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Development of Oral Self-Nanoemulsifying Drug Delivery System (SNEDDS) Of Rosuvastatin Calcium: Formulation, Characterization, And In-Vitro Drug Release Study
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| Author:
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ADNAN BURHAN QADER, AHMED ABBAS HUSSEIN
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| Abstract:
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Background and Objective: rosuvastatin calcium is a very effective anti-hyperlipidemic agent, however, being a biopharmaceutical classification system (BCS) class II drug, results in poor solubility and poor oral bioavailability. This study aims to develop and optimize a self-nanoemulsifying drug delivery system (SNEDDS) for the enhancement of rosuvastatin calcium solubility and dissolution rate.
Methods: in this study, self-nanoemulsifying drug delivery system (SNEDDS) containing rosuvastatin calcium along with garlic oil was formulated. Ternary phase diagrams were constructed based on rosuvastatin calcium solubility analysis for optimizing the system. Based on the preliminary screening of different unloaded SNEDDS formulas, eight formulas of rosuvastatin loaded SNEEDS were prepared using a mixture of garlic oil and Stepan-Mild® GCC (1:1) as oil phase, tween 80 as a surfactant and PEG 400 as co-surfactant. The prepared formulas were evaluated for robustness to dilution, efficiency of self-emulsification, turbidity measurement, drug loading ef?ciency, globule size determination, polydispersity index (PDI), zeta potential analysis, surface morphology, and in-vitro dissolution release study.
Results: results showed that the prepared SNEDDS was robust in different pH media and dilution volume, with good self-emulsification efficiency, good optical clarity (99.86 – 95.40 %), high drug loading ef?ciency (98.05 – 94.20 %), the mean globule size of SNEDDS was found to be in the nanometric range (48.32 – 73.64 nm) with optimum PDI values (0.215 – 0.448). All formulas also showed acceptable Zeta Potentials (-29.50 to -38.90). TEM analysis revealed the formation of spherical and homogeneous globules with a size smaller than 100 nm. In-vitro release of rosuvastatin from SNEDDS formulas showed that more than 75% of rosuvastatin released in approximately 30 min.
Conclusion: rosuvastatin SNEDDS formulas exhibited an enhanced release. Thus, this greater availability of dissolved rosuvastatin from the SNEDDS formulation could lead to higher absorption and higher oral bioavailability.
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| Keyword:
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rosuvastatin calcium, Self - Nano Emulsifying Drug Delivery System (SNEDDS), Bioavailability and Biopharmaceutical Classification Systems(BCS).
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| EOI:
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| DOI:
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https://doi.org/10.31838/ijpr/2021.13.01.296
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| Download:
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