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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
Enhancing dissolution of poorly water-soluble prednisolone via spray-dried arabinoxylan microspheres: a novel
Muniyandy Saravanan1, Rowena Gan1, Chin Jia Rei2
1Department of Pharmacy, Fatima College of Health Sciences, Abu Dhabi, United Arab Emirates.
Background:
Prednisolone's poor aqueous solubility limits its oral bioavailability, necessitating the development of innovative formulation strategies.
Objective:
This study aimed to extract AX from ispaghula husk and develop AX-based spray-dried microspheres to improve prednisolone dissolution.
Methods:
AX was extracted from ispaghula husk, and its molecular weight was determined using gel permeation chromatography. Prednisolone-loaded AX microspheres (F1-F4) were prepared by spray drying and evaluated for drug loading, entrapment efficiency, and product yield. Structural and physicochemical characterization was performed using NMR, FTIR, SEM, and DSC. In vitro dissolution studies were conducted over 60 min. Initial and relative dissolution rates, along with similarity factor (f2) analysis, were used to compare formulations.
Main Findings:
Drug loading ranged from 3.7 to 15.63% w/w, with the highest values observed for F3 and F4. Entrapment efficiency increased with drug loading, ranging from 15.85% (F1) to 36.43% (F4), while product yield ranged from 52.4 to 63.1% w/w. NMR confirmed drug stability following spray drying. SEM revealed irregular, rough-surfaced microspheres and reduced drug particle size. FTIR demonstrated drug-polymer compatibility, and DSC indicated drug amorphization. Formulations F3 and F4 achieved >72% dissolution within 60 min, exceeding pure prednisolone (26.8%) and the commercial tablet (49.9%). Similarity factor analysis indicated that F1 was closest to the marketed product, whereas F3 and F4 exhibited superior dissolution rates.
Conclusion:
Spray-dried AX microspheres significantly enhanced prednisolone dissolution, highlighting AX as a biocompatible, scalable, and promising excipient for poorly water-soluble drugs.
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