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Formulation Development and in vitro Characterization of Proliposomes for Topical Delivery of Aceclofenac.

Gupta V, Barupal AK, Ramteke S - Indian J Pharm Sci (2008)

Bottom Line: The maximum entrapment efficiency of reconstituted liposomes was 80.31% whereas the drug content in proliposomes was found to be more than 90%.In vitro release of drug was significantly retarded indicating sustained release of aceclofenac from proliposomes.Stability study was performed at various temperatures indicating that aceclofenac proliposomes are stable at lower temperature.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Airport Bypass Road, Gandhi Nagar, Bhopal-462036, India.

ABSTRACT
Non-steroidal antiinflammatory drugs are routinely prescribed for the patients with rheumatic disease and such patients are at increased risk of serious gastrointestinal complications, when non-steroidal antiinflammatory drugs administered by oral route. The aim of the present study was to develop and characterized a vesicular drug carrier system (proliposome) for topical delivery of aceclofenac to overcome the problems related with oral route. Aceclofenac proliposome were prepared by the film-deposition on carriers method and characterized for size and surface morphology, drug content in both proliposomes and liposomal system, percent yield, in vitro drug release studies and drug permeation studies. The prepared system was also characterized for drug-excipients interaction by Fourier transform infrared spectrophotometer and stability studies. The size and surface morphology were studied using optical microscopy, scanning electron microscopy and transmission electron microscopy. A spherical shape of reconstituted aceclofenac liposome with an average vesicular size of about 500 nm was observed in photomicrographs. The maximum entrapment efficiency of reconstituted liposomes was 80.31% whereas the drug content in proliposomes was found to be more than 90%. In vitro release of drug was significantly retarded indicating sustained release of aceclofenac from proliposomes. Stability study was performed at various temperatures indicating that aceclofenac proliposomes are stable at lower temperature.

No MeSH data available.


Related in: MedlinePlus

In vitro drug permeation profileIn vitro drug permeation profiles of aceclofenac from proliposome formulation containing drug/lecithin ratios of 0.1/0.5 (-◆-), 0.1/1.0 (-■-), 0.1/1.5 (-▲-) and 0.1/2.0 (-●-) in pH 7.4 phosphate buffer saline. Each point represents mean±SD of three different determinations.
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Figure 0005: In vitro drug permeation profileIn vitro drug permeation profiles of aceclofenac from proliposome formulation containing drug/lecithin ratios of 0.1/0.5 (-◆-), 0.1/1.0 (-■-), 0.1/1.5 (-▲-) and 0.1/2.0 (-●-) in pH 7.4 phosphate buffer saline. Each point represents mean±SD of three different determinations.

Mentions: The objective of this study was to examine the feasibility of proliposomes as a transdermal dosage form. The simplest way of topical application may be a direct spread of the proliposomes on the skin followed by occlusive dressing of the dosed site. The permeation of the aceclofenac following application of the proliposomes on the skin under occlusive condition was studied. Fig. 5 and Table 2 show the cumulative amount of aceclofenac permeated from aceclofenac proliposomes to the receptor compartment. PBS (pH 7.4 phosphate buffer saline solution) of the franz diffusion cell, through rat skin.


Formulation Development and in vitro Characterization of Proliposomes for Topical Delivery of Aceclofenac.

Gupta V, Barupal AK, Ramteke S - Indian J Pharm Sci (2008)

In vitro drug permeation profileIn vitro drug permeation profiles of aceclofenac from proliposome formulation containing drug/lecithin ratios of 0.1/0.5 (-◆-), 0.1/1.0 (-■-), 0.1/1.5 (-▲-) and 0.1/2.0 (-●-) in pH 7.4 phosphate buffer saline. Each point represents mean±SD of three different determinations.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3040871&req=5

Figure 0005: In vitro drug permeation profileIn vitro drug permeation profiles of aceclofenac from proliposome formulation containing drug/lecithin ratios of 0.1/0.5 (-◆-), 0.1/1.0 (-■-), 0.1/1.5 (-▲-) and 0.1/2.0 (-●-) in pH 7.4 phosphate buffer saline. Each point represents mean±SD of three different determinations.
Mentions: The objective of this study was to examine the feasibility of proliposomes as a transdermal dosage form. The simplest way of topical application may be a direct spread of the proliposomes on the skin followed by occlusive dressing of the dosed site. The permeation of the aceclofenac following application of the proliposomes on the skin under occlusive condition was studied. Fig. 5 and Table 2 show the cumulative amount of aceclofenac permeated from aceclofenac proliposomes to the receptor compartment. PBS (pH 7.4 phosphate buffer saline solution) of the franz diffusion cell, through rat skin.

Bottom Line: The maximum entrapment efficiency of reconstituted liposomes was 80.31% whereas the drug content in proliposomes was found to be more than 90%.In vitro release of drug was significantly retarded indicating sustained release of aceclofenac from proliposomes.Stability study was performed at various temperatures indicating that aceclofenac proliposomes are stable at lower temperature.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Airport Bypass Road, Gandhi Nagar, Bhopal-462036, India.

ABSTRACT
Non-steroidal antiinflammatory drugs are routinely prescribed for the patients with rheumatic disease and such patients are at increased risk of serious gastrointestinal complications, when non-steroidal antiinflammatory drugs administered by oral route. The aim of the present study was to develop and characterized a vesicular drug carrier system (proliposome) for topical delivery of aceclofenac to overcome the problems related with oral route. Aceclofenac proliposome were prepared by the film-deposition on carriers method and characterized for size and surface morphology, drug content in both proliposomes and liposomal system, percent yield, in vitro drug release studies and drug permeation studies. The prepared system was also characterized for drug-excipients interaction by Fourier transform infrared spectrophotometer and stability studies. The size and surface morphology were studied using optical microscopy, scanning electron microscopy and transmission electron microscopy. A spherical shape of reconstituted aceclofenac liposome with an average vesicular size of about 500 nm was observed in photomicrographs. The maximum entrapment efficiency of reconstituted liposomes was 80.31% whereas the drug content in proliposomes was found to be more than 90%. In vitro release of drug was significantly retarded indicating sustained release of aceclofenac from proliposomes. Stability study was performed at various temperatures indicating that aceclofenac proliposomes are stable at lower temperature.

No MeSH data available.


Related in: MedlinePlus