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Docetaxel/dimethyl-β-cyclodextrin inclusion complexes: preparation, in vitro evaluation and physicochemical
Bhupendra Raj Giri1, Jaehyeok Lee1, Dong Yu Lim2
1Vessel-Organ Interaction Research Center (VOICE, MRC), BK21 FOUR Community-Based Intelligent Novel Drug Discovery Education Unit, College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu, South Korea.
This study developed an oral drug delivery system for hydrophobic docetaxel (DTX) using dimethyl-β-cyclodextrin (DM-β-CD). The resulting inclusion complex significantly improved DTX solubility and dissolution, enhancing its oral bioavailability.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Materials Science
Background:
- Oral delivery of hydrophobic drugs like docetaxel (DTX) remains a significant challenge in pharmaceutical development.
- Novel drug delivery systems and multifunctional excipients are crucial for overcoming limitations in drug solubility and bioavailability.
- Cyclodextrins, particularly modified forms like dimethyl-β-cyclodextrin (DM-β-CD), offer potential for encapsulating hydrophobic drugs.
Purpose of the Study:
- To investigate the inclusion complexation of docetaxel (DTX) with dimethyl-β-CD (DM-β-CD) to enhance DTX's solubility, dissolution, and permeability for oral delivery.
- To characterize the physicochemical properties of the DTX/DM-β-CD inclusion complex.
- To evaluate the biopharmaceutical performance of the developed inclusion complex.
Main Methods:
- Preparation of solid binary inclusion complex (IC) of DTX with DM-β-CD using the solvent evaporation technique.
- Comprehensive characterization of the IC using solubility, dissolution, permeability, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FT-IR), and nuclear magnetic resonance (¹H NMR).
- Comparison of the properties of the inclusion complex with free DTX powder.
Main Results:
- DM-β-CD exhibited the highest solubility enhancement for DTX among tested β-cyclodextrins.
- The aqueous solubility and in vitro dissolution rate of DTX/DM-β-CD IC increased by 76.04- and 3.55-fold, respectively, compared to free DTX.
- Physicochemical analyses confirmed the formation of a true inclusion complex at a 1:1 molar ratio, with DTX transitioning from a crystalline to an amorphous state within the complex.
- The inclusion complex showed similar absorptive permeability but reduced efflux compared to pure DTX.
Conclusions:
- Solid inclusion complexes of DTX with DM-β-CD prepared via solvent evaporation are effective in significantly enhancing the solubility and dissolution rate of the hydrophobic drug.
- The amorphous nature and inclusion complex formation contribute to improved drug performance.
- This approach represents a promising strategy for enhancing the biopharmaceutical properties of hydrophobic drugs like docetaxel for oral administration.
