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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 release of aceclofenac from proliposomesIn vitro drug release profiles of aceclofenac from proliposome formulations 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 0004: In vitro drug release of aceclofenac from proliposomesIn vitro drug release profiles of aceclofenac from proliposome formulations 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 mean cumulative percentage of aceclofenac release from the aceclofenac loaded proliposomes of various formulations in PBS (pH 7.4) are given in fig. 4, as a function of time (Table 1). It was seen that increase in the lecithin concentration further retarded the cumulative release of aceclofenac from proliposomes, indicating sustained release of drug for a longer period of time.


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 release of aceclofenac from proliposomesIn vitro drug release profiles of aceclofenac from proliposome formulations 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 0004: In vitro drug release of aceclofenac from proliposomesIn vitro drug release profiles of aceclofenac from proliposome formulations 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 mean cumulative percentage of aceclofenac release from the aceclofenac loaded proliposomes of various formulations in PBS (pH 7.4) are given in fig. 4, as a function of time (Table 1). It was seen that increase in the lecithin concentration further retarded the cumulative release of aceclofenac from proliposomes, indicating sustained release of drug for a longer period of time.

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