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Objective: To formulate and characterize 5-fluorouracil loaded niosomal-in-situ gel for sustained drug delivery to reduce dosing frequency at the same time, follow a local drug delivery for cancer targeting. Methods: Cholesterol and span-60-based niosomes were prepared after following the modified ether injection method. Best formulation selected after characterization through FTIR, SEM, % Entrapment efficiency, zeta potential, polydispersity index, in vitro release, and vesicle size whereas, based on cold method niosomes encapsulated in-situ gel was formulated and characterized through gelling temperature and time, spreadability and syringe ability, gel strength, adhesive force, and drug release. Results: Based on various studies, included particle size, PDI, zeta potential value, % Entrapment efficiency and % drug release, F1 formulation was selected as a best formulation, as niosomal particle size of 388.3 nm proved a higher drug permeation through the buccal area, whereas PDI and zeta potential value of 0.304 and+50.5 are proved a uniform niosomal size with optimum charge distribution which helps to attain higher stability of the formulation, on the other hand % Entrapment efficiency of 87.825% proved that niosomes are capable to hold higher drug concentration; lastly 84.567% of drug release within 12 h of time period prove that higher amount of drug release occur by following sustained release pattern. On the other hand Mucoadhesion, gelling strength and in vitro permeation studies prove that niosomes containing in-situ gel has a capacity to adhere over the mucosa with minimum dissolution with saliva up to 12 h and is capable of 95% of drug permeation capacity. Lastly FTIR and SEM images confirmed about niosomal formation with optimum stability. Conclusion: 5-Fluorouracil encapsulated niosomal in-situ gel will be superior and effective alternative to parenteral dosage forms available in the market for mouth cancer treatment.

Objective: Current work aimed to enhance solubility and stability of 5-fluorouracil drugs by preparing inclusion complex with β-cyclodextrin. Methods: In this study, inclusion complex preparation ratio selected on the basis of slope and Kc (binding constant) value in between 5-fluorouracil-β-cyclodextrin and best method out of the physical mixture, kneading method, and co-evaporation method for solubility and stability enhancement is selected on the basis of % yield, drug content, dissolution rate study and stability study. Results: Based on the phase solubility graph, a 1:1 ratio was selected for complex formation by Kc value which decided a quite stable form of a complex. The characterization of all three types of inclusion complex was performed by DSC and SEM. It proved that different moiety of the complex was formed, but all are quite stable with negligible interaction. The kneading method as the best inclusion complex at ratio 1:1 was selected after evaluating by performing percent yield and drug content and dissolution rate study for solubility profile and physical appearance, drug content, and drug release study for stability profile. Conclusion: We finally conclude that the Kc value proved that the inclusion complex is quite stable and ready to convert in any dosage form of choice. Inclusion complex formed by kneading method is one of the best options among all three techniques for solubility and stability enhancement of drug, which definitely help for a 5-fluorouracil drug to convert into a better dosage form to treat carcinoma.