Artikel ; Online: Synthesis of Microwave Functionalized, Nanostructured Polylactic Co-Glycolic Acid ( nf PLGA) for Incorporation into Hydrophobic Dexamethasone to Enhance Dissolution
Nanomaterials, Vol 13, Iss 943, p
2023 Band 943
Abstract: The low solubility and slow dissolution of hydrophobic drugs is a major challenge for the pharmaceutical industry. In this paper, we present the synthesis of surface-functionalized poly(lactic-co-glycolic acid) (PLGA) nanoparticles for incorporation into ...
Abstract | The low solubility and slow dissolution of hydrophobic drugs is a major challenge for the pharmaceutical industry. In this paper, we present the synthesis of surface-functionalized poly(lactic-co-glycolic acid) (PLGA) nanoparticles for incorporation into corticosteroid dexamethasone to improve its in vitro dissolution profile. The PLGA crystals were mixed with a strong acid mixture, and their microwave-assisted reaction led to a high degree of oxidation. The resulting nanostructured, functionalized PLGA ( nf PLGA), was quite water-dispersible compared to the original PLGA, which was non-dispersible. SEM-EDS analysis showed 53% surface oxygen concentration in the nf PLGA compared to the original PLGA, which had only 25%. The nf PLGA was incorporated into dexamethasone (DXM) crystals via antisolvent precipitation. Based on SEM, RAMAN, XRD, TGA and DSC measurements, the nf PLGA-incorporated composites retained their original crystal structures and polymorphs. The solubility of DXM after nf PLGA incorporation (DXM– nf PLGA) increased from 6.21 mg/L to as high as 87.1 mg/L and formed a relatively stable suspension with a zeta potential of −44.3 mV. Octanol–water partitioning also showed a similar trend as the logP reduced from 1.96 for pure DXM to 0.24 for DXM– nf PLGA. In vitro dissolution testing showed 14.0 times higher aqueous dissolution of DXM– nf PLGA compared to pure DXM. The time for 50% (T 50 ) and 80% (T 80 ) of gastro medium dissolution decreased significantly for the nf PLGA composites; T 50 reduced from 57.0 to 18.0 min and T 80 reduced from unachievable to 35.0 min. Overall, the PLGA, which is an FDA-approved, bioabsorbable polymer, can be used to enhance the dissolution of hydrophobic pharmaceuticals and this can lead to higher efficacy and lower required dosage. |
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Schlagwörter | hydrophobic drug ; FDA polymer ; microwave functionalization ; dexamethasone ; in vitro dissolution ; absorption bioavailability ; Chemistry ; QD1-999 |
Thema/Rubrik (Code) | 500 |
Sprache | Englisch |
Erscheinungsdatum | 2023-03-01T00:00:00Z |
Verlag | MDPI AG |
Dokumenttyp | Artikel ; Online |
Datenquelle | BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl) |
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