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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

Optical microphotograph of aceclofenac-loaded proliposomes after hydrationOptical microphotographs of aceclofenac-loaded proliposomes after hydration at 30 s (a) and at 60 s (b) at the magnification of 1000 X to examine the formation of liposomes.
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Figure 0002: Optical microphotograph of aceclofenac-loaded proliposomes after hydrationOptical microphotographs of aceclofenac-loaded proliposomes after hydration at 30 s (a) and at 60 s (b) at the magnification of 1000 X to examine the formation of liposomes.

Mentions: The surface morphology of proliposome granules and plain mannitol granules were examined by scanning electron microscopy. The surface morphology of proliposome powder was different as compare to plain mannitol powder as shown in SEM (fig. 1). From SEM photographs it is clear that, the surface of mannitol crystals becomes illegible due to deposition of phospholipid on mannitol surface. Observation under an optical microscope revealed that proliposome particles are progressively, but rapidly converted to liposomes within minutes following contact with water (fig. 2). Liposome formation was confirmed again by transmission electron microscopy. A TEM image of the liposomes (reconstituted from the proliposomes) was observed (fig. 3) which confirms that, a suspension of monolayer liposomes with approximate diameter of 200 nm was formed from the proliposomes following contact with water.


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

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

Optical microphotograph of aceclofenac-loaded proliposomes after hydrationOptical microphotographs of aceclofenac-loaded proliposomes after hydration at 30 s (a) and at 60 s (b) at the magnification of 1000 X to examine the formation of liposomes.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 0002: Optical microphotograph of aceclofenac-loaded proliposomes after hydrationOptical microphotographs of aceclofenac-loaded proliposomes after hydration at 30 s (a) and at 60 s (b) at the magnification of 1000 X to examine the formation of liposomes.
Mentions: The surface morphology of proliposome granules and plain mannitol granules were examined by scanning electron microscopy. The surface morphology of proliposome powder was different as compare to plain mannitol powder as shown in SEM (fig. 1). From SEM photographs it is clear that, the surface of mannitol crystals becomes illegible due to deposition of phospholipid on mannitol surface. Observation under an optical microscope revealed that proliposome particles are progressively, but rapidly converted to liposomes within minutes following contact with water (fig. 2). Liposome formation was confirmed again by transmission electron microscopy. A TEM image of the liposomes (reconstituted from the proliposomes) was observed (fig. 3) which confirms that, a suspension of monolayer liposomes with approximate diameter of 200 nm was formed from the proliposomes following contact with water.

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