Carboxymethyl starch as a solid dispersion carrier to enhance the dissolution and bioavailability of piperine and 18β-glycyrrhetinic acid
OBJECTIVE: To investigate the applicability of carboxymethyl starch (CMS) as a carrier to prepare solid dispersions (SDs) of piperine (PIP) and 18β-glycyrrhetinic acid (β-GA) (PIP-CMS and β-GA-CMS SDs) and to explore the influence of drug properties on carrier selection.
SIGNIFICANCE: The low oral bioavailability of natural therapeutic molecules, including PIP and β-GA, severely restricts their pharmaceutical applications. Moreover, CMS, a natural polymer, is rarely reported as a carrier for SDs.
METHODS: PIP-CMS and β-GA-CMS SDs were prepared using the solvent evaporation method. Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Fourier transform infrared (FT-IR) spectroscopy, and scanning electron microscopy (SEM) were used for formulation characterization. Additionally, drug release characteristics were investigated.
RESULTS: In vitro dissolution studies showed that the dissolutions of PIP-CMS and β-GA-CMS SDs were 1.90-2.04 and 1.97-2.22 times higher than pure PIP and β-GA, respectively, at a drug:polymer ratio of 1:6. DSC, XRPD, FT-IR, and SEM analyses confirmed the formation of SDs in their amorphous states. Significant improvements in Cmax and AUC0-24 h of PIP-CMS and β-GA-CMS SDs (17.51 ± 8.15 μg/mL and 210.28 ± 117.13 μg·h/mL, respectively) and (32.17 ± 9.45 μg/mL and 165.36 ± 38.75 μg·h/mL, respectively) were observed in the pharmacokinetic study. Compared with weakly acidic β-GA, loading weakly basic PIP seemed to have a profound effect on stability through intermolecular forces.
CONCLUSIONS: Our findings showed CMS could be a promising carrier for SDs, and loading weakly basic drug may be more suitable, especially in binary SDs system.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:49 |
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| Enthalten in: |
Drug development and industrial pharmacy - 49(2023), 1 vom: 17. Jan., Seite 30-41 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Shi, Fanli [VerfasserIn] |
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| Links: |
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| Themen: |
1449-05-4 |
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| Anmerkungen: |
Date Completed 22.03.2023 Date Revised 22.03.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1080/03639045.2023.2182120 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM353097438 |
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| 100 | 1 | |a Shi, Fanli |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Carboxymethyl starch as a solid dispersion carrier to enhance the dissolution and bioavailability of piperine and 18β-glycyrrhetinic acid |
| 264 | 1 | |c 2023 | |
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| 500 | |a Date Completed 22.03.2023 | ||
| 500 | |a Date Revised 22.03.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a OBJECTIVE: To investigate the applicability of carboxymethyl starch (CMS) as a carrier to prepare solid dispersions (SDs) of piperine (PIP) and 18β-glycyrrhetinic acid (β-GA) (PIP-CMS and β-GA-CMS SDs) and to explore the influence of drug properties on carrier selection | ||
| 520 | |a SIGNIFICANCE: The low oral bioavailability of natural therapeutic molecules, including PIP and β-GA, severely restricts their pharmaceutical applications. Moreover, CMS, a natural polymer, is rarely reported as a carrier for SDs | ||
| 520 | |a METHODS: PIP-CMS and β-GA-CMS SDs were prepared using the solvent evaporation method. Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Fourier transform infrared (FT-IR) spectroscopy, and scanning electron microscopy (SEM) were used for formulation characterization. Additionally, drug release characteristics were investigated | ||
| 520 | |a RESULTS: In vitro dissolution studies showed that the dissolutions of PIP-CMS and β-GA-CMS SDs were 1.90-2.04 and 1.97-2.22 times higher than pure PIP and β-GA, respectively, at a drug:polymer ratio of 1:6. DSC, XRPD, FT-IR, and SEM analyses confirmed the formation of SDs in their amorphous states. Significant improvements in Cmax and AUC0-24 h of PIP-CMS and β-GA-CMS SDs (17.51 ± 8.15 μg/mL and 210.28 ± 117.13 μg·h/mL, respectively) and (32.17 ± 9.45 μg/mL and 165.36 ± 38.75 μg·h/mL, respectively) were observed in the pharmacokinetic study. Compared with weakly acidic β-GA, loading weakly basic PIP seemed to have a profound effect on stability through intermolecular forces | ||
| 520 | |a CONCLUSIONS: Our findings showed CMS could be a promising carrier for SDs, and loading weakly basic drug may be more suitable, especially in binary SDs system | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a 18β-glycyrrhetinic acid | |
| 650 | 4 | |a Piperine | |
| 650 | 4 | |a bioavailability | |
| 650 | 4 | |a carboxymethyl starch | |
| 650 | 4 | |a pharmacokinetics | |
| 650 | 4 | |a solid dispersion | |
| 650 | 7 | |a piperine |2 NLM | |
| 650 | 7 | |a U71XL721QK |2 NLM | |
| 650 | 7 | |a carboxymethyl starch |2 NLM | |
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| 650 | 7 | |a 18alpha-glycyrrhetinic acid |2 NLM | |
| 650 | 7 | |a 1449-05-4 |2 NLM | |
| 650 | 7 | |a Polymers |2 NLM | |
| 650 | 7 | |a Excipients |2 NLM | |
| 700 | 1 | |a Li, Ruilong |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Wenjing |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Xiangyu |e verfasserin |4 aut | |
| 700 | 1 | |a Zhu, Fenxia |e verfasserin |4 aut | |
| 700 | 1 | |a Huang, Yiping |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Jing |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Zhenhai |e verfasserin |4 aut | |
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