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Formulation of Self-Nanoemulsifying Drug Delivery System of Cephalexin: Physiochemical Characterization and Antibacterial Evaluation
A cephalexin (CEP) self-nanoemulsifying drug delivery system (SNEDDS) was developed in this study to improve the drug’s oral administration. The CEP-SNEDDS was made utilizing an aqueous titration method employing Lauroglycol 90, Poloxamer 188, and Transcutol-HP. Box-Behnken design (BBD) with three f...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8915057/ https://www.ncbi.nlm.nih.gov/pubmed/35267877 http://dx.doi.org/10.3390/polym14051055 |
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author | Zafar, Ameeduzzafar Yasir, Mohd Alruwaili, Nabil K. Imam, Syed Sarim Alsaidan, Omar Awad Alshehri, Sultan Ghoneim, Mohammed M. Alquraini, Ali Rawaf, Alenazy Ansari, Mohammad Javed Sara, Udai Vir Singh |
author_facet | Zafar, Ameeduzzafar Yasir, Mohd Alruwaili, Nabil K. Imam, Syed Sarim Alsaidan, Omar Awad Alshehri, Sultan Ghoneim, Mohammed M. Alquraini, Ali Rawaf, Alenazy Ansari, Mohammad Javed Sara, Udai Vir Singh |
author_sort | Zafar, Ameeduzzafar |
collection | PubMed |
description | A cephalexin (CEP) self-nanoemulsifying drug delivery system (SNEDDS) was developed in this study to improve the drug’s oral administration. The CEP-SNEDDS was made utilizing an aqueous titration method employing Lauroglycol 90, Poloxamer 188, and Transcutol-HP. Box-Behnken design (BBD) with three factors at three levels was used for optimization, and their impacts on globule size (nm), transmittance (percent), and emulsification time (s) were assessed. The optimized formulation (Opt-F3) was further tested for zeta potential, refractive index, percent transmittance, thermodynamic stability, in-vitro release, ex vivo permeability, antibacterial activity, and bioavailability. The chosen formulation (Opt-F3) had a globule size of 87.25 ± 3.16 nm, PDI of 0.25, zeta potential of −24.37 mV, self-emulsification duration of 52 ± 1.7 s, and percentage transmittance of 99.13 ± 1.5%, viscosity of 96.26 ± 2.72 cp, and refractive index of 1.29 ± 0.1. It showed a sustained release profile (94.28 ± 5.92 percent in 24 h). The Opt-F3 formulation had 3.95 times the permeability of CEP-dispersion. In comparison to CEP-dispersion, it also demonstrated greater antibacterial efficacy against tested Gram-positive and Gram-negative pathogens. The oral bioavailability of Opt-F3 is 3.48 times higher than that of CEP-dispersion, according to an in-vivo investigation. It has been determined that the prepared CEP-SNEDDS may be an advantageous carrier for CEP delivery. |
format | Online Article Text |
id | pubmed-8915057 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-89150572022-03-12 Formulation of Self-Nanoemulsifying Drug Delivery System of Cephalexin: Physiochemical Characterization and Antibacterial Evaluation Zafar, Ameeduzzafar Yasir, Mohd Alruwaili, Nabil K. Imam, Syed Sarim Alsaidan, Omar Awad Alshehri, Sultan Ghoneim, Mohammed M. Alquraini, Ali Rawaf, Alenazy Ansari, Mohammad Javed Sara, Udai Vir Singh Polymers (Basel) Article A cephalexin (CEP) self-nanoemulsifying drug delivery system (SNEDDS) was developed in this study to improve the drug’s oral administration. The CEP-SNEDDS was made utilizing an aqueous titration method employing Lauroglycol 90, Poloxamer 188, and Transcutol-HP. Box-Behnken design (BBD) with three factors at three levels was used for optimization, and their impacts on globule size (nm), transmittance (percent), and emulsification time (s) were assessed. The optimized formulation (Opt-F3) was further tested for zeta potential, refractive index, percent transmittance, thermodynamic stability, in-vitro release, ex vivo permeability, antibacterial activity, and bioavailability. The chosen formulation (Opt-F3) had a globule size of 87.25 ± 3.16 nm, PDI of 0.25, zeta potential of −24.37 mV, self-emulsification duration of 52 ± 1.7 s, and percentage transmittance of 99.13 ± 1.5%, viscosity of 96.26 ± 2.72 cp, and refractive index of 1.29 ± 0.1. It showed a sustained release profile (94.28 ± 5.92 percent in 24 h). The Opt-F3 formulation had 3.95 times the permeability of CEP-dispersion. In comparison to CEP-dispersion, it also demonstrated greater antibacterial efficacy against tested Gram-positive and Gram-negative pathogens. The oral bioavailability of Opt-F3 is 3.48 times higher than that of CEP-dispersion, according to an in-vivo investigation. It has been determined that the prepared CEP-SNEDDS may be an advantageous carrier for CEP delivery. MDPI 2022-03-07 /pmc/articles/PMC8915057/ /pubmed/35267877 http://dx.doi.org/10.3390/polym14051055 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Zafar, Ameeduzzafar Yasir, Mohd Alruwaili, Nabil K. Imam, Syed Sarim Alsaidan, Omar Awad Alshehri, Sultan Ghoneim, Mohammed M. Alquraini, Ali Rawaf, Alenazy Ansari, Mohammad Javed Sara, Udai Vir Singh Formulation of Self-Nanoemulsifying Drug Delivery System of Cephalexin: Physiochemical Characterization and Antibacterial Evaluation |
title | Formulation of Self-Nanoemulsifying Drug Delivery System of Cephalexin: Physiochemical Characterization and Antibacterial Evaluation |
title_full | Formulation of Self-Nanoemulsifying Drug Delivery System of Cephalexin: Physiochemical Characterization and Antibacterial Evaluation |
title_fullStr | Formulation of Self-Nanoemulsifying Drug Delivery System of Cephalexin: Physiochemical Characterization and Antibacterial Evaluation |
title_full_unstemmed | Formulation of Self-Nanoemulsifying Drug Delivery System of Cephalexin: Physiochemical Characterization and Antibacterial Evaluation |
title_short | Formulation of Self-Nanoemulsifying Drug Delivery System of Cephalexin: Physiochemical Characterization and Antibacterial Evaluation |
title_sort | formulation of self-nanoemulsifying drug delivery system of cephalexin: physiochemical characterization and antibacterial evaluation |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8915057/ https://www.ncbi.nlm.nih.gov/pubmed/35267877 http://dx.doi.org/10.3390/polym14051055 |
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