the SasView application, originally developed under NSF Award DMR- 0520547. SasView also contains code developed with funding from the EU Horizon 2020 programme under the SINE2020 project. Grant No 654000. Funding Information: This work is based upon experiments performed at the KWS-2 instrument operated by JCNS at the Heinz Maier-Leibnitz Zentrum (MLZ) , Garching, Germany. This work benefited from the use of the SasView application, originally developed under NSF Award DMR- 0520547 . SasView also contains code developed with funding from the EU Horizon 2020 programme under the SINE2020 project . Grant No 654000 . Publisher Copyright: © 2020 Copyright: Copyright 2020 Elsevier B.V., All rights reserved.

PY - 2021/1/15

Y1 - 2021/1/15

N2 - The present work examines the behavior of salicylic acid (SAL)-loaded F127 micelles as drug nanocarriers for controlled release by means of interaction with 2,6-dimethyl-β-cyclodextrin (DIMEB) in the intestine at basic pH = 7–8, both important excipients, of pharmaceutical formulations.The results show that acidic pH (pH = 1) strongly increases the partitioning of SAL in F127 micelles compared to neutral pH, due to the drug being in its molecular form. Fluorescence spectroscopy and small-angle neutron scattering show that free and SAL-loaded F127 micelles transition to cylindrical micelles at pH = 1 and high temperatures (37 °C). Micelles loaded with SAL are disrupted by DIMEB to a higher extent than at pH = 7 at physiological temperature. This study reveals that F127 could be a valuable nanocarrier for intestine controlled release of SAL. Taken together, our results highlight the importance of water in the structure of the micelles and their interaction with DIMEB, and bring precious insights into the mechanisms that regulate drug loading and release in complex formulations.

AB - The present work examines the behavior of salicylic acid (SAL)-loaded F127 micelles as drug nanocarriers for controlled release by means of interaction with 2,6-dimethyl-β-cyclodextrin (DIMEB) in the intestine at basic pH = 7–8, both important excipients, of pharmaceutical formulations.The results show that acidic pH (pH = 1) strongly increases the partitioning of SAL in F127 micelles compared to neutral pH, due to the drug being in its molecular form. Fluorescence spectroscopy and small-angle neutron scattering show that free and SAL-loaded F127 micelles transition to cylindrical micelles at pH = 1 and high temperatures (37 °C). Micelles loaded with SAL are disrupted by DIMEB to a higher extent than at pH = 7 at physiological temperature. This study reveals that F127 could be a valuable nanocarrier for intestine controlled release of SAL. Taken together, our results highlight the importance of water in the structure of the micelles and their interaction with DIMEB, and bring precious insights into the mechanisms that regulate drug loading and release in complex formulations.

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Solubilisation of salicylate in F127 micelles: Effect of pH and temperature on morphology and interactions with cyclodextrin

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