Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo Salmo salar Intestine Membranes
In this work, two microencapsulation techniques were used to protect and improve the absorption of emamectin benzoate (EB), which is an antiparasitic drug used to control Caligus rogercresseyi . EB has a low aqueous solubility, which affects its absorption in the intestine of Salmo salar . Micropart...
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MDPI AG
2022
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ftdoajarticles:oai:doaj.org/article:c95a84da5fae4fb08dcf84485e44cad8 2023-05-15T18:09:50+02:00 Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo Salmo salar Intestine Membranes Victoria Molina Carlos von Plessing Alex Romero Sergio Benavides José Miguel Troncoso José Ricardo Pérez-Correa Wendy Franco 2022-05-01T00:00:00Z https://doi.org/10.3390/ph15060652 https://doaj.org/article/c95a84da5fae4fb08dcf84485e44cad8 EN eng MDPI AG https://www.mdpi.com/1424-8247/15/6/652 https://doaj.org/toc/1424-8247 doi:10.3390/ph15060652 1424-8247 https://doaj.org/article/c95a84da5fae4fb08dcf84485e44cad8 Pharmaceuticals, Vol 15, Iss 652, p 652 (2022) emamectin benzoate dissolution/permeation release kinetics apparent solubility apparent permeability uptake Medicine R Pharmacy and materia medica RS1-441 article 2022 ftdoajarticles https://doi.org/10.3390/ph15060652 2022-12-30T22:58:16Z In this work, two microencapsulation techniques were used to protect and improve the absorption of emamectin benzoate (EB), which is an antiparasitic drug used to control Caligus rogercresseyi . EB has a low aqueous solubility, which affects its absorption in the intestine of Salmo salar . Microparticles were produced by spray drying and ionic gelation, using Soluplus ® (EB–SOL) and sodium alginate (EB–ALG) as polymers, respectively. Studies were conducted on dissolution/permeation, apparent permeability (Papp), apparent solubility (Sapp), and absorption using synthetic and biological membranes. Based on these results, the amount of EB in the microparticles needed to achieve a therapeutic dose was estimated. The EB–ALG microparticles outperformed both EB–SOL and free EB, for all parameters analyzed. The results show values of 0.45 mg/mL (80.2%) for dissolution/permeation, a Papp of 6.2 mg/mL in RS–L, an absorption of 7.3% in RS, and a Sapp of 53.1% in EM medium. The EB–ALG microparticles decrease the therapeutic dose necessary to control the parasite, with values of 3.0 −2 mg/mL and 1.1 −2 mg/mL for EB in EM and RS, respectively. The Korsmeyer–Peppas kinetic model was the best model to fit the EB–ALG and EB–SOL dissolution/permeation experiments. In addition, some of our experimental results using synthetic membranes are similar to those obtained with biological membranes, which suggests that, for some parameters, it is possible to replace biological membranes with synthetic membranes. The encapsulation of EB by ionic gelation shows it is a promising formulation to increase the absorption of the poorly soluble drug. In contrast, the spray-dried microparticles produced using Soluplus ® result in even less dissolution/permeation than free EB, so the technique cannot be used to improve the solubility of EB. Article in Journal/Newspaper Salmo salar Directory of Open Access Journals: DOAJ Articles Pharmaceuticals 15 6 652 |
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op_collection_id |
ftdoajarticles |
language |
English |
topic |
emamectin benzoate dissolution/permeation release kinetics apparent solubility apparent permeability uptake Medicine R Pharmacy and materia medica RS1-441 |
spellingShingle |
emamectin benzoate dissolution/permeation release kinetics apparent solubility apparent permeability uptake Medicine R Pharmacy and materia medica RS1-441 Victoria Molina Carlos von Plessing Alex Romero Sergio Benavides José Miguel Troncoso José Ricardo Pérez-Correa Wendy Franco Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo Salmo salar Intestine Membranes |
topic_facet |
emamectin benzoate dissolution/permeation release kinetics apparent solubility apparent permeability uptake Medicine R Pharmacy and materia medica RS1-441 |
description |
In this work, two microencapsulation techniques were used to protect and improve the absorption of emamectin benzoate (EB), which is an antiparasitic drug used to control Caligus rogercresseyi . EB has a low aqueous solubility, which affects its absorption in the intestine of Salmo salar . Microparticles were produced by spray drying and ionic gelation, using Soluplus ® (EB–SOL) and sodium alginate (EB–ALG) as polymers, respectively. Studies were conducted on dissolution/permeation, apparent permeability (Papp), apparent solubility (Sapp), and absorption using synthetic and biological membranes. Based on these results, the amount of EB in the microparticles needed to achieve a therapeutic dose was estimated. The EB–ALG microparticles outperformed both EB–SOL and free EB, for all parameters analyzed. The results show values of 0.45 mg/mL (80.2%) for dissolution/permeation, a Papp of 6.2 mg/mL in RS–L, an absorption of 7.3% in RS, and a Sapp of 53.1% in EM medium. The EB–ALG microparticles decrease the therapeutic dose necessary to control the parasite, with values of 3.0 −2 mg/mL and 1.1 −2 mg/mL for EB in EM and RS, respectively. The Korsmeyer–Peppas kinetic model was the best model to fit the EB–ALG and EB–SOL dissolution/permeation experiments. In addition, some of our experimental results using synthetic membranes are similar to those obtained with biological membranes, which suggests that, for some parameters, it is possible to replace biological membranes with synthetic membranes. The encapsulation of EB by ionic gelation shows it is a promising formulation to increase the absorption of the poorly soluble drug. In contrast, the spray-dried microparticles produced using Soluplus ® result in even less dissolution/permeation than free EB, so the technique cannot be used to improve the solubility of EB. |
format |
Article in Journal/Newspaper |
author |
Victoria Molina Carlos von Plessing Alex Romero Sergio Benavides José Miguel Troncoso José Ricardo Pérez-Correa Wendy Franco |
author_facet |
Victoria Molina Carlos von Plessing Alex Romero Sergio Benavides José Miguel Troncoso José Ricardo Pérez-Correa Wendy Franco |
author_sort |
Victoria Molina |
title |
Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo Salmo salar Intestine Membranes |
title_short |
Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo Salmo salar Intestine Membranes |
title_full |
Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo Salmo salar Intestine Membranes |
title_fullStr |
Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo Salmo salar Intestine Membranes |
title_full_unstemmed |
Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo Salmo salar Intestine Membranes |
title_sort |
determination of the dissolution/permeation and apparent solubility for microencapsulated emamectin benzoate using in vitro and ex vivo salmo salar intestine membranes |
publisher |
MDPI AG |
publishDate |
2022 |
url |
https://doi.org/10.3390/ph15060652 https://doaj.org/article/c95a84da5fae4fb08dcf84485e44cad8 |
genre |
Salmo salar |
genre_facet |
Salmo salar |
op_source |
Pharmaceuticals, Vol 15, Iss 652, p 652 (2022) |
op_relation |
https://www.mdpi.com/1424-8247/15/6/652 https://doaj.org/toc/1424-8247 doi:10.3390/ph15060652 1424-8247 https://doaj.org/article/c95a84da5fae4fb08dcf84485e44cad8 |
op_doi |
https://doi.org/10.3390/ph15060652 |
container_title |
Pharmaceuticals |
container_volume |
15 |
container_issue |
6 |
container_start_page |
652 |
_version_ |
1766182510933311488 |