Delivery of retinoic acid to LNCap human prostate cancer cells using solid lipid nanoparticles

[Display omitted] In this study retinoic acid (RTA) loaded solid lipid nanoparticles (SLNs) were optimized by tuning the process parameters (pressure/temperature) and using different lipids to develop nanodispersions with enhanced anticancer activity. The RTA-SLN dispersions were produced by high-pr...

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Published inInternational journal of pharmaceutics Vol. 493; no. 1-2; pp. 161 - 171
Main Authors Akanda, Mushfiq H., Rai, Rajeev, Slipper, Ian J., Chowdhry, Babur Z., Lamprou, Dimitrios, Getti, Giulia, Douroumis, Dennis
Format Journal Article
LanguageEnglish
Published Netherlands Elsevier B.V 30.09.2015
Subjects
Antineoplastic Agents - administration & dosage
Antineoplastic Agents - pharmacology
Calorimetry, Differential Scanning
Cell Line, Tumor
Chemistry, Pharmaceutical
Cytotoxicity
Dose-Response Relationship, Drug
Drug Carriers
Drug Liberation
Drug Stability
Flow Cytometry
Freeze Drying
Humans
Lipids - chemistry
Male
Microscopy, Electron, Transmission
Nanoparticles - chemistry
Particle Size
Prostate cancer
Prostatic Neoplasms - drug therapy
Retinoic acid
Solid lipid nanoparticles
Solubility
Tretinoin - administration & dosage
Tretinoin - pharmacology
X-Ray Diffraction
Flow cytometry
Cytotoxicity
Retinoic acid
Prostate cancer
Solid lipid nanoparticles
Online AccessGet full text

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Abstract [Display omitted] In this study retinoic acid (RTA) loaded solid lipid nanoparticles (SLNs) were optimized by tuning the process parameters (pressure/temperature) and using different lipids to develop nanodispersions with enhanced anticancer activity. The RTA-SLN dispersions were produced by high-pressure homogenization and characterized in terms of particle size, zeta potential, drug entrapment efficiency, stability, transmission electron microscopy (TEM), atomic force microscopy (AFM), X-ray diffraction (XRD) and in vitro drug release. Thermal and X-ray analysis showed the RTA to be in the amorphous state, whilst microscopic images revealed a spherical shape and uniform particle size distribution of the nanoparticles. Anticancer efficiency was evaluated by incubating RTA-SLNs with human prostate cancer (LNCap) cells, which demonstrated reduced cell viability with increased drug concentrations (9.53% at 200ug/ml) while blank SLNs displayed negligible cytotoxicity. The cellular uptake of SLN showed localization within the cytoplasm of cells and flow cytometry analysis indicated an increase in the fraction of cells expressing early apoptotic markers, suggesting that the RTA loaded SLNs are able to induce apoptosis in LNCap cells. The RTA-SLN dispersions have the potential to be used for prostate anticancer treatment.
AbstractList In this study retinoic acid (RTA) loaded solid lipid nanoparticles (SLNs) were optimized by tuning the process parameters (pressure/temperature) and using different lipids to develop nanodispersions with enhanced anticancer activity. The RTA-SLN dispersions were produced by high-pressure homogenization and characterized in terms of particle size, zeta potential, drug entrapment efficiency, stability, transmission electron microscopy (TEM), atomic force microscopy (AFM), X-ray diffraction (XRD) and in vitro drug release. Thermal and X-ray analysis showed the RTA to be in the amorphous state, whilst microscopic images revealed a spherical shape and uniform particle size distribution of the nanoparticles. Anticancer efficiency was evaluated by incubating RTA-SLNs with human prostate cancer (LNCap) cells, which demonstrated reduced cell viability with increased drug concentrations (9.53% at 200 ug/ml) while blank SLNs displayed negligible cytotoxicity. The cellular uptake of SLN showed localization within the cytoplasm of cells and flow cytometry analysis indicated an increase in the fraction of cells expressing early apoptotic markers, suggesting that the RTA loaded SLNs are able to induce apoptosis in LNCap cells. The RTA-SLN dispersions have the potential to be used for prostate anticancer treatment.
[Display omitted] In this study retinoic acid (RTA) loaded solid lipid nanoparticles (SLNs) were optimized by tuning the process parameters (pressure/temperature) and using different lipids to develop nanodispersions with enhanced anticancer activity. The RTA-SLN dispersions were produced by high-pressure homogenization and characterized in terms of particle size, zeta potential, drug entrapment efficiency, stability, transmission electron microscopy (TEM), atomic force microscopy (AFM), X-ray diffraction (XRD) and in vitro drug release. Thermal and X-ray analysis showed the RTA to be in the amorphous state, whilst microscopic images revealed a spherical shape and uniform particle size distribution of the nanoparticles. Anticancer efficiency was evaluated by incubating RTA-SLNs with human prostate cancer (LNCap) cells, which demonstrated reduced cell viability with increased drug concentrations (9.53% at 200ug/ml) while blank SLNs displayed negligible cytotoxicity. The cellular uptake of SLN showed localization within the cytoplasm of cells and flow cytometry analysis indicated an increase in the fraction of cells expressing early apoptotic markers, suggesting that the RTA loaded SLNs are able to induce apoptosis in LNCap cells. The RTA-SLN dispersions have the potential to be used for prostate anticancer treatment.
Author Chowdhry, Babur Z.
Lamprou, Dimitrios
Douroumis, Dennis
Getti, Giulia
Akanda, Mushfiq H.
Slipper, Ian J.
Rai, Rajeev
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Keywords Flow cytometry
Cytotoxicity
Retinoic acid
Prostate cancer
Solid lipid nanoparticles
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Snippet [Display omitted] In this study retinoic acid (RTA) loaded solid lipid nanoparticles (SLNs) were optimized by tuning the process parameters...
In this study retinoic acid (RTA) loaded solid lipid nanoparticles (SLNs) were optimized by tuning the process parameters (pressure/temperature) and using...
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SubjectTerms Antineoplastic Agents - administration & dosage
Antineoplastic Agents - pharmacology
Calorimetry, Differential Scanning
Cell Line, Tumor
Chemistry, Pharmaceutical
Cytotoxicity
Dose-Response Relationship, Drug
Drug Carriers
Drug Liberation
Drug Stability
Flow Cytometry
Freeze Drying
Humans
Lipids - chemistry
Male
Microscopy, Electron, Transmission
Nanoparticles - chemistry
Particle Size
Prostate cancer
Prostatic Neoplasms - drug therapy
Retinoic acid
Solid lipid nanoparticles
Solubility
Tretinoin - administration & dosage
Tretinoin - pharmacology
X-Ray Diffraction
Title Delivery of retinoic acid to LNCap human prostate cancer cells using solid lipid nanoparticles
URI https://dx.doi.org/10.1016/j.ijpharm.2015.07.042
https://www.ncbi.nlm.nih.gov/pubmed/26200751
https://search.proquest.com/docview/1708898128
Volume 493
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