To augment oral bioavailability, linagliptin (LGP) loaded solid lipid nanoparticles (SLNs) have been formed using the solvent evaporation technique of emulsification. Utilizing the Box Behken design (BBD), examining the relation between independent and dependent variables was possible. Particle size (PS), entrapment efficiency (EE), and in-vitro drug release (DR) studies were considered response factors, whereas the various concentrations of lipid carrier, surfactant, and co-surfactant were considered process variables for optimization. The design expert program was used to obtain the optimized batch. At 24 hours, it was discovered that the optimized batch expected responses for PS, %EE, and %DR were 105.83 nm, 81.19, and 96.69%, respectively. The observed PS, %EE, and %DR responses of the optimized batch at 24 hours were determined to be 101.36 nm, 80.56, and 96.31%, respectively. There is no interaction seen in the basic physical mixing of drug and polymer, according to the FTIR spectra of pure drugs, polymers, and drug and polymer mixtures. The optimized formulation’s average size was found to be 138 nm by the particle size analysis. Similarly, a value of 0.255 was found by the polydispersity index (PDI). This suggests that the SLN in the formulation has a homogeneous size dispersion. With a zeta value of -32.8 mV, stability is indicated. Linagliptin was effectively developed as a drug with a 24-hour sustained release. Wistar rats were used in the in-vivo evaluation of linagliptin SLN formulations. The drug bioavailability increased five times (a highly significant fivefold increase) in LGP-loaded SLNs (AUC0-t ≈ 134.5 μg*h/mL) compared to raw LGP (AUC0-t = 27.23 μg*h/mL).
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