Enhancing the Solubility of Co-Formulated Hydrophobic Drugs by Incorporating Functionalized Nano-Structured Poly Lactic-<i>co</i>-glycolic Acid (<i>nf</i>PLGA) During Co-Precipitation
<b>Background/Objectives</b>: The co-formulation of active pharmaceutical ingredients (APIs) is a growing strategy in biopharmaceutical development, particularly when it comes to improving solubility and bioavailability. This study explores a co-precipitation method to prepare co-formula...
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| Main Authors: | , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-01-01
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| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/17/1/77 |
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| Summary: | <b>Background/Objectives</b>: The co-formulation of active pharmaceutical ingredients (APIs) is a growing strategy in biopharmaceutical development, particularly when it comes to improving solubility and bioavailability. This study explores a co-precipitation method to prepare co-formulated crystals of griseofulvin (GF) and dexamethasone (DXM), utilizing nanostructured, functionalized polylactic glycolic acid (<i>nf</i>PLGA) as a solubility enhancer. <b>Methods</b>: An antisolvent precipitation technique was employed to incorporate <i>nf</i>PLGA at a 3% concentration into the co-formulated GF and DXM, referred to as DXM-GF-<i>nf</i>PLGA. The dissolution performance of this formulation was compared to that of the pure drugs and the co-precipitated DXM-GF without <i>nf</i>PLGA. <b>Results</b>: Several characterization techniques, including electron microscopy (SEM), RAMAN, FTIR, TGA, and XRD, were used to analyze the <i>nf</i>PLGA incorporation and the co-precipitated co-formulations. The inclusion of <i>nf</i>PLGA significantly enhanced the dissolution and initial dissolution rate of both GF and DXM in the DXM-GF-<i>nf</i>PLGA formulation, achieving a maximum dissolution of 100%, which was not attained by the pure drugs or the DXM-GF formulation. The incorporation of <i>nf</i>PLGA also reduced the amount of time taken to reach 50% (T<sub>50</sub>) and 80% (T<sub>80</sub>) dissolution. T<sub>50</sub> values decreased from 52 and 82 min (for pure DXM and GF) to 23 min for DXM-GF-<i>nf</i>PLGA, and the T<sub>80</sub> improved to 50 min for DXM-GF-<i>nf</i>PLGA, significantly outpacing the pure compounds. Furthermore, incorporating <i>nf</i>PLGA into the crystal structures greatly accelerated the dissolution rates, with initial rates reaching 650.92 µg/min for DXM-GF-<i>nf</i>PLGA compared to 540.60 µg/min for DXM-GF, while pure GF and DXM showed lower rates. <b>Conclusions</b>: This work demonstrates that <i>nf</i>PLGA incorporation enhances dissolution performance by forming water channels within the API crystal via hydrogen-bonding interactions. This innovative <i>nf</i>PLGA incorporation method holds promise for developing hydrophobic co-formulations with faster solubility and dissolution rates. |
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| ISSN: | 1999-4923 |