Abstract
Rosuvastatin calcium (Rsv) is an effective statin, with a potent antihyperlipidemic effect. However, it suffers poor bioavailability owing to its poor solubility. Thus; encapsulating Rsv into a nanovesicular structure could overcome this problem. The aim of this work is to investigate the potential of solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) in enhancing the solubility of Rsv, using the quality by design (QbD) concept. A complete risk assessment study has been conducted, where the critical process parameters (CPPs), material attributes (MAs), and critical quality attributes have been identified using Ishikawa diagrams. Selected CPPs/MAs were screened and further upgraded to a 24 full-factorial design to develop a design space with the optimized formula. The screened CPPs/MAs were tested on the particle size, the polydispersity index (PDI), the zeta potential (ζ-pot), and the entrapment efficiency (EE%). A comprehensive approach for Rsv nanovesicular carriers has been conducted, where the NLCs showed better results than the SLNs. The optimized formula was prepared with 3% total lipid content, 0.154% surfactant, and 9.4 mg drug. The optimized formula had a particle size of 310.5 nm, with 0.243 PDI, a ζ-pot of −24.7 mV, and an EE% of 93.87%, and showed a sustained release of the drug for up to 72 h. It successfully lowered total cholesterol, low density lipoprotein, and triglycerides, and elevated the levels of high density lipoprotein in rats, with better results as compared to the standard drug. Thus, a complete QbD study was conducted to explore experimental regions for many successful nanovesicular carriers for the enhancement of the solubility of poorly soluble drugs.
Highlights
Quality by design (QbD) is a systematic science and risk-based approach that plays a great role in product and process understanding in order to achieve a safe product
The nanostructured lipid carriers (NLCs) optimized formula was able to release the drug in a sustained manner, as compared to the standard Rosuvastatin calcium (Rsv) (Figure 2)
The drug on the surface of the vesicles resulted in an initial burst release which was followed by a sustained release pattern [18]
Summary
Quality by design (QbD) is a systematic science and risk-based approach that plays a great role in product and process understanding in order to achieve a safe product. The use of QbD in pharmaceutical formulation assures the quality of a pharmaceutical product through the use of scientific development and risk management tools, producing a high quality product in the most efficient manner [1]. Rosuvastatin calcium (Rsv) is one of the most effective statins, with the potential of reducing low-density lipoprotein (LDL), triglycerides (TGs), and increasing high-density lipoprotein (HDL). Rsv suffers from poor solubility and extensive first-pass effect, resulting in its poor bioavailability [2]. The objective of the current study is the application of a QbD approach in the optimization and formulation of Rsv; in an attempt to improve its solubility Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are vesicular nanoparticles made from physiologically accepted and biodegradable lipid fractions [3].
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