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This work aimed to develop a new one-pot and readily scaled-up formulation capable of retaining 5-fluorouracil and prolonging its release to obtain a site-specific medication delivery for the potential treatment of colorectal cancer. Six polymer-based formulations were successfully produced using a thermal bulk polymerization method and loaded with 5-fluorouracil, which is a chemotherapeutic agent used in the treatment of colorectal carcinoma. The pellets produced were characterized by measuring the glass transition temperature, tensile strength, Young’s modulus, and tensile elongation at break. Studies on in vitro swelling and release were carried out in phosphate-buffered saline to evaluate the behaviour of the developed system. The Young’s modulus, glass transition temperature, and tensile strength all increased significantly as the crosslinker concentration increased, but the fracture strain value reduced significantly. The in vitro swelling profile of the produced formulations was significantly reduced by increasing crosslinking density. Less than 27% cumulative drug release was achieved for all formulations after 5 h of starting the release study. The highest cumulative drug release reached after 24 h was 69%. The developed drug delivery system demonstrated the ability to delay the release of 5-fluorouracil in upper gastrointestinal tract-mimicking conditions, while permitting its release in a controlled way afterward, which makes it promising for the potential delivery of 5-fluorouracil to the colon.

Zeolitic imidazole frameworks are emerging materials and have been considered an efficient platform for biomedical applications. The present study highlights the simple fabrication of methyl gallate encapsulated folate-ZIF-L nanoframeworks (MG@Folate ZIF-L) by a simple synthesis. The nanoframeworks were characterized by different sophisticated instruments. In addition, the drug-releasing mechanism was evidenced by in vitro releasing kinetics at various pH conditions. The anti-biofilm potential confirmed by the biofilm architectural deformations against human infectious pathogens MRSA and N7 clinical strains. Furthermore, anticancer efficacy assessed against A549 lung cancer cells. The result reveals that the MG@Folate ZIF-L exposed a superior cytotoxic effect due to the pH-responsive and receptor-based drug-releasing mechanism. Based on the unique physicochemical and biological characteristics of nanoframeworks, it has overcome the problems of undesired side effects and uncontrolled drug release of existing drug delivery systems. Finally, the in vitro toxicity effect of MG@Folate ZIF-L was tested against the Artemia salina (A. salina) model organism, and the results show enhanced biocompatibility. Overall, the study suggested that the novel MG@Folate ZIF-L nanoframeworks is a suitable material for biomedical applications. It will be very helpful to the future design for targeted drug delivery systems.

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Objective: The objective of this study was to evaluate the suitability of ternary mixture of smart polymers comprised of Eudragit®E100, Eudragit®L100, and sodium alginate to serve as a carrier for sustained drug release for weakly basic drugs. The model drug chosen in this part of the study is Metronidazole. Methods: Matrix tablets formulations were prepared by either direct compression or by wet granulation. Dissolution studies were conducted using USP XXΠ rotating paddle apparatus in three different consecutive stages (pH 1.2, 4.8 and 6.8). Tablets made of low to intermediate proportions of sodium alginate and an approximately equal proportions of Eudragit®E100 and Eudragit®L100 were found to have significant modification of drug release rates. Result: Thus, indicating a potential for controlling the drug release for 12 hours depending on polymers ratios in the formulation. The ratio of sodium alginate to total Eudragit® polymers and the ratio of Eudragit®E100 to Eudragit®L100 within the ternary polymeric composition were found critical in determining the controlled release performance. Conclusion: Results of swelling studies were in agreement with the dissolution behaviors of the tablets. The findings suggest the significance of the ternary polymeric compositions in controlling the release of weakly basic drug.