Dissolution Enhancement and Controlled Release of Paclitaxel Drug via a Hybrid Nanocarrier Based on mPEG-PCL Amphiphilic Copolymer and Fe-BTC Porous Metal-Organic Framework

作者: Nikolaos Bikiaris , Nina Ainali , Evi Christodoulou , Margaritis Kostoglou , Thomas Kehagias

DOI: 10.3390/NANO10122490

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摘要: In the present work, porous metal-organic framework (MOF) Basolite®F300 (Fe-BTC) was tested as a potential drug-releasing depot to enhance solubility of anticancer drug paclitaxel (PTX) and prepare controlled release formulations after its encapsulation in amphiphilic methoxy poly(ethylene glycol)-poly(e-caprolactone) (mPEG-PCL) nanoparticles. Investigation revealed that adsorption Fe-BTC reached approximately 40%, relatively high level, also led an overall amorphization confirmed by differential scanning calorimetry (DSC) X-ray diffraction (XRD). The dissolution rate PTX-loaded MOF substantially enhanced achieving complete (100%) within four days, while neat only 13% maximum (3–4 days). This PTX-Fe-BTC nanocomposite further encapsulated into mPEG-PCL matrix, typical aliphatic copolyester synthesized our lab, whose biocompatibility validated vitro cytotoxicity tests toward human umbilical vein endothelial cells (HUVEC). Encapsulation performed according solid-in-oil-in-water emulsion/solvent evaporation technique, resulting nanoparticles about 143 nm, slightly larger those prepared without pre-adsorption PTX on (138 respectively). Transmission electron microscopy (TEM) imaging spherical with embedded were indeed fabricated, sizes ranging from 80 150 nm. Regions composite Fe-BTC-PTX system infrared (IR) spectrum are identified signatures drug-MOF interaction. profiles all showed initial burst release, attributed amount located at surface or close it, followed steadily release. is corroborated computational analysis reveals attaches effectively building blocks, but large size limits diffusion through crystalline regions Fe-BTC. behaviour can be described bimodal diffusivity model. studied could serve chemotherapeutic candidates for delivery.

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