研究目的
To design a new aqueous-based anti-inflammatory eye drop containing nepafenac, cyclodextrin, and polymer to improve drug solubility and bioavailability for ocular delivery.
研究成果
The study successfully developed nepafenac-loaded cyclodextrin/polymer nanoaggregates for eye drop formulations, with HPβCD enhancing solubility and γCD promoting nanoaggregate formation. Formulations with specific polymer combinations showed promising properties for improved ocular drug delivery, but further studies are needed for clinical application.
研究不足
The study did not include in vivo testing to assess bioavailability or toxicity in biological systems. The formulations may require further optimization for osmolality adjustment to reach normal values. No synergistic effect was found with CD mixtures for solubility enhancement.
1:Experimental Design and Method Selection:
The study involved phase solubility studies to evaluate drug solubility with different cyclodextrins, characterization of inclusion complexes using DSC, FT-IR, and 1H-NMR, and formulation of eye drops with various polymers. Methods included sonication for heating, freeze-drying for sample preparation, and analytical techniques like UHPLC for quantification.
2:Sample Selection and Data Sources:
Nepafenac was used as the drug model. Cyclodextrins (αCD, βCD, γCD, HPαCD, HPβCD, HPγCD) and polymers (PVP, PVA, CMC, HPMC, MC, tyloxapol) were selected based on previous studies. Data were sourced from experimental measurements.
3:List of Experimental Equipment and Materials:
Equipment included moisture analyser, sonicator, UHPLC system, FT-IR spectrometer, DSC instrument, 1H-NMR spectrometer, centrifuge, particle size analyser, viscometer, osmometer, and TEM. Materials included nepafenac, cyclodextrins, polymers, solvents, and chemicals of analytical grade.
4:Experimental Procedures and Operational Workflow:
Procedures involved moisture content measurement, chemical stability tests, phase solubility studies with sonication and shaking, complex preparation by freeze-drying, spectroscopic analyses, formulation of eye drops with specific compositions, and characterization of formulations for solubility, viscosity, osmolality, and particle size.
5:Data Analysis Methods:
Data were analyzed using software like Chromeleon for HPLC, with calculations for stability constants and complexation efficiency. Statistical analysis included mean and standard deviation from triplicate measurements.
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FT-IR spectrometer
Nicolet iS10
Thermo Fisher Scientific
Characterizing inclusion complexes by infrared spectroscopy
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1H-NMR spectrometer
AVANCE 400
Bruker
Structural elucidation of inclusion complexes
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TEM
JEM 1400
JEOL
Visual analysis of nanoaggregate morphology
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moisture analyser
MX-50
A&D company
Measuring water content of cyclodextrins
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UHPLC system
Ultimate 3000 series
Dionex
Quantitative analysis of nepafenac by HPLC
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column
Kinetex C18
Phenomenex
Stationary phase for HPLC separation
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DSC instrument
DSC 214 polyma
Netzsch
Thermal analysis of complexes
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freeze dryer
2040
Snijders scientific
Preparation of inclusion complexes by freeze-drying
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centrifuge
MC6
Sarstedt
Centrifuging formulations for solid drug fraction analysis
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particle size analyser
Nanotrac Wave
Microtrac
Characterizing particle sizes in formulations
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viscometer
DV2T
Brookfield
Measuring viscosity of formulations
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osmometer
Osmomat 030
Gonotec
Determining osmolality of formulations
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