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. 2022 Jun 29;7(27):23643-23652.
doi: 10.1021/acsomega.2c02242. eCollection 2022 Jul 12.

Simvastatin-Loaded Lipid Emulsion Nanoparticles: Characterizations and Applications

Faiz Ullah  1 , Muhammad Farhan Ali Khan  2 , Nazeer Hussain Khan  3   4 , Muhammad Fayyaz Rehman  5 , Syed Sakhawat Shah  1 , Muhammad Mustaqeem  6 , Sami Ullah  7 , Qidi Zhang  8 , Hongchao Shi  9
Affiliations

Simvastatin-Loaded Lipid Emulsion Nanoparticles: Characterizations and Applications

Faiz Ullah et al. ACS Omega. .

Abstract

Simvastatin (SIM) is a diet drug to treat high lipid levels in the blood. It has the drawback of being metabolized in humans' gastrointestinal tract (GIT) when taken in an oral dosage form. To enhance the role of SIM in treating hyperlipidemias and bypassing its metabolism in GIT, a biodegradable nanocarrier as a SIM-loaded lipid emulsion nanoparticle via the solvent injection method was designed. Cholesterol acts as a lipid core, and Tween 80 was utilized to stabilize the core. The optimized nanoformulation was characterized for its particle diameter, zeta potential, surface morphology, entrapment efficiency, crystallinity, and molecular interaction. Furthermore, the transdermal hydrogel was characterized by physical appearance, rheology, pH, and spreadability. In vitro assays were executed to gauge the potential of LENPs and olive oil for transdermal delivery. The mean particle size and zeta potential of the optimized nanoparticles were 174 nm and -22.5 mV 0.127, respectively. Crystallinity studies and Fourier transform infrared analyses revealed no molecular interactions. Hydrogels showed a sustained release compared to SIM-loaded LENPs that can be proposed as a better delivery system for SIM. We encourage further investigations to explore the effect of reported formulations for transdermal delivery by in vivo experiments.

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Conflict of interest statement

The authors declare no competing financial interest.

Figures

Figure 1
Figure 1
Association between surfactant percentage, lipid concentration, temperature, and size of nanoparticles.
Figure 2
Figure 2
(a) Particle size and PDI of the selected blank nanoparticle. (b) Particle size and PDI of the selected drug-loaded nanoparticle.
Figure 3
Figure 3
Zeta potential of optimized emulsion.
Figure 4
Figure 4
FTIR spectrum for both B-LENPs and medication-loaded LENPs (D-LENPs).
Figure 5
Figure 5
DSC spectrum of LENs, lipid, and drug (SIM).
Figure 6
Figure 6
X-ray diffraction spectrum of LENs, lipid, and drug (SIM).
Figure 7
Figure 7
Viscosity of SIM-LENP gel at different shear rates.
Figure 8
Figure 8
Spreadability of SIM-LENP gel.
Figure 9
Figure 9
Swelling index of SIM-LENP gel at different time intervals.
Figure 10
Figure 10
In vitro release profile of SIM.
Figure 11
Figure 11
Fabrication of drug (SIM)-loaded LENPs.
Figure 12
Figure 12
Fabrication of SIM-loaded hydrogels.
See this image and copyright information in PMC

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