Objectives: To enhance solubility, dissolution, and permeability of poorly water-soluble drug Ezetimibe (EZE) using a self-nano emulsifying drug delivery system (SNEDDS). Methods: Initially, the solubility of the EZE was determined in various oils and buffers. Surfactants and co-surfactants were screened based on the solubility of the drug in oil as per the emulsification efficacy test. Liquid SNEDDS was developed and characterized. Solid SNEDDS was developed and characterized using optimized liquid SNEDDS followed by the development of EZE-loaded Tablet SNEDDS. Finding: Liquid SNEDDS (L-SNEDDS) was formulated using Capmul MCM C8 EP, Cremophore RH 40, and Labrafil M 2125 CS as oil, surfactant, and co-surfactant respectively. Optimized L-SNEDDS formulation was found to be efficient with an average %T of 99.5%, drug content of 98.43%, flask inversion 0 numbers, and the average particle size of 36.7 nm, zeta potential of -57.5 mV, Polydispersibility index in of 0.119. Also, the in vitro release profile of drug from L-SNEDDS encapsulated in hard gelatin capsules was evaluated in different dissolution media viz. simulated gastric fluid and simulated intestinal fluid. For the drug, more than 95% cumulative release was observed within 30 min exclusive of the pH of the medium. The L-SNEDDS were adsorbed on a solid support and then mixed with tablet blends and compressed into tablets. Further, no adverse changes in globule size, shape, the zeta potential of SNEDDS, and dissolution profile were apparent on conversion to solid powder form and tablet form. Novelty: The developed liquid SNEDDS form of EZE showed enhanced solubility, dissolution, and permeability in comparison to pure drugs. Conversion of L-SNEDDS to P-SNEDDS would be a novel approach to overcome the limitations associated https://www.indjst.org/ 1504
Objective: To improve solubility, dissolution, and permeability of BCS class II drug Itraconazole (ITZ) using a self solidifying self nano emulsifying drug delivery system (SNEDDS). Method: The solubility of ITZ was assessed in oils, surfactants, co-surfactants, and buffers. Surfactants, co-surfactants, and combination of surfactants (S-comb) were selected on the basis of emulsification efficacy test. The ability to solidify self emulsifying mixture was assessed and solid SNEDDSS was developed and optimised. Finding: Solubility of ITZ was found maximum in 0.1N HCl (0.120 ± 0.07mg/mL) followed by SGF (0.089 ± 0.01mg/mL). Out of 20 oils screened, Peceol showed highest solubility. Among all surfactants and co-surfactants studied, Labrafil M 1944 CS (LM 1944) showed highest potential to solubilize ITZ (14.91 mg/g). The globule size of the optimised formulation was found to be 40.11 nm with PDI of 0.144. Zeta potential study revealed the stability of the SNEDDS. Drug content of solid SNEDDS of ITZ was found within the range of 98.11% to 102.51%, which was found in the acceptable limit. It was observed that ITZ solid SNEDDS (S-SNEDDS) showed a promising improvement in the in vitro dissolution profile compared to the plain ITZ and marketed product in all three-dissolution media. Nearly 3-fold enhancement of permeability of ITZ was attributed by uniformly dispersed globules with nano size. Analytical characterization demonstrated that the drug and excipients are compatible with amorphous characteristics of the ITZ. Novelty: The developed self solidifying SNEDDS of ITZ showed enhanced solubility, dissolution, and permeability in comparison to the pure drugs (ITZ). Self solidifying SNEDDS would be a novel approach to overcome the limitations associated with liquid dosage forms.
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