• Journal of Powder Materials
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• v.30 no.4
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• pp.305-309
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• 2023

This study aims to prepare a colloidal silica-containing powder to enhance the solubility and dissolution rate of rivaroxaban using a self-nanoemulsifying drug delivery system (SNEDDS). We investigate the impact of colloidal silica on a nanoemulsion system for preparing powdered SNEDDS. The liquid SNEDDS comprises 30/20/50 (w/w/w) Peceol/Cremophor RH40/Tween 80, which results in the formation of the smallest droplets. Three powdered SNEDDS formulations are prepared by suspending the liquid SNEDDS formulation using colloidal silica and spray drying. The powdered SNEDDS prepared with liquid SNEDDS and colloidal silica at a ratio of 1/0.5 (w/w) exhibits the highest water solubility (0.94 ± 0.62 vs. 26.70 ± 1.81 ㎍/mL) and dissolution rate (38.4 ± 3.6 vs. 85.5 ± 3.4%, 45 min) when compared to the drug alone. Morphologically, the liquid SNEDDS is adsorbed onto colloidal silica and forms smaller particles. In conclusion, an SNEDDS containing rivaroxaban, prepared using colloidal silica, facilitates the creation of a nanoemulsion and enhances the water solubility of rivaroxaban. Accordingly, this technology holds significant potential for commercialization.

• Journal of Powder Materials
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• v.30 no.6
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• pp.493-501
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• 2023

This study aimed to develop a solid self-nanoemulsifying drug delivery system (solid-SNEDDS) to enhance the formulation of ketoconazole (KTZ), a BCS Class II drug with poor solubility. Ketoconazole, which is insoluble above pH 3, requires solubilization for effective delivery. This SNEDDS comprises oil, surfactant, and co-surfactant, which spontaneously emulsify in the gastrointestinal tract environment to form nanoemulsions with droplet sizes less than 100 nm. The optimal SNE-vehicle composition of oleic acid, TPGS, and PEG 400 at a 10:80:10 weight ratio was determined based on the smallest droplet size achieved. This composition was used to prepare liquid SNEDDS containing ketoconazole. The droplet size and polydispersity index (PDI) of the resulting liquid SNEDDS were analyzed. Subsequently, solid-SNEDDS was fabricated using a spray-drying method with solidifying carriers such as silicon dioxide, crospovidone, and magnesium alumetasilicate. The physicochemical properties of the solid-SNEDDS were characterized by scanning electron microscopy and powder X-ray diffraction, and its solubility, droplet size, and PDI were evaluated. In particular, the solid-SNEDDS containing ketoconazole and crospovidone in a 2:1 weight ratio exhibited significantly enhanced solubility, highlighting its potential for improved medication adherence and dissolution rates.

• Journal of Life Science
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• v.31 no.5
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• pp.502-510
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• 2021

The objective of this study was to develop a novel ticagrelor-loaded self-nanoemulsifying drug delivery system with an enhanced solubility and dissolution rate. Numerous oils and surfactants were screened, then medium chain triglyceride (MCT) oil and the surfactants polyoxyethylene sorbitan monooleate (Tween 80) and Labrafil M1944CS were selected for the preparation of the ticagrelor-loaded self-nanoemulsifying drug delivery system. A pseudo-ternary phase diagram was constructed to detect the nanoemulsion region. Of the various formulations tested, the liquid SNEDDS, composed of MCT (oil), Tween 80 (surfactant), and Labrafil M1944CS (cosurfactant) at a weight ratio of 20/70/10 produced the smallest emulsion droplet size (around 20.56±0.70 nm). Then, particle size, polydispersity, and zeta potential were measured using drugs containing liquid SNEDDS. The selected ticagrelor-loaded liquid SNEDDS was spray-dried to convert it into a ticagrelor-loaded solid SNEDDS with a suitable inert carrier, such as silicon dioxide, calcium silicate, or magnesium aluminometasilicate. The solid SNEDDS was characterized by scanning electron microscopy, transmission electron microscopy, and in vitro dissolution studies. SEM, PXRD, and DSC results suggested that amorphous ticagrelor was present in the solid SNEDDS. Also, the solid SNEDDS significantly increased the dissolution rate of ticagrelor. In particular, the emulsion particle size and the polydispersity index of the solid SNEDDS using silicon dioxide (SS1) as a carrier was the smallest among the evaluated solid SNEDDS, and the flowability and compressibility result of the SS1 was the most suitable for the manufacturing of solid dosage forms. Therefore, solid SNEDDS using silicon dioxide (SS1) could be a potential nano-sized drug delivery system for the poorly water-soluble drug ticagrelor.

• Biomolecules & Therapeutics
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• v.21 no.2
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• pp.173-179
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• 2013

Objective of present study was to prepare and characterize self-nanoemulsifying drug delivery system (SNEDDS) of lutein and to evaluate its effect on bioavailability of warfarin. The SNEDDS was prepared using an oil, a surfactant, and co-surfactants with optimal composition based on pseudo-ternary phase diagram. Effect of the SNEDDS on the bioavailability of warfarin was performed using Sprague Dawley rats. Lutein was successfully formulated as SNEDDS for immediate self-emulsification and dissolution by using combination of Peceol as oil, Labrasol as surfactant, and Transcutol-HP or Lutrol-E400 as co-surfactant. Almost complete dissolution was achieved after 15 min while lutein was not detectable from the lutein powder or intra-capsule content of a commercial formulation. SNEDDS formulation of lutein affected bioavailability of warfarin, showing about 10% increase in $C_{max}$ and AUC of the drug in rats while lutein as non-SNEDDS did not alter these parameters. Although exact mechanism is not yet elucidated, it appears that surfactant and co-surfactant used for SNEDDS formulation caused disturbance in the anatomy of small intestinal microvilli, leading to permeability change of the mucosal membrane. Based on this finding, it is suggested that drugs with narrow therapeutic range such as warfarin be administered with caution to avoid undesirable drug interaction due to large amount of surfactants contained in SNEDDS.

• Journal of Pharmaceutical Investigation
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• v.40 no.5
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• pp.263-267
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• 2010

Nanoemulsions have been widely investigated for many years because of their attractive and unique characteristics. Nanoemulsions are composed of oil, surfactant, co-surfactant and water. Especially, cosurfactant plays a critical role in formation of nanoemulsions. In pharmaceutical area, a pre-concentrate form of nanoemulsions which is known as self-nanoemulsifying drug delivery systems (SNEDDS) was available for some water-insoluble drugs. In this study, we investigated the functional behaviors of cosurfactant in design of SNEDDS and nanoemulsions. Cremophor RH 40$^{(R)}$, Propylene carbonate and medium chain triglyceride were selected for surfactant, cosurfactant and oil, respectively. Cyclosporine was employed as a drug. Phase diagrams showed the area of isotropic o/w region which forms o/w nanoemulsions was not significantly affected by the compositional ratio of cosurfactant. But, drug solubilization capacity, droplet size of nanoemulsions and drug release rate were greatly affected by the cosurfactant.