Hemil S. Patel, Anju P. Kunjadiya, A. Rahdar, Rakesh K. Sharma
{"title":"用于姜黄素药物生物利用度的pluronic -磷脂酰胆碱混合聚合物纳米束制剂:设计、制造、表征和体外生物研究","authors":"Hemil S. Patel, Anju P. Kunjadiya, A. Rahdar, Rakesh K. Sharma","doi":"10.1177/08839115231157098","DOIUrl":null,"url":null,"abstract":"Curcumin (CUR), obtained from turmeric, has biological advantages, but low aqueous solubility restricts its pharmaceutical applications. In the present work, a mixed polymeric nanomicellar formulation composed of bioactive Pluronic P123, Pluronic F68, and biocompatible phosphatidylcholine (PC) was designed and examined as the nanovehicles for overcoming the major barriers of poor bioavailability related to CUR. The CUR-incorporated P123/F68/PC mixed nanomicellar formulation (CUR-PFPC) was fabricated by the thin film technique and investigated in vitro. The fabrication of CUR-PFPC was optimized through D-optimal design. CUR-PFPC morphology, size distribution, zeta potential, drug encapsulating and incorporation efficiency, compatibility, and crystallinity were characterized using DLS, TEM, FTIR, XRD, and DSC analysis. Moreover, the cumulative drug release, antioxidant assays, and antimicrobial properties of formulations were also examined. The CUR-PFPC formulation exhibited a micellar size of 67.43 nm, a zeta potential of −15.1 mV, a PDI of 0.528, and a spherical shape. The mixed micellar formulation showed excellent compatibility and stability. The in vitro release profile of the CUR-PFPC reached over 60% in comparison to the 95% release of CUR, indicating a slow and sustained release. The DPPH assay showed that the CUR-PFPC had 96% antioxidant activity. Results show that the CUR-PFPC has powerful antibacterial and antifungal properties, which separates it from the free CUR. These findings suggest that the fabricated CUR-PFPC mixed polymeric nanomicellar formulation is thermodynamically and kinetically stable and may be considered a novel nanovehicle for hydrophobic antimicrobial drugs like CUR. Graphical Abstract","PeriodicalId":15038,"journal":{"name":"Journal of Bioactive and Compatible Polymers","volume":"32 1","pages":"191 - 208"},"PeriodicalIF":2.1000,"publicationDate":"2023-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Pluronic-phosphatidylcholine mixed polymeric nanomicellar formulation for curcumin drug bioavailability: Design, fabrication, characterization and in vitro bioinvestigations\",\"authors\":\"Hemil S. Patel, Anju P. Kunjadiya, A. Rahdar, Rakesh K. Sharma\",\"doi\":\"10.1177/08839115231157098\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Curcumin (CUR), obtained from turmeric, has biological advantages, but low aqueous solubility restricts its pharmaceutical applications. In the present work, a mixed polymeric nanomicellar formulation composed of bioactive Pluronic P123, Pluronic F68, and biocompatible phosphatidylcholine (PC) was designed and examined as the nanovehicles for overcoming the major barriers of poor bioavailability related to CUR. The CUR-incorporated P123/F68/PC mixed nanomicellar formulation (CUR-PFPC) was fabricated by the thin film technique and investigated in vitro. The fabrication of CUR-PFPC was optimized through D-optimal design. CUR-PFPC morphology, size distribution, zeta potential, drug encapsulating and incorporation efficiency, compatibility, and crystallinity were characterized using DLS, TEM, FTIR, XRD, and DSC analysis. Moreover, the cumulative drug release, antioxidant assays, and antimicrobial properties of formulations were also examined. The CUR-PFPC formulation exhibited a micellar size of 67.43 nm, a zeta potential of −15.1 mV, a PDI of 0.528, and a spherical shape. The mixed micellar formulation showed excellent compatibility and stability. The in vitro release profile of the CUR-PFPC reached over 60% in comparison to the 95% release of CUR, indicating a slow and sustained release. The DPPH assay showed that the CUR-PFPC had 96% antioxidant activity. Results show that the CUR-PFPC has powerful antibacterial and antifungal properties, which separates it from the free CUR. These findings suggest that the fabricated CUR-PFPC mixed polymeric nanomicellar formulation is thermodynamically and kinetically stable and may be considered a novel nanovehicle for hydrophobic antimicrobial drugs like CUR. 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Pluronic-phosphatidylcholine mixed polymeric nanomicellar formulation for curcumin drug bioavailability: Design, fabrication, characterization and in vitro bioinvestigations
Curcumin (CUR), obtained from turmeric, has biological advantages, but low aqueous solubility restricts its pharmaceutical applications. In the present work, a mixed polymeric nanomicellar formulation composed of bioactive Pluronic P123, Pluronic F68, and biocompatible phosphatidylcholine (PC) was designed and examined as the nanovehicles for overcoming the major barriers of poor bioavailability related to CUR. The CUR-incorporated P123/F68/PC mixed nanomicellar formulation (CUR-PFPC) was fabricated by the thin film technique and investigated in vitro. The fabrication of CUR-PFPC was optimized through D-optimal design. CUR-PFPC morphology, size distribution, zeta potential, drug encapsulating and incorporation efficiency, compatibility, and crystallinity were characterized using DLS, TEM, FTIR, XRD, and DSC analysis. Moreover, the cumulative drug release, antioxidant assays, and antimicrobial properties of formulations were also examined. The CUR-PFPC formulation exhibited a micellar size of 67.43 nm, a zeta potential of −15.1 mV, a PDI of 0.528, and a spherical shape. The mixed micellar formulation showed excellent compatibility and stability. The in vitro release profile of the CUR-PFPC reached over 60% in comparison to the 95% release of CUR, indicating a slow and sustained release. The DPPH assay showed that the CUR-PFPC had 96% antioxidant activity. Results show that the CUR-PFPC has powerful antibacterial and antifungal properties, which separates it from the free CUR. These findings suggest that the fabricated CUR-PFPC mixed polymeric nanomicellar formulation is thermodynamically and kinetically stable and may be considered a novel nanovehicle for hydrophobic antimicrobial drugs like CUR. Graphical Abstract
期刊介绍:
The use and importance of biomedical polymers, especially in pharmacology, is growing rapidly. The Journal of Bioactive and Compatible Polymers is a fully peer-reviewed scholarly journal that provides biomedical polymer scientists and researchers with new information on important advances in this field. Examples of specific areas of interest to the journal include: polymeric drugs and drug design; polymeric functionalization and structures related to biological activity or compatibility; natural polymer modification to achieve specific biological activity or compatibility; enzyme modelling by polymers; membranes for biological use; liposome stabilization and cell modeling. This journal is a member of the Committee on Publication Ethics (COPE).