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Development and evaluation of pharmacosomes of aceclofenac.

Semalty A, Semalty M, Rawat BS, Singh D, Rawat MS - Indian J Pharm Sci (2010)

Bottom Line: Pharmacosomes are amphiphilic lipid vesicular systems containing phospholipid complexes with a potential to improve bioavailability of poorly water soluble as well as poorly lipophilic drugs.Drug content was found to be 91.88% (w/w) for aceclofenac phospholipid complex (1:1) and 89.03% (w/w) aceclofenac-phospholipid complex (2:1).Solubility and dissolution profile of the prepared complex was found to be much better than aceclofenac.

View Article: PubMed Central - PubMed

Affiliation: Departments of Pharmaceutical Sciences H. N. B. Garhwal University, Srinagar (Garhwal)-246 174, India.

ABSTRACT
Pharmacosomes are amphiphilic lipid vesicular systems containing phospholipid complexes with a potential to improve bioavailability of poorly water soluble as well as poorly lipophilic drugs. To improve the water solubility, bioavailability and minimize the gastrointestinal toxicity of aceclofenac, its pharmacosomes were prepared. Aceclofenac was complexed with phosphatidylcholine (80%) in two different ratios (1:1 and 2:1) using conventional solvent evaporation technique. Pharmacosomes thus prepared were subjected to solubility and drug content evaluation, scanning electron microscopy, differential scanning calorimetry, X ray powder diffraction and in vitro dissolution study. Pharmacosomes of aceclofenac were found to be disc shaped with rough surface in scanning electron microscopy. Drug content was found to be 91.88% (w/w) for aceclofenac phospholipid complex (1:1) and 89.03% (w/w) aceclofenac-phospholipid complex (2:1). Differential scanning calorimetric thermograms and X ray powder diffraction datas confirmed the formation of phospholipid complex. Solubility and dissolution profile of the prepared complex was found to be much better than aceclofenac.

No MeSH data available.


Related in: MedlinePlus

DSC thermograms of drug, complex and physical mixture Aceclofenac (a), Phosphatidylcholine (80% PC) (b), aceclofenac-PC complex (2:1) (c) and aceclofenac-PC complex (1:1) (d).
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Figure 2: DSC thermograms of drug, complex and physical mixture Aceclofenac (a), Phosphatidylcholine (80% PC) (b), aceclofenac-PC complex (2:1) (c) and aceclofenac-PC complex (1:1) (d).

Mentions: For evaluating interaction/complexation of aceclofenac with PC, DSC analysis was performed on aceclofenac, PC, and the aceclofenac-PC complex[16]. The results of the DSC test confirmed the formation of a complex of aceclofenac and PC due to presence of unique peak in the complex which were entirely different from the positions of the peaks of aceclofenac and PC (fig. 2).


Development and evaluation of pharmacosomes of aceclofenac.

Semalty A, Semalty M, Rawat BS, Singh D, Rawat MS - Indian J Pharm Sci (2010)

DSC thermograms of drug, complex and physical mixture Aceclofenac (a), Phosphatidylcholine (80% PC) (b), aceclofenac-PC complex (2:1) (c) and aceclofenac-PC complex (1:1) (d).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3116301&req=5

Figure 2: DSC thermograms of drug, complex and physical mixture Aceclofenac (a), Phosphatidylcholine (80% PC) (b), aceclofenac-PC complex (2:1) (c) and aceclofenac-PC complex (1:1) (d).
Mentions: For evaluating interaction/complexation of aceclofenac with PC, DSC analysis was performed on aceclofenac, PC, and the aceclofenac-PC complex[16]. The results of the DSC test confirmed the formation of a complex of aceclofenac and PC due to presence of unique peak in the complex which were entirely different from the positions of the peaks of aceclofenac and PC (fig. 2).

Bottom Line: Pharmacosomes are amphiphilic lipid vesicular systems containing phospholipid complexes with a potential to improve bioavailability of poorly water soluble as well as poorly lipophilic drugs.Drug content was found to be 91.88% (w/w) for aceclofenac phospholipid complex (1:1) and 89.03% (w/w) aceclofenac-phospholipid complex (2:1).Solubility and dissolution profile of the prepared complex was found to be much better than aceclofenac.

View Article: PubMed Central - PubMed

Affiliation: Departments of Pharmaceutical Sciences H. N. B. Garhwal University, Srinagar (Garhwal)-246 174, India.

ABSTRACT
Pharmacosomes are amphiphilic lipid vesicular systems containing phospholipid complexes with a potential to improve bioavailability of poorly water soluble as well as poorly lipophilic drugs. To improve the water solubility, bioavailability and minimize the gastrointestinal toxicity of aceclofenac, its pharmacosomes were prepared. Aceclofenac was complexed with phosphatidylcholine (80%) in two different ratios (1:1 and 2:1) using conventional solvent evaporation technique. Pharmacosomes thus prepared were subjected to solubility and drug content evaluation, scanning electron microscopy, differential scanning calorimetry, X ray powder diffraction and in vitro dissolution study. Pharmacosomes of aceclofenac were found to be disc shaped with rough surface in scanning electron microscopy. Drug content was found to be 91.88% (w/w) for aceclofenac phospholipid complex (1:1) and 89.03% (w/w) aceclofenac-phospholipid complex (2:1). Differential scanning calorimetric thermograms and X ray powder diffraction datas confirmed the formation of phospholipid complex. Solubility and dissolution profile of the prepared complex was found to be much better than aceclofenac.

No MeSH data available.


Related in: MedlinePlus