Tri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions

Ji-Jun Fu,1 Cheng-Cheng Liu2 1Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Science, The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, People’s Republic of China; 2Department of Medical On...

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Autores principales:	Fu JJ, Liu CC
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	micelles disintegrate stability in blood circulation solid dispersions recrystallization Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/74d3e870938e441b810cfa7d6ece6227
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spelling	oai:doaj.org-article:74d3e870938e441b810cfa7d6ece62272021-12-02T00:58:32ZTri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions1178-2013https://doaj.org/article/74d3e870938e441b810cfa7d6ece62272018-03-01T00:00:00Zhttps://www.dovepress.com/tri-block-polymer-with-interfacial-layer-formation-ability-and-its-use-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ji-Jun Fu,1 Cheng-Cheng Liu2 1Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Science, The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, People’s Republic of China; 2Department of Medical Oncology, The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, People’s Republic of China Background: Maintaining a supersaturated drug solution after the dissolution of the solid dispersions of water insoluble drugs continues to be a great challenge and is important to the oral bioavailability enhancement of hardly soluble drugs.Methods: Nimodipine solid dispersions were prepared by hot-melt extrusion and a special tri-block polymer was employed as a co-carrier. The solid dispersions were characterized by modulated differential scanning calorimetry, transmission electron microscopy, hydrogen-nuclear magnetic resonance and so on.Results: The tri-block polymer was able to inhibit the formation of drug crystals after dissolution of the solid dispersions. Due to the unique interfacial layer formation ability of the tri-block polymer, a special drug loading micelle which encapsulated the compound and the hydrophobic fragments of the copolymers appeared in the release media. The tri-block polymer was composed of a hydrophilic part forming the shell of micelles, a hydrophobic part shaping the core of micelles, and a special intermediate hydrophilicity part constructing the interfacial layer of micelles.Conclusion: The tri-block polymer was not only able to stabilize the supersaturated drug solution of solid dispersions to enhance the oral bioavailability of hardly soluble drugs, but is also a potential candidate to construct micelles for systemic administration, due to the good compatibility and organic solvents free micelle formation procedure. Keywords: micelles, disintegrate, stability in blood circulation, solid dispersions, recrystallizationFu JJLiu CCDove Medical Pressarticlemicellesdisintegratestability in blood circulationsolid dispersionsrecrystallizationMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 1611-1619 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	micelles disintegrate stability in blood circulation solid dispersions recrystallization Medicine (General) R5-920
spellingShingle	micelles disintegrate stability in blood circulation solid dispersions recrystallization Medicine (General) R5-920 Fu JJ Liu CC Tri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions
description	Ji-Jun Fu,1 Cheng-Cheng Liu2 1Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Science, The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, People’s Republic of China; 2Department of Medical Oncology, The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, People’s Republic of China Background: Maintaining a supersaturated drug solution after the dissolution of the solid dispersions of water insoluble drugs continues to be a great challenge and is important to the oral bioavailability enhancement of hardly soluble drugs.Methods: Nimodipine solid dispersions were prepared by hot-melt extrusion and a special tri-block polymer was employed as a co-carrier. The solid dispersions were characterized by modulated differential scanning calorimetry, transmission electron microscopy, hydrogen-nuclear magnetic resonance and so on.Results: The tri-block polymer was able to inhibit the formation of drug crystals after dissolution of the solid dispersions. Due to the unique interfacial layer formation ability of the tri-block polymer, a special drug loading micelle which encapsulated the compound and the hydrophobic fragments of the copolymers appeared in the release media. The tri-block polymer was composed of a hydrophilic part forming the shell of micelles, a hydrophobic part shaping the core of micelles, and a special intermediate hydrophilicity part constructing the interfacial layer of micelles.Conclusion: The tri-block polymer was not only able to stabilize the supersaturated drug solution of solid dispersions to enhance the oral bioavailability of hardly soluble drugs, but is also a potential candidate to construct micelles for systemic administration, due to the good compatibility and organic solvents free micelle formation procedure. Keywords: micelles, disintegrate, stability in blood circulation, solid dispersions, recrystallization
format	article
author	Fu JJ Liu CC
author_facet	Fu JJ Liu CC
author_sort	Fu JJ
title	Tri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions
title_short	Tri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions
title_full	Tri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions
title_fullStr	Tri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions
title_full_unstemmed	Tri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions
title_sort	tri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/74d3e870938e441b810cfa7d6ece6227
work_keys_str_mv	AT fujj triblockpolymerwithinterfaciallayerformationabilityanditsuseinmaintainingsupersaturateddrugsolutionafterdissolutionofsoliddispersions AT liucc triblockpolymerwithinterfaciallayerformationabilityanditsuseinmaintainingsupersaturateddrugsolutionafterdissolutionofsoliddispersions
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Tri-block polymer with interfacial layer formation ability and its use in maintaining supersaturated drug solution after dissolution of solid dispersions

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