Calcium carbonate is an abundant mineral with several advantages to be a successful carrier to improve oral bioavailability of poorly water-soluble drugs, such as praziquantel. Praziquantel is an antiparasitic drug classified in group II of the Biopharmaceutical Classification System hence characterized by high-permeability and low-solubility. Therefore, the dissolution rate is the limiting factor for the gastrointestinal absorption that contributes to the low bioavailability. Consequently, the therapeutic dose of the praziquantel must be high and big tablets and capsules are required, which are difficult to swallow, especially for pediatric and elderly patients. Mixtures of praziquantel and calcium carbonate using solid-solid physical mixtures and solid dispersions were prepared and characterized using several techniques (X-ray diffraction differential scanning calorimetry, thermogravimetric analysis, scanning electron microscopy, laser diffraction, Fourier transform infrared and Raman spectroscopies). Solubility of these formulations evidenced that the solubility of praziquantel-calcium carbonate interaction product increased in physiological media. In vitro dissolution tests showed that the interaction product increased the dissolution rate of the drug in acidic medium. Theoretical models were studied to understand this experimental behavior. Cytotoxicity and cell cycle studies were performed, showing that praziquantel-calcium carbonate physical mixture and interaction product were biocompatible with the HTC116 cells, because it did not produce a decrease in cell viability or alterations in the cell cycle.

Borrego-Sanchez A., Sanchez-Espejo R., Albertini B., Passerini N., Cerezo P., Viseras C., et al. (2019). Ground calcium carbonate as a low cost and biosafety excipient for solubility and dissolution improvement of praziquantel. PHARMACEUTICS, 11(10), 1-12 [10.3390/pharmaceutics11100533].

Ground calcium carbonate as a low cost and biosafety excipient for solubility and dissolution improvement of praziquantel

Albertini B.;Passerini N.;
2019

Abstract

Calcium carbonate is an abundant mineral with several advantages to be a successful carrier to improve oral bioavailability of poorly water-soluble drugs, such as praziquantel. Praziquantel is an antiparasitic drug classified in group II of the Biopharmaceutical Classification System hence characterized by high-permeability and low-solubility. Therefore, the dissolution rate is the limiting factor for the gastrointestinal absorption that contributes to the low bioavailability. Consequently, the therapeutic dose of the praziquantel must be high and big tablets and capsules are required, which are difficult to swallow, especially for pediatric and elderly patients. Mixtures of praziquantel and calcium carbonate using solid-solid physical mixtures and solid dispersions were prepared and characterized using several techniques (X-ray diffraction differential scanning calorimetry, thermogravimetric analysis, scanning electron microscopy, laser diffraction, Fourier transform infrared and Raman spectroscopies). Solubility of these formulations evidenced that the solubility of praziquantel-calcium carbonate interaction product increased in physiological media. In vitro dissolution tests showed that the interaction product increased the dissolution rate of the drug in acidic medium. Theoretical models were studied to understand this experimental behavior. Cytotoxicity and cell cycle studies were performed, showing that praziquantel-calcium carbonate physical mixture and interaction product were biocompatible with the HTC116 cells, because it did not produce a decrease in cell viability or alterations in the cell cycle.
2019
Borrego-Sanchez A., Sanchez-Espejo R., Albertini B., Passerini N., Cerezo P., Viseras C., et al. (2019). Ground calcium carbonate as a low cost and biosafety excipient for solubility and dissolution improvement of praziquantel. PHARMACEUTICS, 11(10), 1-12 [10.3390/pharmaceutics11100533].
Borrego-Sanchez A.; Sanchez-Espejo R.; Albertini B.; Passerini N.; Cerezo P.; Viseras C.; Sainz-Diaz C.I.
File in questo prodotto:
File Dimensione Formato  
PZQ_pharmaceutics-granada.pdf

accesso aperto

Tipo: Versione (PDF) editoriale
Licenza: Licenza per Accesso Aperto. Creative Commons Attribuzione (CCBY)
Dimensione 1.26 MB
Formato Adobe PDF
1.26 MB Adobe PDF Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/721688
Citazioni
  • ???jsp.display-item.citation.pmc??? 4
  • Scopus 18
  • ???jsp.display-item.citation.isi??? 18
social impact