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Swed, A., Cordonnier, T., Dénarnaud, A., Boyer, C., Guicheux, J., Weiss, P., & Boury, F. (2015). International journal of pharmaceutics, 493(1-2), 357-365.
Glycofurol (GF) has been successfully applied as a non-volatile, biocompatible solvent in the preparation of PLGA microparticles for controlled delivery of transforming growth factor β1 (TGF-β1), a pivotal protein in cartilage regeneration. Its unique solvent properties enable efficient protein precipitation and subsequent encapsulation under mild, CO₂-assisted emulsification/extraction conditions, preserving the bioactivity of TGF-β1.
Experimental Approach:
TGF-β1 was first precipitated by mixing 120 μL of GF with 75 μL of isosorbide dimethyl ether (DMI) in a buffered Tris-HCl/NaCl solution containing Lutrol® F68 and TGF-β1, forming a 200 μL suspension of protein precipitates. The precipitation efficiency was determined via centrifugation at 10,000 × g for 30 minutes, with the pellet dissolved for quantification. Subsequently, the protein precipitates were encapsulated into PLGA microparticles through a CO₂-assisted emulsification/extraction process conducted under mild temperature and pressure, using GF to dissolve the polymer matrix.
Results and Implications:
The process achieved high encapsulation efficiency while retaining the bioactivity of TGF-β1. Microparticle characterization by SEM and AFM revealed uniform size distribution, stable surface morphology, and favorable zeta potential. In vitro release studies demonstrated sustained protein delivery, and cytotoxicity assays confirmed excellent cytocompatibility of the microparticles.
The application of Glycofurol in this process highlights its dual functionality as a protein precipitation agent and polymer solvent, enabling the fabrication of advanced PLGA-based delivery systems. These systems offer precise control over protein release and hold significant potential for regenerative medicine, particularly for cartilage repair and other tissue engineering applications.
Sobel, Douglas, et al. Polymers 16.3 (2024): 434.
Glycofurol (GF) has been employed as a non-toxic, biocompatible solvent for the preparation of poly(D,L-lactide-co-glycolide) (PLGA) microspheres, enabling the sustained release of dexamethasone with enhanced clinical performance. Traditional preparation methods relying on volatile organic solvents often result in drug denaturation, cytotoxicity, and suboptimal release kinetics. By using glycofurol, these limitations are effectively addressed.
Experimental Approach:
PLGA (lactide:glycolide 75:25) was dissolved in undiluted glycofurol at 1-20% w/v concentrations. Dexamethasone (1-20% wt./wt. PLGA) was incorporated, and the mixture was processed via either a modified phase inversion (GPI) or glycofurol extraction method (GEM). For GPI, the polymer-drug solution was pumped through a fine needle into distilled water under controlled airflow, promoting rapid phase inversion and microsphere formation. GEM involved emulsifying the polymer-drug-glycofurol solution in 0.1% PVA, followed by gradual addition of water to precipitate microspheres. Collected microspheres were filtered, washed, lyophilized, and stored at -20 °C.
Results and Implications:
Glycofurol-fabricated PLGA microspheres exhibited higher drug loading, lower water diffusion rates, and reduced burst release compared to dichloromethane-prepared spheres. Importantly, the drug retained its chemical integrity, and the microspheres demonstrated no cytotoxicity toward target cells. These attributes collectively translate into prolonged, clinically advantageous drug release profiles, supporting local therapy while minimizing systemic side effects.
This study highlights glycofurol's dual role as a polymer solvent and processing medium, offering a safer, more efficient route for fabricating PLGA-based drug delivery systems. Its application represents a significant advancement in the preparation of microsphere carriers for sustained-release therapeutics.
Thedrattanawong, Chitinart, Chawan Manaspon, and Norased Nasongkla. Journal of Drug Delivery Science and Technology 46 (2018): 446-451.
Glycofurol (GF) was utilized as a non-toxic, injectable solvent to prepare poly(D,L-lactide-co-glycolide) (PLGA)-based depots loaded with doxorubicin (Dox) for sustained-release pharmaceutical applications. Conventional organic solvents often pose toxicity and biocompatibility issues, whereas GF provides a safe alternative that efficiently dissolves both PLGA and Dox to form a homogeneous polymer-drug solution.
Experimental Approach:
PLGA (LA:GA = 70:30, Mw = 28.5 kDa, PDI = 1.52) was dissolved in glycofurol at concentrations of 5-20% w/v. Doxorubicin, in protonated and deprotonated forms, was incorporated at 15% w/w relative to PLGA. The mixture was incubated overnight at 37 °C under gentle agitation to ensure complete polymer-drug homogenization. Depots (~25 mg) were formed by injecting the solution into PBS (pH 7.4), where rapid phase inversion precipitated PLGA as a solid matrix, encapsulating Dox while glycofurol diffused into the aqueous phase.
Results and Implications:
Optimal depot formation occurred at 15% w/v PLGA, achieving high encapsulation efficiency of protonated Dox (97.7 ± 0.4%). Lower polymer concentrations failed to produce coherent depots, while higher concentrations caused excessive viscosity and needle obstruction. GF's biocompatibility and rapid clearance (0.598 ± 0.051 L/h/kg in humans) further support its use in injectable systems. This methodology enables the fabrication of PLGA depots with controlled drug release, minimized burst effects, and preserved drug integrity.
The study demonstrates glycofurol's critical role in enabling safe, efficient preparation of polymeric depots for chemotherapeutic delivery, offering a scalable and clinically relevant platform for sustained-release therapies.
What is the molecular formula of Glycofurol?
The molecular formula of Glycofurol is C7H14O3.
What is the molecular weight of Glycofurol?
The molecular weight of Glycofurol is 146.18 g/mol.
What are the synonyms for Glycofurol?
Some synonyms for Glycofurol include 5831-59-4, 2-[(tetrahydrofurfuryl)oxy]ethanol, and 31692-85-0.
When was Glycofurol created and last modified?
Glycofurol was created on 2005-08-08 and last modified on 2023-12-30.
What is the IUPAC name of Glycofurol?
The IUPAC name of Glycofurol is 2-(oxolan-2-ylmethoxy)ethanol.
What is the InChIKey of Glycofurol?
The InChIKey of Glycofurol is CTPDSKVQLSDPLC-UHFFFAOYSA-N.
How many hydrogen bond acceptors does Glycofurol have?
Glycofurol has 3 hydrogen bond acceptors.
What is the topological polar surface area of Glycofurol?
The topological polar surface area of Glycofurol is 38.7 Å2.
How many rotatable bond counts does Glycofurol have?
Glycofurol has 4 rotatable bond counts.
Is Glycofurol considered as a canonicalized compound?
Yes, Glycofurol is considered as a canonicalized compound.
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