Non-lamellar lyotropic liquid crystalline nanoparticles as nanocarriers for enhanced drug encapsulation of atorvastatin calcium and proanthocyanidins
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View abstract on PubMed
Summary
This summary is machine-generated.Lyotropic liquid crystalline nanoparticles effectively encapsulate atorvastatin calcium and proanthocyanidins, improving drug delivery for atherosclerosis treatment. These nanoparticles demonstrate tunable structures and enhanced biological activity, offering a promising alternative drug platform.
Area Of Science
- Nanotechnology and Drug Delivery
- Materials Science
- Biomedical Engineering
Background
- Atorvastatin calcium (ATV) and proanthocyanidins (PAC) show antioxidant properties beneficial for atherosclerosis but face bioavailability challenges.
- ATV exhibits poor solubility, while PAC is unstable when exposed to atmospheric oxygen, limiting their therapeutic efficacy.
- Existing drug delivery systems struggle to effectively encapsulate both hydrophobic ATV and hydrophilic PAC simultaneously.
Purpose Of The Study
- To develop and characterize lyotropic liquid crystalline nanoparticles (LLCNPs) using soy phosphatidylcholine (SPC) and citrem for co-encapsulating ATV and PAC.
- To investigate the effect of citrem/SPC ratios on LLCNP structure, drug encapsulation efficiency, and drug release kinetics.
- To evaluate the biological activity, specifically the impact on TNF-α expression, of the drug-loaded LLCNPs.
Main Methods
- LLCNPs were formulated using binary mixtures of SPC and citrem at varying weight ratios.
- Small-angle X-ray scattering and dynamic light scattering were employed for structural and size characterization.
- Encapsulation efficiency, drug release profiles, and TNF-α expression were analyzed for ATV- and PAC-loaded LLCNPs.
Main Results
- LLCNPs successfully encapsulated both ATV and PAC with efficiencies ranging from 90-100%.
- The nanoparticle structure transitioned from hexosomes (H2) to inverse micellar (L2) with increasing citrem content.
- Optimal encapsulation efficiencies were achieved at specific citrem/SPC ratios (4:1 for ATV, 1:1 for PAC), with notable colloidal instability observed in ATV-loaded LLCNPs over 30 days.
- ATV-loaded LLCNPs exhibited biphasic release, while PAC-loaded LLCNPs showed burst release.
- PAC-LLCNPs significantly upregulated TNF-α expression compared to controls.
Conclusions
- Citrem/SPC-based LLCNPs provide a versatile platform for co-delivering hydrophobic and hydrophilic drugs like ATV and PAC.
- The tunable nanoparticle structure influences drug release patterns and biological activity.
- These LLCNPs demonstrate potential as an alternative drug delivery system for atherosclerosis treatment, particularly due to the enhanced TNF-α modulation by PAC-LLCNPs.
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