Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).
The present investigation aims at developing models by response surface methodology (FCCCD) followed by the scale-up method in preparing control release microsponge particles loaded with 5- fluorouracil, a drug used to treat actinic keratosis and colon cancer, and producing a new Dermal Delivery System.
The polymer-based (ethyl cellulose and Eudragit RS 100) microsponge particles were prepared by the w/o/w double emulsification method. The optimized product was formed with the combination of independent variables levels: polymer (600 mg), stirring speed (1198 rpm) and surfactant (2% w/v), yielding responses as yield (~63.6257%), the average size of particles (~151.563 µm), entrapment efficiency (~75.319 %) and drug release in 8hr (~75.75%), with desirability value of 0.737.
The products showed similar responses as obtained in scale-up work. FT-IR, DSC and SEM studies confirmed the drug’s compatibility with polymers and porous morphology. Finally, gel embedded optimised product showed shear-thinning rheological property, ideal for drug release from the thixotropic gel.
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Shahjaman Halder, Sourav Poddar, Jasmina Khanam et al. Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU)., 27 October 2021, PREPRINT (Version 1) available at Research Square [https://doi.org/10.21203/rs.3.rs-989826/v1]