Development of Curcumin-Loaded Solid Lipid Nanoparticles Utilizing Glyceryl Monostearate as Single Lipid Using QbD Approach: Characterization and Evaluation of Anticancer Activity Against Human Breast Cancer Cell Line

May 8, 2018Current drug delivery

Curcumin-packed solid lipid nanoparticles made with glyceryl monostearate: design, testing, and effects on human breast cancer cells

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mRNA Technology on OpenScience ↗PubMed ↗DOI ↗

Abstract

The optimized solid lipid nanoparticles (SLNs) demonstrated a particle size of 226.802±3.92 nm and encapsulated curcumin at a rate of 67.88±2.08%.

The SLNs showed a low polydispersity index of 0.244±0.018, indicating uniform particle size distribution.
Differential scanning calorimetry, Fourier Transform Infra-red Spectroscopy, and X-Ray Diffraction confirmed stable encapsulation of curcumin within the lipid matrix.
Sustained drug release was observed for curcumin-loaded SLNs compared to free curcumin solution.
Higher cellular uptake of curcumin was noted in human breast adenocarcinoma cells when delivered via SLNs compared to free curcumin at both 1 and 4 hours.
Treatment with curcumin-loaded SLNs resulted in decreased cell viability (43.97±1.53%) compared to free curcumin (59.33±0.95%) at a concentration of 50 µg/mL after 24 hours.
Curcumin-loaded SLNs induced significantly higher apoptosis (37.28±5.3%) in cancer cells compared to free curcumin (21.06±0.97%).

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BACKGROUND: Solid lipid nanoparticles (SLNs) represent an affordable, easily scalable, stable and biocompatible drug delivery system with a high drug to lipid ratio which also improves solubility of poorly soluble drugs.

OBJECTIVE: SLNs were developed by using glyceryl monostearate as the single lipid in the presence of surfactant Poloxamer 188 and evaluated the efficiency of SLNs to load the therapeutic cargo, curcumin (CUR).

METHOD: The nano-formulation was optimized by Quality by Design approach to understand the effect of various process parameters on various quality attributes, including drug loadability, particle size and polydispersity. The nanoparticles were characterized using Differential scanning calorimetry (DSC), Fourier Transform Infra-red Spectroscopy (FT-IR) and X-Ray Diffraction (XRD) analysis. These novel SLNs were evaluated for in-vitro anticancer activity using breast adenocarcinoma cells (MDA-MB-231).

RESULTS: The optimized formulation had a particle size of 226.802±3.92 nm with low polydispersity index of 0.244±0.018. The % encapsulation of CUR into SLNs was found to be 67.88±2.08 %. DSC, FT-IR and XRD confirmed that the CUR was encapsulated stably into the lipid matrix, thereby improving the solubility of the drug. CUR-SLN showed sustained drug release in comparison to the free CUR solution. CUR-SLNs exhibited higher cellular uptake in human breast adenocarcinoma cells compared to free CUR at both 1 and 4 h time points. CUR-SLNs demonstrated decreased cell viability (43.97±1.53%) compared to free CUR (59.33±0.95%) at a concentration of 50 µg/mL after 24 h treatment. Furthermore, the treatment of MDA-MB-231 cells with CUR-SLNs for 24 h induced significantly higher apoptosis (37.28±5.3%) in cells compared to the free CUR (21.06±0.97%).

CONCLUSION: The results provide a strong rationale for further exploration of the newly developed CUR-SLN to be utilized as a potent chemotherapeutic agent in cancer therapy.

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Development of Curcumin-Loaded Solid Lipid Nanoparticles Utilizing Glyceryl Monostearate as Single Lipid Using QbD Approach: Characterization and Evaluation of Anticancer Activity Against Human Breast Cancer Cell Line

Abstract

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