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Facile methodology of nanoemulsion preparation using oily polymer for the delivery of poorly soluble drugs

Aqueous solubility of an active pharmaceutical ingredient (API) is a determining factor that has a direct impact on formulation strategies and overall bioavailability. Fabrication of nanoemulsions of poorly soluble drugs is one of the widely utilized approaches to overcome this problem. However, the...

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Autores principales: Wik, Johanna, Bansal, Kuldeep K., Assmuth, Tatu, Rosling, Ari, Rosenholm, Jessica M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer US 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7447668/
https://www.ncbi.nlm.nih.gov/pubmed/31858441
http://dx.doi.org/10.1007/s13346-019-00703-5
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author Wik, Johanna
Bansal, Kuldeep K.
Assmuth, Tatu
Rosling, Ari
Rosenholm, Jessica M.
author_facet Wik, Johanna
Bansal, Kuldeep K.
Assmuth, Tatu
Rosling, Ari
Rosenholm, Jessica M.
author_sort Wik, Johanna
collection PubMed
description Aqueous solubility of an active pharmaceutical ingredient (API) is a determining factor that has a direct impact on formulation strategies and overall bioavailability. Fabrication of nanoemulsions of poorly soluble drugs is one of the widely utilized approaches to overcome this problem. However, thermodynamic instability and tedious manufacturing processes of nanoemulsions limit their clinical translation. Therefore, this study was focused on circumventing the abovementioned hurdles by utilizing the polymer as an oil phase, instead of conventional oils. The nanoemulsion was prepared via a facile low-energy nanoprecipitation method using renewable poly(δ-decalactone) (PDL), as an oil phase and Pluronic F-68 as surfactant. The prepared nanoemulsions were characterized in terms of size, drug encapsulation efficiency, stability, and toxicity. Five different hydrophobic drugs were utilized to evaluate the drug delivery capability of the PDL nanoemulsion. The prepared nanoemulsions with sizes less than 200 nm were capable to enhance the aqueous solubility of the drugs by 3 to 10 times compared with the well-established Pluronic F-68 micelles. No phase separation or significant changes in size and drug content was observed with PDL nanoemulsions after high-speed centrifugation and 3 months of storage at two different temperatures (20 °C and 50 °C). PDL nanoemulsions were found to be non-heamolytic up to concentrations of 1 mg/mL, and the cell cytotoxicity studies on MDA-MB-231 and MEF cells suggest a concentration and time-dependent toxicity, where the PDL polymer itself induced no cytotoxicity. The results from this study clearly indicate that the PDL polymer has a tremendous potential to be utilized as an oil phase to prepare stable nanoemulsions via a facile methodology, ultimately favouring clinical translations. [Figure: see text] ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (10.1007/s13346-019-00703-5) contains supplementary material, which is available to authorized users.
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spelling pubmed-74476682020-09-02 Facile methodology of nanoemulsion preparation using oily polymer for the delivery of poorly soluble drugs Wik, Johanna Bansal, Kuldeep K. Assmuth, Tatu Rosling, Ari Rosenholm, Jessica M. Drug Deliv Transl Res Original Article Aqueous solubility of an active pharmaceutical ingredient (API) is a determining factor that has a direct impact on formulation strategies and overall bioavailability. Fabrication of nanoemulsions of poorly soluble drugs is one of the widely utilized approaches to overcome this problem. However, thermodynamic instability and tedious manufacturing processes of nanoemulsions limit their clinical translation. Therefore, this study was focused on circumventing the abovementioned hurdles by utilizing the polymer as an oil phase, instead of conventional oils. The nanoemulsion was prepared via a facile low-energy nanoprecipitation method using renewable poly(δ-decalactone) (PDL), as an oil phase and Pluronic F-68 as surfactant. The prepared nanoemulsions were characterized in terms of size, drug encapsulation efficiency, stability, and toxicity. Five different hydrophobic drugs were utilized to evaluate the drug delivery capability of the PDL nanoemulsion. The prepared nanoemulsions with sizes less than 200 nm were capable to enhance the aqueous solubility of the drugs by 3 to 10 times compared with the well-established Pluronic F-68 micelles. No phase separation or significant changes in size and drug content was observed with PDL nanoemulsions after high-speed centrifugation and 3 months of storage at two different temperatures (20 °C and 50 °C). PDL nanoemulsions were found to be non-heamolytic up to concentrations of 1 mg/mL, and the cell cytotoxicity studies on MDA-MB-231 and MEF cells suggest a concentration and time-dependent toxicity, where the PDL polymer itself induced no cytotoxicity. The results from this study clearly indicate that the PDL polymer has a tremendous potential to be utilized as an oil phase to prepare stable nanoemulsions via a facile methodology, ultimately favouring clinical translations. [Figure: see text] ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (10.1007/s13346-019-00703-5) contains supplementary material, which is available to authorized users. Springer US 2019-12-19 2020 /pmc/articles/PMC7447668/ /pubmed/31858441 http://dx.doi.org/10.1007/s13346-019-00703-5 Text en © The Author(s) 2019 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/.
spellingShingle Original Article
Wik, Johanna
Bansal, Kuldeep K.
Assmuth, Tatu
Rosling, Ari
Rosenholm, Jessica M.
Facile methodology of nanoemulsion preparation using oily polymer for the delivery of poorly soluble drugs
title Facile methodology of nanoemulsion preparation using oily polymer for the delivery of poorly soluble drugs
title_full Facile methodology of nanoemulsion preparation using oily polymer for the delivery of poorly soluble drugs
title_fullStr Facile methodology of nanoemulsion preparation using oily polymer for the delivery of poorly soluble drugs
title_full_unstemmed Facile methodology of nanoemulsion preparation using oily polymer for the delivery of poorly soluble drugs
title_short Facile methodology of nanoemulsion preparation using oily polymer for the delivery of poorly soluble drugs
title_sort facile methodology of nanoemulsion preparation using oily polymer for the delivery of poorly soluble drugs
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7447668/
https://www.ncbi.nlm.nih.gov/pubmed/31858441
http://dx.doi.org/10.1007/s13346-019-00703-5
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