Potential Use of Nanostructured Lipid Carriers for Topical Delivery of Flurbiprofen

González‐Mira, Elisabet; Nikolic, Sasha; García, María L.; Egea, M.A.; Souto, Eliana B.; Calpena, Ana Cristina

doi:10.1002/jps.22271

Cited by 76 publications

(20 citation statements)

References 32 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…We also found that the tumor inhibition rate was much greater in mice treated with CT-NLC and T-NLC at low doses (2 mg/kg) than in mice treated with free tripterine at a high (4 mg/kg) dose (P,0.05), especially in the CT-NLC group. The higher antitumor activity of CT-NLC and T-NLC may be attributable to the following: the structure of NLC, which contains a liquid and solid lipid core, could increase the solubility and stability of tripterine and improve its oral absorption; 29 the optimal particle size of NLC could enhance the accumulation and penetration of tripterine into the tumor area via the EPR effect; 26 and tripterine, released slowly from NLC, would be maintained at a constant concentration for a relatively long period in vivo, thereby having consistent antitumor efficacy. Further, Ste-R 6 L 2 (a type of CPP composed mainly of arginine and leucine) could confer a positive charge to the nanoparticles.…”

Section: Discussionmentioning

confidence: 99%

Antitumor activity of tripterine via cell-penetrating peptide-coated nanostructured lipid carriers in a prostate cancer model

Yuan¹,

Liu²,

Chen³

et al. 2013

IJN

View full text Add to dashboard Cite

Background The purpose of this study was to evaluate the antitumor effect of cell-penetrating peptide-coated tripterine-loaded nanostructured lipid carriers (CT-NLC) on prostate tumor cells in vitro and in vivo. Methods CT-NLC were developed to improve the hydrophilicity of tripterine. The antiproliferative effects of CT-NLC, tripterine-loaded nanostructured lipid carriers (T-NLC), and free tripterine in a human prostatic carcinoma cell line (PC-3) and a mouse prostate carcinoma cell line (RM-1) were evaluated using an MTT assay. The advantage of CT-NLC over T-NLC and free tripterine with regard to antitumor activity in vivo was evaluated in a prostate tumor-bearing mouse model. The induced tumor necrosis factor-alpha and interleukin-6 cytokine content was investigated by enzyme-linked immunosorbent assay to determine the effect of CT-NLC, T-NLC, and free tripterine on immune responses. Histologic and TUNEL assays were carried out to investigate the mechanisms of tumor necrosis and apoptosis. Results CT-NLC, T-NLC, and free tripterine showed high antiproliferative activity in a dose-dependent manner, with an IC 50 of 0.60, 0.81, and 1.02 μg/mL in the PC-3 cell line and 0.41, 0.54, and 0.89 μg/mL in the RM-1 cell line after 36 hours. In vivo, the tumor inhibition rates for cyclophosphamide, high-dose (4 mg/kg) and low-dose (2 mg/kg) tripterine, high-dose (4 mg/kg) and low-dose (2 mg/kg) T-NLC, high-dose (4 mg/kg) and low-dose (2 mg/kg) CT-NLC were 76.51%, 37.07%, 29.53%, 63.56%, 48.25%, 72.68%, and 54.50%, respectively, showing a dose-dependent pattern. The induced tumor necrosis factor-alpha and interleukin-6 cytokine content after treatment with CT-NLC and T-NLC was significantly higher than that of high-dose tripterine. Moreover, CT-NLC showed the expected advantage of inducing necrosis and apoptosis in prostate tumor cells. Conclusion CT-NLC noticeably enhanced antitumor activity in vitro and in vivo and showed dramatically improved cytotoxicity in normal cells in comparison with free tripterine. In summary, CT-NLC could be used as a promising drug delivery system for the treatment of prostate cancer.

show abstract

Section: Discussionmentioning

confidence: 99%

Antitumor activity of tripterine via cell-penetrating peptide-coated nanostructured lipid carriers in a prostate cancer model

Yuan¹,

Liu²,

Chen³

et al. 2013

IJN

View full text Add to dashboard Cite

show abstract

“…Inhibition of COX-1 and COX-2 leads to anti-inflammatory, analgesic and antipyretic effects (Knights et al, 2010). This NSAID agent is widely used as painkiller in diseases such as gout, osteoarthritis and rheumatoid arthritis; It is also used in the treatment of sunburn (Gonzalez-Mira et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Investigation of flurbiprofen genotoxicity and cytotoxicity in rat bone marrow cells

Timocin

İla

2014

Drug and Chemical Toxicology

View full text Add to dashboard Cite

This study was performed to investigate cytogenetic effects of NSAID flurbiprofen which was used as active ingredient in some analgesic, antipyretic and anti-inflammatory drugs. Genotoxic effect of flurbiprofen was investigated using in vivo chromosome aberration (CA) test and random amplified polymorphic DNA-polymerase chain reaction (RAPD-PCR) test. Also, oxidative stress potential of flurbiprofen was determined by measuring total oxidant and antioxidant level which occurred with flurbiprofen treatment in rat peripheral blood. For these purposes, rats were treated with three concentrations of flurbiprofen (29.25, 58.50 and 117 mg/kg, body weight) in single dose at two different treatment periods (12 and 24 h). According to the results, flurbiprofen did not affect chromosome aberrations in rat bone marrow cells with CA test. In RAPD-PCR test, polymorphic bands were unaffected. Also, test substance did not change total oxidant and antioxidant status (except for 58.50 and 117 mg/kg, 12 h) and therefore it did not lead to significant increase on oxidative stress (again except 58.50 and 117 mg/kg, 12 h). However, flurbiprofen reduced to mitotic indexes and these reductions were dose-dependent for 12 h treatment. In summary, flurbiprofen did not show significant genotoxic effect. But it caused cytotoxicity in rat bone marrow cells.

show abstract

“…Owing to their small size, they act as occlusives, i.e., they form a film on the skin and thereby enhance the penetration of drugs through stratum corneum. Further, they have skin deposition potential and work well for sustained release owing to the possible formation of a drug reservoir (Khurana et al 2009;Lacerda et al, 2011;Gonzalez-Mira et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Khurana

Bedi

Jain

2012

IJBNN

View full text Add to dashboard Cite

This study was aimed to develop nanostructured lipid carriers (NLC) for the possible delivery of mefenamic acid. This study describes the effect of liquid lipid concentration on the characteristics of NLC such as particle size, polydispersity index, zeta potential, drug entrapment efficiency, and occlusivity index. Transmission electron microscopy revealed nearly spherical shape NLC with negligible effect of liquid lipid content on the particle morphology. The differential scanning calorimetry demonstrated a depression in the melting point and crystallinity index of the NLC with an increase in the amount of liquid lipid. The in vitro drug release studies demonstrated that solid lipid nanoparticle (0% oil), and NLC possessed a biphasic release pattern characterised by a rapid initial release followed by a sustained release, in comparison to nanoemulsions (100% oil) of which a nearly constant release was observed. Compared to NE and SLN, the excellent physical stability of NLC against drug leakage was seen.

show abstract

Potential Use of Nanostructured Lipid Carriers for Topical Delivery of Flurbiprofen

Cited by 76 publications

References 32 publications

Antitumor activity of tripterine via cell-penetrating peptide-coated nanostructured lipid carriers in a prostate cancer model

Antitumor activity of tripterine via cell-penetrating peptide-coated nanostructured lipid carriers in a prostate cancer model

Investigation of flurbiprofen genotoxicity and cytotoxicity in rat bone marrow cells

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Contact Info

Product

Resources

About