Solid-state interactions and drug release of teicoplanin in binary combinations with peracetylated α-, β-, and γ-cyclodextrins

Giampiero Bettinetti, Milena Sorrenti, Laura Catenacci, Franca Ferrari, Silvia Rossi, Ilaria Salvadeo, Paolo Carraro

Research output: Contribution to journalArticle

Abstract

Triacetyl α-cyclodextrin, triacetyl β-cyclodextrin and triacetyl γ-cyclodextrin were tested as possible hydrophobic carriers to prolong the release of hydrophilic teicoplanin (TCP). Physical-chemical characterization of individual components, drug-carrier physical mixtures at 0.5, 0.67 and 0.75 mass fraction of carrier, and the respective interaction products by kneading or evaporative crystallization under microwave irradiation was carried out using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). In vitro drug release in pH 7.4 phosphate buffer at 37°C was determined by intrinsic dissolution rate (IDR) measurements on non disintegrating compressed discs. Solid-state interactions of TCP with triacetyl α-cyclodextrin by evaporative crystallization and kneading and with triacetyl β-cyclodextrin by evaporative crystallization (probably resulting in carrier amorphization) were demonstrated. The role of carrier hydrophobicity, carrier mass fraction and preparation method of solid drug-carrier combinations on solid-state drug-carrier interactions and slowing down of TCP release was assessed. Modulation of drug release can be achieved using TCP-triacetyl γ-cyclodextrin combinations at 0.5 mass fraction of carrier.

Original languageEnglish
Pages (from-to)329-332
Number of pages4
JournalJournal of Inclusion Phenomena and Macrocyclic Chemistry
Volume57
Issue number1-4
DOIs
Publication statusPublished - Apr 2007

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Keywords

  • Differential scanning calorimetry
  • Intrinsic dissolution rate
  • Peracetylated α-, β-, and γ-cyclodextrins
  • Teicoplanin
  • Thermogravimetric analysis

ASJC Scopus subject areas

  • Chemistry(all)
  • Condensed Matter Physics

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