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. 2008;9(1):154-62.
doi: 10.1208/s12249-007-9028-2. Epub 2008 Jan 25.

Lipospheres as carriers for topical delivery of aceclofenac: preparation, characterization and in vivo evaluation

Maha Nasr  1 , Samar Mansour, Nahed D Mortada, A A El Shamy
Affiliations

Lipospheres as carriers for topical delivery of aceclofenac: preparation, characterization and in vivo evaluation

Maha Nasr et al. AAPS PharmSciTech. 2008.

Abstract

The purpose of this study was to prepare lipospheres containing aceclofenac intended for topical skin delivery with the aim of exploiting the favorable properties of this carrier system and developing a sustained release formula to overcome the side effects resulting from aceclofenac oral administration. Lipospheres were prepared using different lipid cores and phospholipid coats adopting melt and solvent techniques. Characterization was carried out through photomicroscopy, scanning electron microscopy, particle size analysis, DSC, In vitro drug release and storage study. The anti-inflammatory effect of liposphere systems was assessed by the rat paw edema technique and compared to the marketed product. Results revealed that liposphere systems were able to entrap aceclofenac at very high levels (93.1%). The particle size of liposphere systems was well suited for topical drug delivery. DSC revealed the molecular dispersion of aceclofenac when incorporated in lipospheres. Both entrapment efficiency and release were affected by the technique of preparation, core and coat types, core to coat ratio and drug loading. Lipospheres were very stable after 3 months storage at 2-8 degrees C manifested by low leakage rate (less than 7%) and no major changes in particle size. Finally, liposphere systems were found to possess superior anti-inflammatory activity compared to the marketed product in both lotion and paste consistencies. Liposphere systems proved to be a promising topical system for the delivery of aceclofenac as they possessed the ability to entrap the drug at very high levels and high stability, and to sustain the anti-inflammatory effect of the drug.

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Figures

Fig. 1
Fig. 1
Photomicrograph of aceclofenac lipospheres prepared by melt method at a magnification of ×400
Fig. 2
Fig. 2
Scanning electron micrographs of aceclofenac lipospheres prepared by melt method
Fig. 3
Fig. 3
DSC thermogram of aceclofenac, plain and drug loaded lipospheres
Fig. 4
Fig. 4
Inhibition percentage of aceclofenac lipospheres compared to the marketed product
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