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Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies.

Bhaskar K, Anbu J, Ravichandiran V, Venkateswarlu V, Rao YM - Lipids Health Dis (2009)

Bottom Line: The Cmax of the B1 formulation was 38.67 +/- 2.77 microg/ml, which was significantly higher than the A1 formulation (Cmax = 21.79 +/- 2.96 microg/ml).The bioavailability of flurbiprofen with reference to oral administration was found to increase by 4.4 times when gel formulations were applied.Both the SLN and NLC dispersions and gels enriched with SLN and NLC possessed a sustained drug release over period of 24 h but the sustained effect was more pronounced with the SLN and NLC gel.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, VELS University, Velan Nagar, Pallavaram, Chennai, Tamil Nadu, India. bhaskurra@yahoo.com

ABSTRACT
The aim of the study is to prepare aqueous dispersions of lipid nanoparticles--flurbiprofen solid lipid nanoparticles (FLUSLN) and flurbiprofen nanostructured lipid carriers (FLUNLC) by hot homogenization followed by sonication technique and then incorporated into the freshly prepared hydrogels for transdermal delivery. They are characterized for particle size, for all the formulations, more than 50% of the particles were below 300 nm after 90 days of storage at RT. DSC analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by TEM which revealed fairly spherical shape of the formulations. Further they were evaluated for in vitro drug release characteristics, rheological behaviour, pharmacokinetic and pharmacodynamic studies. The pharmacokinetics of flurbiprofen in rats following application of SLN gel (A1) and NLC gel (B1) for 24 h were evaluated. The Cmax of the B1 formulation was 38.67 +/- 2.77 microg/ml, which was significantly higher than the A1 formulation (Cmax = 21.79 +/- 2.96 microg/ml). The Cmax and AUC of the B1 formulation were 1.8 and 2.5 times higher than the A1 gel formulation respectively. The bioavailability of flurbiprofen with reference to oral administration was found to increase by 4.4 times when gel formulations were applied. Anti-inflammatory effect in the Carrageenan-induced paw edema in rat was significantly higher for B1 and A1 formulation than the orally administered flurbiprofen. Both the SLN and NLC dispersions and gels enriched with SLN and NLC possessed a sustained drug release over period of 24 h but the sustained effect was more pronounced with the SLN and NLC gel.

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In vitro release of FLU from gels enriched with NLC dispersions, Mean S.D (n = 3)
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Figure 9: In vitro release of FLU from gels enriched with NLC dispersions, Mean S.D (n = 3)

Mentions: FLUNLC, the liquid lipid enriched shell possessed soft and considerable higher solubility for lipophilic drugs character, in which the drug was easily loaded to higher amount and the drug could be easily released as well by the drug diffusion or the matrix erosion manners [15]. Furthermore, the incorporation of liquid lipid into solid lipid matrix caused the FLUNLC become more imperfect and allowed the loaded drug to easy release, thus increased the drug release rate when liquid lipid was included in NLC matrix. The results of sustained release and increased drug release rate were achieved compared to FLUSLN. Comparing the drug release from FLUSLN and FLUNLC dispersions and FLUSLN and FLUNLC in gels (figures 8 and 9), the release of FLU was slower from gel formulation. The percentage drug release at the end of 24 h in A1 (FLUSLN) and B1 (FLUNLC) gel formulations was found to 54.87% and 64.45% respectively whereas the percentage drug release at the end of 24 h in A (FLUSLN) and B (FLUNLC) dispersions was 63.66% and 72.65% respectively. Incorporation of SLN and NLC dispersion into gels decreased the drug release; this may be due to the release retarding effect of the polymeric matrix of the gelling agent.


Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies.

Bhaskar K, Anbu J, Ravichandiran V, Venkateswarlu V, Rao YM - Lipids Health Dis (2009)

In vitro release of FLU from gels enriched with NLC dispersions, Mean S.D (n = 3)
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2651881&req=5

Figure 9: In vitro release of FLU from gels enriched with NLC dispersions, Mean S.D (n = 3)
Mentions: FLUNLC, the liquid lipid enriched shell possessed soft and considerable higher solubility for lipophilic drugs character, in which the drug was easily loaded to higher amount and the drug could be easily released as well by the drug diffusion or the matrix erosion manners [15]. Furthermore, the incorporation of liquid lipid into solid lipid matrix caused the FLUNLC become more imperfect and allowed the loaded drug to easy release, thus increased the drug release rate when liquid lipid was included in NLC matrix. The results of sustained release and increased drug release rate were achieved compared to FLUSLN. Comparing the drug release from FLUSLN and FLUNLC dispersions and FLUSLN and FLUNLC in gels (figures 8 and 9), the release of FLU was slower from gel formulation. The percentage drug release at the end of 24 h in A1 (FLUSLN) and B1 (FLUNLC) gel formulations was found to 54.87% and 64.45% respectively whereas the percentage drug release at the end of 24 h in A (FLUSLN) and B (FLUNLC) dispersions was 63.66% and 72.65% respectively. Incorporation of SLN and NLC dispersion into gels decreased the drug release; this may be due to the release retarding effect of the polymeric matrix of the gelling agent.

Bottom Line: The Cmax of the B1 formulation was 38.67 +/- 2.77 microg/ml, which was significantly higher than the A1 formulation (Cmax = 21.79 +/- 2.96 microg/ml).The bioavailability of flurbiprofen with reference to oral administration was found to increase by 4.4 times when gel formulations were applied.Both the SLN and NLC dispersions and gels enriched with SLN and NLC possessed a sustained drug release over period of 24 h but the sustained effect was more pronounced with the SLN and NLC gel.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, VELS University, Velan Nagar, Pallavaram, Chennai, Tamil Nadu, India. bhaskurra@yahoo.com

ABSTRACT
The aim of the study is to prepare aqueous dispersions of lipid nanoparticles--flurbiprofen solid lipid nanoparticles (FLUSLN) and flurbiprofen nanostructured lipid carriers (FLUNLC) by hot homogenization followed by sonication technique and then incorporated into the freshly prepared hydrogels for transdermal delivery. They are characterized for particle size, for all the formulations, more than 50% of the particles were below 300 nm after 90 days of storage at RT. DSC analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by TEM which revealed fairly spherical shape of the formulations. Further they were evaluated for in vitro drug release characteristics, rheological behaviour, pharmacokinetic and pharmacodynamic studies. The pharmacokinetics of flurbiprofen in rats following application of SLN gel (A1) and NLC gel (B1) for 24 h were evaluated. The Cmax of the B1 formulation was 38.67 +/- 2.77 microg/ml, which was significantly higher than the A1 formulation (Cmax = 21.79 +/- 2.96 microg/ml). The Cmax and AUC of the B1 formulation were 1.8 and 2.5 times higher than the A1 gel formulation respectively. The bioavailability of flurbiprofen with reference to oral administration was found to increase by 4.4 times when gel formulations were applied. Anti-inflammatory effect in the Carrageenan-induced paw edema in rat was significantly higher for B1 and A1 formulation than the orally administered flurbiprofen. Both the SLN and NLC dispersions and gels enriched with SLN and NLC possessed a sustained drug release over period of 24 h but the sustained effect was more pronounced with the SLN and NLC gel.

Show MeSH
Related in: MedlinePlus