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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| Format: | Article |
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MDPI AG
2022-04-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/14/7/1489 |
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| author | Barkat Ali Khan Maryam Waheed Khaled M. Hosny Waleed Y. Rizg Samar S. Murshid Majed Alharbi Muhammad Khalid Khan |
| author_facet | Barkat Ali Khan Maryam Waheed Khaled M. Hosny Waleed Y. Rizg Samar S. Murshid Majed Alharbi Muhammad Khalid Khan |
| author_sort | Barkat Ali Khan |
| collection | DOAJ |
| 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 (<i>p</i> < 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. |
| first_indexed | 2024-03-09T11:29:16Z |
| format | Article |
| id | doaj.art-28d3faf0445648bd9d005593f8807d73 |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-09T11:29:16Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-28d3faf0445648bd9d005593f8807d732023-11-30T23:55:10ZengMDPI AGPolymers2073-43602022-04-01147148910.3390/polym14071489Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement ApproachBarkat Ali Khan0Maryam Waheed1Khaled M. Hosny2Waleed Y. Rizg3Samar S. Murshid4Majed Alharbi5Muhammad Khalid Khan6Drug Delivery and Cosmetic Lab (DDCL), Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanDrug Delivery and Cosmetic Lab (DDCL), Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDrug Delivery and Cosmetic Lab (DDCL), Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanKojic 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 (<i>p</i> < 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.https://www.mdpi.com/2073-4360/14/7/1489sustainability of natural resourcesnanocrystalskojic acidsolubility enhancementtop-down technique |
| spellingShingle | Barkat Ali Khan Maryam Waheed Khaled M. Hosny Waleed Y. Rizg Samar S. Murshid Majed Alharbi Muhammad Khalid Khan Formulation and Characterization of Carbopol-934 Based Kojic Acid-Loaded Smart Nanocrystals: A Solubility Enhancement Approach Polymers sustainability of natural resources nanocrystals kojic acid solubility enhancement top-down technique |
| 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 | sustainability of natural resources nanocrystals kojic acid solubility enhancement top-down technique |
| url | https://www.mdpi.com/2073-4360/14/7/1489 |
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