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...
Saved in:
| Main Authors: | , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-01-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/17/1/77 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1832587710856953856 |
|---|---|
| author | Mohammad Saiful Islam Somenath Mitra |
| author_facet | Mohammad Saiful Islam Somenath Mitra |
| author_sort | Mohammad Saiful Islam |
| collection | DOAJ |
| description | <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. |
| format | Article |
| id | doaj-art-63059674b94d4393985207d192150579 |
| institution | Kabale University |
| issn | 1999-4923 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj-art-63059674b94d4393985207d1921505792025-01-24T13:45:51ZengMDPI AGPharmaceutics1999-49232025-01-011717710.3390/pharmaceutics17010077Enhancing 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-PrecipitationMohammad Saiful Islam0Somenath Mitra1Department of Chemistry and Environmental Science, New Jersey Institute of Technology, Newark, NJ 07102, USADepartment of Chemistry and Environmental Science, New Jersey Institute of Technology, Newark, NJ 07102, USA<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.https://www.mdpi.com/1999-4923/17/1/77co-formulationfunctional <i>nf</i>PLGAincorporationantisolvent technologyco-precipitationdissolution |
| spellingShingle | Mohammad Saiful Islam Somenath Mitra 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 Pharmaceutics co-formulation functional <i>nf</i>PLGA incorporation antisolvent technology co-precipitation dissolution |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| topic | co-formulation functional <i>nf</i>PLGA incorporation antisolvent technology co-precipitation dissolution |
| url | https://www.mdpi.com/1999-4923/17/1/77 |
| work_keys_str_mv | AT mohammadsaifulislam enhancingthesolubilityofcoformulatedhydrophobicdrugsbyincorporatingfunctionalizednanostructuredpolylacticicoiglycolicacidinfiplgaduringcoprecipitation AT somenathmitra enhancingthesolubilityofcoformulatedhydrophobicdrugsbyincorporatingfunctionalizednanostructuredpolylacticicoiglycolicacidinfiplgaduringcoprecipitation |