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Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach

Kojic acid (KA) is a BCS class II drug having low solubility and high permeability. This study was designed to enhance the aqueous solubility of KA, as well as its dissolution rate and, in turn, bioavailability, by formulating its smart nanocrystals. Nanocrystals of pure KA were formulated by the to...

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Autores principales: Khan, Barkat Ali, Waheed, Maryam, Hosny, Khaled M., Rizg, Waleed Y., Murshid, Samar S., Alharbi, Majed, Khan, Muhammad Khalid
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9003442/
https://www.ncbi.nlm.nih.gov/pubmed/35406362
http://dx.doi.org/10.3390/polym14071489
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author Khan, Barkat Ali
Waheed, Maryam
Hosny, Khaled M.
Rizg, Waleed Y.
Murshid, Samar S.
Alharbi, Majed
Khan, Muhammad Khalid
author_facet Khan, Barkat Ali
Waheed, Maryam
Hosny, Khaled M.
Rizg, Waleed Y.
Murshid, Samar S.
Alharbi, Majed
Khan, Muhammad Khalid
author_sort Khan, Barkat Ali
collection PubMed
description Kojic acid (KA) is a BCS class II drug having low solubility and high permeability. This study was designed to enhance the aqueous solubility of KA, as well as its dissolution rate and, in turn, bioavailability, by formulating its smart nanocrystals. Nanocrystals of pure KA were formulated by the top-down method under high-pressure homogenization followed by freeze drying. The nanocrystals were evaluated for stability and other physical characteristics, including zeta sizer analysis, DSC, surface morphology, XRD, drug content, solubility, FTIR and in vitro drug release. The KA nanocrystals were found to be stable when kept at exaggerated conditions. The particle size of the nanocrystals was 137.5 ± 1.7, 150 ± 2.8, and 110 ± 3.0 nm for the F1, F2 and F3 formulations, respectively. There was negative zeta potential for all the formulations. The dispersity index was 0.45 ± 0.2, 0.36 ± 0.4 and 0.41 ± 1.5 for the F1, F2 and F3, respectively. The DSC studies showed that there was no interaction between the KA and the excipients of the nanocrystals. The morphological studies confirmed the presence of rough crystalline surfaces on the nanosized particles. XRD studies showed the successful preparation of nanocrystals. The drug content was in the official range of 90 ± 10%. The solubility of KA was significantly (p < 0.05) enhanced in the formulations of its nanocrystals as compared with pure KA powder. The ATR-FTIR studies revealed the presence of functional groups in both KA and KA-loaded nanocrystals, and no interaction was found between them. The nanocrystals released 83.93 ± 1.22% of KA in 24 h. The study concluded that the nanocrystals were successfully formulated using the top-down method followed by high-pressure homogenization. The solubility, as well as the dissolution, of the KA was enhanced, and this could improve the therapeutic effects of KA.
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spelling pubmed-90034422022-04-13 Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach Khan, Barkat Ali Waheed, Maryam Hosny, Khaled M. Rizg, Waleed Y. Murshid, Samar S. Alharbi, Majed Khan, Muhammad Khalid Polymers (Basel) Article Kojic acid (KA) is a BCS class II drug having low solubility and high permeability. This study was designed to enhance the aqueous solubility of KA, as well as its dissolution rate and, in turn, bioavailability, by formulating its smart nanocrystals. Nanocrystals of pure KA were formulated by the top-down method under high-pressure homogenization followed by freeze drying. The nanocrystals were evaluated for stability and other physical characteristics, including zeta sizer analysis, DSC, surface morphology, XRD, drug content, solubility, FTIR and in vitro drug release. The KA nanocrystals were found to be stable when kept at exaggerated conditions. The particle size of the nanocrystals was 137.5 ± 1.7, 150 ± 2.8, and 110 ± 3.0 nm for the F1, F2 and F3 formulations, respectively. There was negative zeta potential for all the formulations. The dispersity index was 0.45 ± 0.2, 0.36 ± 0.4 and 0.41 ± 1.5 for the F1, F2 and F3, respectively. The DSC studies showed that there was no interaction between the KA and the excipients of the nanocrystals. The morphological studies confirmed the presence of rough crystalline surfaces on the nanosized particles. XRD studies showed the successful preparation of nanocrystals. The drug content was in the official range of 90 ± 10%. The solubility of KA was significantly (p < 0.05) enhanced in the formulations of its nanocrystals as compared with pure KA powder. The ATR-FTIR studies revealed the presence of functional groups in both KA and KA-loaded nanocrystals, and no interaction was found between them. The nanocrystals released 83.93 ± 1.22% of KA in 24 h. The study concluded that the nanocrystals were successfully formulated using the top-down method followed by high-pressure homogenization. The solubility, as well as the dissolution, of the KA was enhanced, and this could improve the therapeutic effects of KA. MDPI 2022-04-06 /pmc/articles/PMC9003442/ /pubmed/35406362 http://dx.doi.org/10.3390/polym14071489 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
Khan, Barkat Ali
Waheed, Maryam
Hosny, Khaled M.
Rizg, Waleed Y.
Murshid, Samar S.
Alharbi, Majed
Khan, Muhammad Khalid
Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach
title Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach
title_full Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach
title_fullStr Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach
title_full_unstemmed Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach
title_short Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach
title_sort formulation and characterization of carbopol-934 based kojic acid-loaded smart nanocrystals: a solubility enhancement approach
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9003442/
https://www.ncbi.nlm.nih.gov/pubmed/35406362
http://dx.doi.org/10.3390/polym14071489
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