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DOI:
10.4314/tjpr.v14i4.3Keywords:
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Main Article Content
Development and Evaluation of Solid Self Nano- Emulsifying Formulation of Rosuvastatin Calcium for Improved Bioavailability
Abstract
Purpose: To develop rosuvastatin calcium-loaded self-nanoemulsifying powder for improved oral delivery of the drug.
Methods: Solubility study was carried out in different oils, surfactants and co-surfactants. Based on the solubility study, liquid formulations were prepared using LAS/Capryol 90: Maisine 35-1 as oil phase and Tween 20 with Lutrol E400 as surfactant mixture (Smix). The liquid formulations were adsorbed onto Aerosil 200 in a ratio of 1: 0.25 % w/w to convert them into a solid form. The formulations were evaluated for globule size, zeta potential, and emulsion properties. Transmittance study, scanning electron microscopy, and in-vitro dissolution studies were carried out. Biochemical studies were carried out using a triton-induced hyperlipidemia model in Wistar rats.
Results: The developed formulations exhibited some desirable characteristics of self-emulsifying systems with nano-sized globules in the range 119.8 to 228.9 nm, rapid emulsification in approximately 60 s and transmittance of close to 100 %. In-vitro dissolution studies on the developed formulations indicate a 4-fold increase in drug release in 10 min, compared to the pure drug (ROC) while pharmacodynamic data showed significant improvement in oral bioavailability compared to the pure drug.
Conclusion: The developed formulation containing the oils, LAS and combination of capryol 90 with Maisine 35-1, has the capability to improve the solubility and bioavailability of rosuvastatin calcium when formulated as a self-nanoemulsifying product.
Keywords: Rosuvastatin, Particle size, Zeta potential, Nanoemulsion, Oral bioavailability,
Hyperlipidemia, Pharmacodynamics, Surfactants, Co-surfactants
