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Carboxymethyl starch as a solid dispersion carrier to enhance the dissolution and bioavailability of piperine and 18 β -glycyrrhetinic acid.

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  • معلومة اضافية
    • المصدر:
      Publisher: Informa Healthcare Country of Publication: England NLM ID: 7802620 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-5762 (Electronic) Linking ISSN: 03639045 NLM ISO Abbreviation: Drug Dev Ind Pharm Subsets: MEDLINE
    • بيانات النشر:
      Publication: London : Informa Healthcare
      Original Publication: New York, Dekker.
    • الموضوع:
      Polymers* ; Excipients*/chemistry; Spectroscopy, Fourier Transform Infrared/methods ; Biological Availability ; Solubility ; Calorimetry, Differential Scanning
    • نبذة مختصرة :
      Objective: To investigate the applicability of carboxymethyl starch (CMS) as a carrier to prepare solid dispersions (SDs) of piperine (PIP) and 18 β -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 AUC 0-24 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.
    • Contributed Indexing:
      Keywords: 18β-glycyrrhetinic acid; Piperine; bioavailability; carboxymethyl starch; pharmacokinetics; solid dispersion
    • الرقم المعرف:
      U71XL721QK (piperine)
      9057-06-1 (carboxymethyl starch)
      1449-05-4 (18alpha-glycyrrhetinic acid)
      0 (Polymers)
      0 (Excipients)
    • الموضوع:
      Date Created: 20230221 Date Completed: 20230322 Latest Revision: 20230322
    • الموضوع:
      20250114
    • الرقم المعرف:
      10.1080/03639045.2023.2182120
    • الرقم المعرف:
      36803327