Formulation design and characterization of self nano emulsifying drug delivery system (SNEDDS) roxitromycin using capryol–90, polysorbat–80 and PEG–400

Background

Roxithromycin is a macrolide antibiotic included in the biopharmaceutics classification system (BCS) class II with poor water solubility (0.0189 mg/mL) resulting poor solubility of roxithromycin in gastrointestinal track and decreases bioavailability. Technology development of self nano emulsifying drug delivery system (SNEDDS) to reduce particle size has known effectively for increasing drug solubility.

Methods

An optimum formulation of this reseach were determined by simplex lattice design method in Design Expert®10. Investigated factors were solubility of roxithromycin in capryol-90 and in mixture of polysorbat-80 and PEG-400 also the ternary phase of capryol-90:polysorbat-80:PEG-400. The emulsification system was performed by ultrasonication. The characters of SNEDS were determined by dynamic light scattering and transmission electron microscopy. The thermodynamic stability test was performed by heating-cooling cycle.

Results

Capryol–90 could dissolve roxithromycin properly (2.355±0.040 mg/mL). Polysorbate–80, and PEG–400 also could increase the solubility of roxithromycin in water. Determination of ternary phase diagram to obtain combination proportions formed a spontaneous range of 10 – 60% capryol–90, 20 – 50% polysorbate–80, and 10 – 70% PEG–400. Proportion of optimum roxithromycin SNEDDS formula obtained from simplex lattice® design was resulted 20.00% capryol–90, 60.00% polysorbate–80, and 20.00% PEG–400. Characterization of optimum formula resulted percent of transmittance (80.60 ± 0.35)%, emulsification time (71.70 ± 0.99) second, viscosity (3.76 ± 0.02) cP, pH (7.84 ± 0.07), and robustness to dilution in aquadest, SGF, and SIF (99.16 ± 0.67)%, (93.23 ± 0.14)%, and (98.34 ± 0.34)%. Dissolution test showed that SNEDDS could improve dissolution of roxithromycin in SIF pH 7.4 compared to pure and generic tablet.

Conclusions

Proportion of optimum roxithromycin SNEDDS was resulted 20.00% capryol–90, 60.00% polysorbate–80, and 20.00% PEG–400. Dissolution profile showed that SNEDDS could improve dissolution of roxithromycin in SIF pH 7.4 compared to pure and generic tablet.

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Article Information: Mardiyanto Mardiyanto, Najma Annuria Fithri, Duha Inda Misdwima; Department of Pharmacy Faculty of Science Sriwijaya University, Kampus UNSRI Indralaya JL Raya Palembang-Prabumulih KM32 South Sumatra, 2019.

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