Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo <i>Salmo salar</i> 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 <i>Caligus rogercresseyi</i>. EB has a low aqueous solubility, which affects its absorption in the intestine of <i...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-05-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/15/6/652 |
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| 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 |
| collection | DOAJ |
| 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 <i>Caligus rogercresseyi</i>. EB has a low aqueous solubility, which affects its absorption in the intestine of <i>Salmo</i> <i>salar</i>. Microparticles were produced by spray drying and ionic gelation, using Soluplus<sup>®</sup> (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<sup>−2</sup> mg/mL and 1.1<sup>−2</sup> 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<sup>®</sup> result in even less dissolution/permeation than free EB, so the technique cannot be used to improve the solubility of EB. |
| first_indexed | 2024-03-09T22:47:47Z |
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| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-09T22:47:47Z |
| publishDate | 2022-05-01 |
| publisher | MDPI AG |
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| series | Pharmaceuticals |
| spelling | doaj.art-c95a84da5fae4fb08dcf84485e44cad82023-11-23T18:26:21ZengMDPI AGPharmaceuticals1424-82472022-05-0115665210.3390/ph15060652Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo <i>Salmo salar</i> Intestine MembranesVictoria Molina0Carlos von Plessing1Alex Romero2Sergio Benavides3José Miguel Troncoso4José Ricardo Pérez-Correa5Wendy Franco6Department of Chemical and Bioprocess Engineering, Pontificia Universidad Católica de Chile, Santiago 6904411, ChileFaculty of Pharmacy, Universidad de Concepción, Concepción 4030000, ChileLaboratory of Immunology and Stress of Aquatic Organisms, Animal Pathology Institute, Universidad Austral de Chile, Valdivia 5090000, ChileResearch Center in Agri-Food and Applied Nutrition, Universidad Adventista de Chile, Chillán 3820572, ChileCargill Innovation Center, Cargill, Calbuco 5570130, ChileDepartment of Chemical and Bioprocess Engineering, Pontificia Universidad Católica de Chile, Santiago 6904411, ChileDepartment of Chemical and Bioprocess Engineering, Pontificia Universidad Católica de Chile, Santiago 6904411, ChileIn 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 <i>Caligus rogercresseyi</i>. EB has a low aqueous solubility, which affects its absorption in the intestine of <i>Salmo</i> <i>salar</i>. Microparticles were produced by spray drying and ionic gelation, using Soluplus<sup>®</sup> (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<sup>−2</sup> mg/mL and 1.1<sup>−2</sup> 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<sup>®</sup> result in even less dissolution/permeation than free EB, so the technique cannot be used to improve the solubility of EB.https://www.mdpi.com/1424-8247/15/6/652emamectin benzoatedissolution/permeationrelease kineticsapparent solubilityapparent permeabilityuptake |
| spellingShingle | 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 <i>Salmo salar</i> Intestine Membranes Pharmaceuticals emamectin benzoate dissolution/permeation release kinetics apparent solubility apparent permeability uptake |
| title | Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo <i>Salmo salar</i> Intestine Membranes |
| title_full | Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo <i>Salmo salar</i> Intestine Membranes |
| title_fullStr | Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo <i>Salmo salar</i> Intestine Membranes |
| title_full_unstemmed | Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo <i>Salmo salar</i> Intestine Membranes |
| title_short | Determination of the Dissolution/Permeation and Apparent Solubility for Microencapsulated Emamectin Benzoate Using In Vitro and Ex Vivo <i>Salmo salar</i> Intestine Membranes |
| title_sort | determination of the dissolution permeation and apparent solubility for microencapsulated emamectin benzoate using in vitro and ex vivo i salmo salar i intestine membranes |
| topic | emamectin benzoate dissolution/permeation release kinetics apparent solubility apparent permeability uptake |
| url | https://www.mdpi.com/1424-8247/15/6/652 |
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