The interactions of phospholipid vesicles with some anti-inflammatory agents

Venema, Fokko R; Weringa, W. D.

doi:10.1016/0021-9797(88)90013-6

Cited by 40 publications

(21 citation statements)

References 21 publications

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“…Three endothermal peaks which differed radically from that of EVO and phospholipids appeared in the thermogram of the complex, and the intrinsic endothermal peak of EVO was "shielded," as depicted by Kidd et al (8). The three new peaks, with onsets and maximums at 152.0 and 163.5°C, 196.0 and 199.3°C, and 255.9 and 262.1°C, respectively, may indicate that EVO and phospholipids had some interaction, as previous researchers claimed in the cases of curcumin-phospholipid complex (27) and silybin-phospholipid complex (28)(29)(30). Here, taking EPLC as a hybrid molecule, we assumed that the first broad peak and the second sharp peak of the complex, shifted right and left respectively when compared with the thermogram of phospholipids, corresponding to the rapid movements and phase transition evoked by endothermal peaks of phospholipids, and the third sharp peak corresponded to that of EVO.…”

Section: Differential Scanning Calorimetrymentioning

confidence: 53%

Design and Evaluation of a Novel Evodiamine-Phospholipid Complex for Improved Oral Bioavailability

et al. 2012

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Abstract. A novel evodiamine (EVO)-phospholipid complex (EPLC) was designed to improve the bioavailability of EVO. A central composite design approach was employed for process optimization. EPLC were characterized by differential scanning calorimetry, ultraviolet spectroscopy, Fourier transformed infrared spectroscopy, 1 H-NMR spectroscopy, matrix-assisted laser desorption/ionization time-offlight spectroscopy, apparent solubility, and dissolution rate. After oral administration of EPLC, the concentrations of EVO at different time points were determined by high-performance liquid chromatography. The optimal formulation for EPLC was obtained where the values of X 1 , X 2 , and X 3 were 2, 0.5, and 2.5 mg/mL, respectively. The average particle size and zeta potential of EPLC with the optimized formulation were 246.1 nm and −26.94 mV, respectively. The EVO and phospholipids in the EPLC were associated with non-covalent interactions. The solubility of EPLC in water and the dissolution rate of EPLC in phosphate-buffered solution (pH 6.8) were substantially enhanced. The plasma EVO concentration-time curves of EPLC and free EVO were both in accordance with the two-compartment model. The peak concentration and AUC 0−∞ of EPLC were increased, and the relative bioavailability was significantly increased to 218.82 % compared with that of EVO.

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Section: Differential Scanning Calorimetrymentioning

confidence: 53%

Design and Evaluation of a Novel Evodiamine-Phospholipid Complex for Improved Oral Bioavailability

et al. 2012

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“…Transmission electron micrographs of BPC after slightly shaking in distilled water at ×1500 magnifi cation (A) and at ×4000 magnifi cation (B), respectively. [18,23,24] . We performed some experiments to prove this point.…”

Section: Discussionmentioning

confidence: 99%

Preparation, characterization and in vivo evaluation of bergenin-phospholipid complex

et al. 2009

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Aim: To prepare a bergenin-phospholipid complex (BPC) to increase oral bioavailability of the drug. Methods: In order to obtain the acceptable BPC, a spherical symmetric design-response surface methodology was used for process optimization. The infl uence of reaction medium, temperature, drug concentration and drug-to-phospholipid ratio on the combination percentage and content of bergenin in BPC were evaluated. BPC was then characterized by thin-layer chromatography (TLC), high-performance liquid chromatography (HPLC), ultra-violet (UV) spectroscopy, fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and X-ray powder diffraction. The physicochemical properties such as microscopic shape, particle size, zetapotential, solubility, crystalline form, and hygroscopicity were tested. The pharmacokinetic characteristics and bioavailability of BPC were investigated after oral administration in rats in comparison to bergenin and the physical mixture (bergenin and phospholipids). Results: BPC was successfully prepared under the optimum conditions [temperature=60 °C, drug concentration=80 g/L and drug-tophospholipids ratio=0.9 (w/w)]. The combination percentage was 100.00%±0.20%, and the content of bergenin in the complex was 45.98%±1.12%. Scanning electron microscopy and transmission electron microscopy of BPC showed spherical particles. The average particle size was 169.2±20.11 nm and the zeta-potential was −21.6±2.4 mV. The solubility of BPC in water and in n-octanol was effectively enhanced. The C max and AUC 0→∞ of BPC were increased, and the relative bioavailability was signifi cantly increased to 439% of bergenin. Conclusion: The BPC is a valuable delivery system to enhance the oral absorption of bergenin.

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“…The lipid carrier displayed a less negative zeta potential at pH 2 than pH 8 and led to aggregation and further precipitation of the mixed micelles at lower pH values, which resulted in less solubilization of SLB under these conditions. However, some interactions between silybin and phospholipids, such as the combination of hydrogen bonds or van der Waals forces [13,30,31] , may not be very stable in highly charged environments (above pH 8). Therefore, a moderate pH value of medium is recommended for the preparation of the SLB-PPC-SDC-MMs.…”

Section: Parametersmentioning

confidence: 99%

“…As mentioned in the identification of the SLB-PPC complex by DSC, hydrogen bonding played a major role in SLB-PPC complexation [13][14][15]31] ; the -OH groups of the phenol rings of SLB were engaged in hydrogen bonding with the phospholipids. This indicated that it was the polar part of PPC that interacted with the silybin.…”

Section: Parametersmentioning

confidence: 99%

Mixed micelles loaded with silybin-polyene phosphatidylcholine complex improve drug solubility

et al. 2010

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Aim: To prepare a novel formulation of phosphatidylcholine (PC)-bile salts (BS)-mixed micelles (MMs) loaded with silybin (SLB)-PC complex for parenteral applications. Methods: SLB-PC-BS-MMs were prepared using the co-precipitation method. Differential scanning calorimetry (DSC) analysis was used to confirm the formation of the complex and several parameters were optimized to obtain a high quality formulation. The water-solubility, drug loading, particle size, zeta potential, morphology and in vivo properties of the SLB-PC-BS-MMs were determined. Results: The solubility of SLB in water was increased from 40.83±1.18 µg/mL to 10.14±0.36 mg/mL with a high drug loading (DL) of 14.43%±0.44% under optimized conditions. The SLB-PC-BS-MMs were observed by transmission electron microscopy (TEM) and scanning electron microscopy (SEM) and showed spherical shapes. The particle size and zeta potential, as measured by photon correlation spectroscopy (PCS), were about 30±4.8 nm and -39±5.0 mV, respectively. In vivo studies showed that incorporation of the SLB-PC complex into PC-BS-MMs led to a prolonged circulation time of the drug. Conclusion:This novel formulation appears to be a good candidate for drug substances that exhibit poor solubility for parenteral administration.

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The interactions of phospholipid vesicles with some anti-inflammatory agents

Cited by 40 publications

References 21 publications

Design and Evaluation of a Novel Evodiamine-Phospholipid Complex for Improved Oral Bioavailability

Design and Evaluation of a Novel Evodiamine-Phospholipid Complex for Improved Oral Bioavailability

Preparation, characterization and in vivo evaluation of bergenin-phospholipid complex

Mixed micelles loaded with silybin-polyene phosphatidylcholine complex improve drug solubility

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