Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and
Heba A Ghanem1, Ali M Nasr2,3, Tamer H Hassan4
1Department of Pharmaceutics, Faculty of Pharmacy, Sinai University, Al Qantarah Sharq 41636, Egypt.
Pharmaceutics
|February 2, 2021
Summary
This study optimized Atorvastatin-loaded nanostructured lipid carriers (AT-NLCs) for improved drug delivery. The developed AT-NLCs effectively reduced cholesterol and triglycerides in rats, showing potential for cardiovascular disease treatment.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Drug Delivery Systems
Background:
- Hyperlipidemia is a major risk factor for cardiovascular diseases.
- Nanostructured lipid carriers (NLCs) offer enhanced drug delivery and stability.
- Atorvastatin is a widely used statin for managing hyperlipidemia.
Purpose of the Study:
- To develop and optimize Atorvastatin-loaded nanostructured lipid carriers (AT-NLCs).
- To evaluate the physicochemical properties and in vivo efficacy of AT-NLCs.
- To establish a robust experimental design for NLC formulation.
Main Methods:
- Utilized D-optimal screening and central composite designs for formulation optimization.
- Investigated factors including lipid composition, surfactant concentration, and processing parameters.
- Characterized AT-NLCs for particle size, PDI, zeta potential, and entrapment efficiency.
- Assessed drug-excipient compatibility using FTIR and DSC.
- Evaluated in vivo lipid-lowering effects in a rat model.
Main Results:
- Optimized AT-NLCs exhibited nanometric size (83.80 nm), favorable PDI (0.38), negative zeta potential (-29.65 mV), and high entrapment efficiency (93.1%).
- FTIR and DSC confirmed no chemical interactions and amorphous state of Atorvastatin within NLCs.
- Oral administration of AT-NLCs significantly reduced serum total cholesterol, triglycerides, and LDL levels in rats (p < 0.001).
- Histological analysis confirmed reduced liver steatosis.
Conclusions:
- The developed experimental design effectively optimized AT-NLCs.
- Optimized AT-NLCs demonstrate excellent physicochemical properties and high Atorvastatin loading.
- AT-NLCs show significant potential as an effective drug delivery system for hyperlipidemia management.
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