Impact of cyclodextrin derivatives on systemic release of duloxetine HCl via buccal route
| Autor: | Rajesh Kumar, Lalita Dahiya, Gurpal Singh, V. R. Sinha, Amita Sarwal |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Pharmacology
Cyclodextrins Chromatography Organic Chemistry Administration Buccal Pharmaceutical Science Duloxetine HCl 02 engineering and technology Buccal administration Permeation Duloxetine Hydrochloride 021001 nanoscience & nanotechnology 030226 pharmacology & pharmacy Cyclodextrin Derivatives 2-Hydroxypropyl-beta-cyclodextrin 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Solubility chemistry Drug Discovery Duloxetine 0210 nano-technology |
| DOI: | 10.6084/m9.figshare.12382664 |
| Popis: | Aim: The aim of this work was to develop buccoadhesive tablets for the systemic delivery of duloxetine HCl (DXT) using more soluble derivatives of β-cyclodextrin, i.e. hydroxypropyl-β-cyclodextrin (HPβCD) and sulfobutylether-β-cyclodextrin (SBEβCD) and to investigate enhanced cellular uptake of inclusion complexed drug. Materials and methods: Freeze dried and spray dried complexes of both cyclodextrin derivatives with DXT (1:1 molar) were prepared and characterized with DSC, FTIR, and PXRD techniques. C971 and PC, on the basis of swelling behavior, erosion and in vitro residence time, were selected for further study at different levels (−1, 0, +1) to optimize the formulation in terms of enhanced drug release and ex vivo permeation. Results: SBEβCD based complexes show more aqueous solubility of DXT (0.782 and 0.958 mM) and more complexation efficiency compared to HPβCD at 25 °C and 37 °C, respectively. Apparent stability constant was reported to be higher (1109.94 and 1693.25 M−1) for DXT-SBEβCD at 25 °C and 37 °C, respectively, than the corresponding values for DXT-HPβCD systems. Enhanced cellular uptake using fibroblast cells was revealed for complexed drug compared to free drug . Conclusion: Both cyclodextrin derivatives are able to enhance drug release and permeation in vitro and ex vivo. |
| Databáze: | OpenAIRE |
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