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Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation

BACKGROUND & OBJECTIVES: Low penetration efficiency and retention time are the main therapeutic concerns that make it difficult for most of the drugs to be delivered to the intraocular tissues. These challenging issues are often related to those drugs, which have low or poor solubility and low p...

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Autores principales: Kumar, Manish, Tiwari, Abhishek, Asdaq, Syed Mohammed Basheeruddin, Nair, Anroop B., Bhatt, Shailendra, Shinu, Pottathil, Al Mouslem, Abdulaziz K., Jacob, Shery, Alamri, Abdulhakeem S., Alsanie, Walaa F., Alhomrani, Majid, Tiwari, Varsha, Devi, Sheetal, Pathania, Ajay, Sreeharsha, Nagaraja
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8717166/
https://www.ncbi.nlm.nih.gov/pubmed/35002390
http://dx.doi.org/10.1016/j.sjbs.2021.11.006
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author Kumar, Manish
Tiwari, Abhishek
Asdaq, Syed Mohammed Basheeruddin
Nair, Anroop B.
Bhatt, Shailendra
Shinu, Pottathil
Al Mouslem, Abdulaziz K.
Jacob, Shery
Alamri, Abdulhakeem S.
Alsanie, Walaa F.
Alhomrani, Majid
Tiwari, Varsha
Devi, Sheetal
Pathania, Ajay
Sreeharsha, Nagaraja
author_facet Kumar, Manish
Tiwari, Abhishek
Asdaq, Syed Mohammed Basheeruddin
Nair, Anroop B.
Bhatt, Shailendra
Shinu, Pottathil
Al Mouslem, Abdulaziz K.
Jacob, Shery
Alamri, Abdulhakeem S.
Alsanie, Walaa F.
Alhomrani, Majid
Tiwari, Varsha
Devi, Sheetal
Pathania, Ajay
Sreeharsha, Nagaraja
author_sort Kumar, Manish
collection PubMed
description BACKGROUND & OBJECTIVES: Low penetration efficiency and retention time are the main therapeutic concerns that make it difficult for most of the drugs to be delivered to the intraocular tissues. These challenging issues are often related to those drugs, which have low or poor solubility and low permeability. The goal of this study was designed to develop nanostructured lipid carriers (NLCs) loaded with itraconazole (ITZ) with the objective of enhancing topical ocular permeation and thereby improving clinical efficacy. MATERIALS AND METHODS: ITZ-loaded NLCs were fabricated by a high-speed homogenization technique using surfactant (Poloxamer 407), and lipids (stearic acid and oleic acid). Optimization of formulations was performed by 3 level factorial design and the selected formulation (F6) was evaluated by differential scanning calorimetry and transmission electron microscopy. Antifungal activity was assessed by measuring the zone of inhibition and irritation potential using the HET-CAM test. RESULTS: The independent variables (lipid ratio-X(1) and percentage of emulsifier-X(2)) have a positive impact on percentage entrapment efficiency (Y(2)) and percentage release (Y(3)) but have a negative impact on particle size (Y(1)). Based on the better entrapment efficiency (94.65%), optimum particle size (150.67 nm), and percentage cumulative drug release (68.67%), batch F6 was selected for further evaluation. Electron microscopic images revealed that the prepared particles are spherical and have nano size. Antifungal studies demonstrated enhancement in the zone of inhibition by formulation F6 as compared to a commercial eye drop. The non-irritancy of optimized formulation (F6) was confirmed with a zero score. INTERPRETATION & CONCLUSION: In summary, the optimized NLCs seem to be a potent carrier for the effective delivery of itraconazole in ocular therapy.
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spelling pubmed-87171662022-01-06 Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation Kumar, Manish Tiwari, Abhishek Asdaq, Syed Mohammed Basheeruddin Nair, Anroop B. Bhatt, Shailendra Shinu, Pottathil Al Mouslem, Abdulaziz K. Jacob, Shery Alamri, Abdulhakeem S. Alsanie, Walaa F. Alhomrani, Majid Tiwari, Varsha Devi, Sheetal Pathania, Ajay Sreeharsha, Nagaraja Saudi J Biol Sci Original Article BACKGROUND & OBJECTIVES: Low penetration efficiency and retention time are the main therapeutic concerns that make it difficult for most of the drugs to be delivered to the intraocular tissues. These challenging issues are often related to those drugs, which have low or poor solubility and low permeability. The goal of this study was designed to develop nanostructured lipid carriers (NLCs) loaded with itraconazole (ITZ) with the objective of enhancing topical ocular permeation and thereby improving clinical efficacy. MATERIALS AND METHODS: ITZ-loaded NLCs were fabricated by a high-speed homogenization technique using surfactant (Poloxamer 407), and lipids (stearic acid and oleic acid). Optimization of formulations was performed by 3 level factorial design and the selected formulation (F6) was evaluated by differential scanning calorimetry and transmission electron microscopy. Antifungal activity was assessed by measuring the zone of inhibition and irritation potential using the HET-CAM test. RESULTS: The independent variables (lipid ratio-X(1) and percentage of emulsifier-X(2)) have a positive impact on percentage entrapment efficiency (Y(2)) and percentage release (Y(3)) but have a negative impact on particle size (Y(1)). Based on the better entrapment efficiency (94.65%), optimum particle size (150.67 nm), and percentage cumulative drug release (68.67%), batch F6 was selected for further evaluation. Electron microscopic images revealed that the prepared particles are spherical and have nano size. Antifungal studies demonstrated enhancement in the zone of inhibition by formulation F6 as compared to a commercial eye drop. The non-irritancy of optimized formulation (F6) was confirmed with a zero score. INTERPRETATION & CONCLUSION: In summary, the optimized NLCs seem to be a potent carrier for the effective delivery of itraconazole in ocular therapy. Elsevier 2022-01 2021-11-12 /pmc/articles/PMC8717166/ /pubmed/35002390 http://dx.doi.org/10.1016/j.sjbs.2021.11.006 Text en © 2021 The Author(s) https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Article
Kumar, Manish
Tiwari, Abhishek
Asdaq, Syed Mohammed Basheeruddin
Nair, Anroop B.
Bhatt, Shailendra
Shinu, Pottathil
Al Mouslem, Abdulaziz K.
Jacob, Shery
Alamri, Abdulhakeem S.
Alsanie, Walaa F.
Alhomrani, Majid
Tiwari, Varsha
Devi, Sheetal
Pathania, Ajay
Sreeharsha, Nagaraja
Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation
title Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation
title_full Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation
title_fullStr Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation
title_full_unstemmed Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation
title_short Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation
title_sort itraconazole loaded nano-structured lipid carrier for topical ocular delivery: optimization and evaluation
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8717166/
https://www.ncbi.nlm.nih.gov/pubmed/35002390
http://dx.doi.org/10.1016/j.sjbs.2021.11.006
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