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Updated: Jun 3, 2026
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Entrapment of 5-fluorouracil into PLGA matrices using supercritical antisolvent processes
Pardis Kalantarian1, Ismaeil Haririan, Abdolhossein Rouholamini Najafabadi
1Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences National Cell Bank of Iran, Pasteur Institute of Iran, Tehran, Iran.
Objectives:
Two different supercritical antisolvent processes were performed to co-precipitate 5-fluorouracil (5-FU) and poly(lactide-co-glycolide) simultaneously. 5-FU is a hydrophilic antitumor agent, and is more effective when administered at a lower dose for a longer period of time.
Methods:
Controlled-release polymeric systems of 5-FU were produced, and morphology, thermal behavior, in-vitro release and cytotoxicity of microparticles were analysed.
Key Findings:
Dissolution studies showed that 33% of drug was released in 21 days, which represents a long-lasting profile. To evaluate the efficacy of the released drug on cancer cells, the MTT assay cytotoxicity test was performed using human lung carcinoma A549 cell lines. There was no significant difference between the cell inhibition rates of the released drug and unprocessed 5-FU at the same drug concentration level. IC50 values were 69.12 mg/ml for unprocessed 5-FU and 68.71 mg/ml for the released drug.
Conclusions:
Application of supercritical processing for co-precipitation of 5-FU and PLGA provided mild and non-aqueous conditions, so the hydrophilic drug incorporated in the polymer had good stability during the process.
