Development and physicochemical evaluation of pharmacosomes of diclofenac.
Pharmacosomes are amphiphilic lipid vesicular systems that have shown their potential in improving the bioavailability of poorly water soluble as well as poorly lipophilic drugs. Diclofenac is a poorly water soluble drug and also causes gastrointestinal toxicity. To improve the water solublity of diclofenac, its pharmacosomes (phospholipid complex) have been prepared and evaluated for physicochemical analysis. Diclofenac was complexed with phosphatidylcholine (80%) in equimolar ratio, in the presence of dichloromethane, by the conventional solvent evaporation technique. Pharmacosomes thus prepared were evaluated for drug solubility, drug content, surface morphology (by scanning electron microscopy), phase transition behaviour (by differential scanning calorimetry), crystallinity (by X-ray powder diffraction) and in vitro dissolution. Pharmacosomes of diclofenac were found to be irregular or disc shaped with rough surfaces in SEM. Drug content was found to be 96.2 +/- 1.1%. DSC thermograms and XRPD data confirmed the formation of the phospholipid complex. Water solubility of the prepared complex was found to be 22.1 microg mL-1 as compared to 10.5 microg mL-1 of diclofenac. This improvement in water solubility in prepared pharmacosomes may result in improved dissolution and lower gastrointestinal toxicity. Pharmacosomes showed 87.8% while the free diclofenac acid showed a total of only 60.4% drug release at the end of 10 h of dissolution study.
Semalty
Ajay
A
Department of Pharmaceutical Sciences, H. N. B. Garhwal University, Srinagar Garhwal, India. semaltyajay@yahoo.co.in
Semalty
Mona
M
Singh
Devendra
D
Rawat
M S M
MS
D002626:Chemistry, Pharmaceutical / Q000379:methods; D004008:Diclofenac / Q000737:chemistry* / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry* / Q000493:pharmacokinetics; D004353:Drug Evaluation, Preclinical / Q000379:methods; D010713:Phosphatidylcholines / Q000737:chemistry / Q000493:pharmacokinetics; D010743:Phospholipids / Q000737:chemistry* / Q000493:pharmacokinetics; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013499:Surface Properties; D014961:X-Ray Diffraction
D004337:Drug Carriers; D010713:Phosphatidylcholines; D010743:Phospholipids; D004008:Diclofenac