Comparative Physicochemical Characterization of Phospholipids Complex of Puerarin Formulated by Conventional and Supercritical Methods

Li, Ying; Yang, Da; Chen, Shilin; Chen, Sibao; Chan, Albert S. C.

doi:10.1007/s11095-007-9418-x

Cited by 66 publications

(23 citation statements)

References 35 publications

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“…The DSC data of the prepared complex showed a noticeable reduction in the enthalpy as well as the melting point in comparison with catechin and PC. These DSC data are well supported by the results of DSC thermograms of the phospholipid complexes of some phytoconstituents like naringenin, silybin, puerarin, curcumin and gallic acid [12,[15][16][17][18][19]. In all these studies the thermogram of the complex also exhibited a single peak which was different from the peak of phytoconstituents and phospholipids.…”

Section: Dsc Studiessupporting

confidence: 70%

Phyto-phospholipid complex of catechin in value added herbal drug delivery

Semalty

Singh

et al. 2011

J Incl Phenom Macrocycl Chem

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Catechin (an anti-inflammatory, antioxidant, antitumour, and hepatoprotective bioflavonoid) is poorly absorbed across the GIT because it has multiple ring molecules that are too large to be absorbed by simple diffusion. It typically has poor miscibility with oils and other lipids which limit their ability to pass across the lipid rich outer membranes of enterocytes of small intestine. Thus catechin-phospholipid complex were prepared to improve its absorption by imparting an environment of improved lipophilicity. The phospholipid complexes of catechin were prepared with phosphatidylcholine in presence of dichloromethane by conventional solvent evaporation technique. Pharmacosomes thus prepared were evaluated for solubility, drug content, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X ray powder diffraction (XRPD), in vitro dissolution study and in vitro antioxidant activity. Prepared phospholipid complex showed high drug content (99.40%. w/w) and improved lipid solubility (0.79-1.97 mg/mL). FTIR, NMR, DSC and XRPD data confirmed the formation of phospholipid complex. Unlike the free catechin, catechin complex showed a sustained release over the 24 h of study. Catechin-phospholipid complex showed slightly better antioxidant activity than that of catechin at all dose levels. Thus it can be concluded that the phospholipid complex of catechin may be of potential use for improving absorption of catechin across the lipidic biological barriers in gastrointestinal tract. It was concluded that the complexation with phospholipids did not interfere with the biological activities. This herbal drug delivery system can pave the way for large molecules to pass through the lipophilic biological membrane (by the virtue of their amphiphilic nature) and get absorbed into the systemic circulation.

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Section: Dsc Studiessupporting

confidence: 70%

Phyto-phospholipid complex of catechin in value added herbal drug delivery

Semalty

Singh

et al. 2011

J Incl Phenom Macrocycl Chem

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“…It is evident that the original peaks of diclofenac and phospholipids disappear from the thermogram of pharmacosomes (complex) and the phase transition temperature is lower than that of phospholipids. The DSC thermograms of the phospholipid complexes of some phytoconstituents, like silybin, puerarin, curcumin and some xanthones, revealed similar results (12)(13)(14).…”

Section: Resultsmentioning

confidence: 75%

Development and physicochemical evaluation of pharmacosomes of diclofenac

Semalty¹,

Semalty²,

Singh³

et al. 2009

Acta Pharmaceutica

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Diclofenac is one of the most widely prescribed non-steroidal anti-inflammatory drugs (NSAIDs). Use of diclofenac is associated with two major limitations; first, rare, but serious and sometimes fatal, gastrointestinal (GI) side-effects, including ulceration, and hemorrhage, especially in the elderly (1, 2), and second, poor water solubility. 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 mg mL -1 as compared to 10.5 mg 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.

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“…3). The integrated intensity (the area under the curves of the XRPD patterns) is the characteristics of given sample[22]. It was observed that crystalline diffraction peaks of aceclofenac were disappeared in XRPD of the complex which in turn confirmed the formation of phospholipid complex.…”

Section: Resultsmentioning

confidence: 99%

Development and evaluation of pharmacosomes of aceclofenac

Semalty¹,

Semalty²,

Rawat³

et al. 2010

Indian J Pharm Sci

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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.

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Comparative Physicochemical Characterization of Phospholipids Complex of Puerarin Formulated by Conventional and Supercritical Methods

Abstract: Supercritical fluid technology for the preparation of puerarin and its phospholipids complex has been proven to have significant advantages over the solvent evaporation technique and other conventional methods.

Cited by 66 publications

References 35 publications

Phyto-phospholipid complex of catechin in value added herbal drug delivery

Phyto-phospholipid complex of catechin in value added herbal drug delivery

Development and physicochemical evaluation of pharmacosomes of diclofenac

Development and evaluation of pharmacosomes of aceclofenac

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