An NMR and DSC study of the interaction of phospholipid vesicles with some anti-inflammatory agents

Lasonder, Edwin; Weringa, W. D.

doi:10.1016/0021-9797(90)90119-9

Cited by 58 publications

(36 citation statements)

References 17 publications

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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%

“…Despite the promising biological effects of SLB, its poor water solubility (about 40 µg/mL) and oral bioavailability (about 0.73%) in both rodents and humans, as reported by several researchers [12][13][14][15] , has restricted its clinical application. To improve this situation, there have been many contributions to the development of SLB formulations [15][16][17] .…”

Section: Introductionmentioning

confidence: 99%

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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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Section: Parametersmentioning

confidence: 99%

Section: Parametersmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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

et al. 2010

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“…On the other hand, DSC results mainly showed the presence of HP-β-CD in the complex with the endotherm of the flavonoid virtually absent, unlike the physical mixture which manifested clearly the presence of the two substances. It is believed that phloridzin was completely dispersed in HP-β-CD and that some interactions, probably involving the combination of hydrogen bonds and van der Waals force [10]. This appears to be buttressed by the xray diffraction (XRD) data.…”

Section: Discussionmentioning

confidence: 99%

Characterization and Antioxidant Activity of the Complex of Phloridzin and Hydroxypropyl-β- cyclodextrin

Yuan¹,

Liu²,

Li³

et al. 2012

Trop. J. Pharm Res

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Purpose: To improve the aqueous solubility of phloridzin by complexing it with hydroxypropyl-β-cyclodextrin (HP-β-CD). Methods: The complex of phloridzin with HP-β-CD was prepared by freeze-drying method. The physicochemical properties of the complex were investigated by ultraviolet-visible spectrometry (UV), infrared spectrometry (IR), differential scanning calorimetry (DSC) and x-ray diffractometry (XRD

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“…It was considered that puerarin and phospholipids should have some interaction, such as the combination of hydrogen bonds or van der Waals force. 14,16,17) Optimization of Emulsion Preparation Central composite design (CCD) was a response surface design which provided information on direct effects, pairwise interaction effects and curvilinear variable effects and was widely used for formulation and process optimization in the field of pharmaceutics. 18,19) It was very efficient and flexible, providing much information on experiment variable effects and overall experimental error in a minimal number of required runs.…”

mentioning

confidence: 99%

Development and Optimization of Intravenous Puerarin Emulsions Formation by a Novel Complex-Phase Inversion-Homogenization Technology

Yue

Yuan

et al. 2007

CHEMICAL & PHARMACEUTICAL BULLETIN

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Puerarin is naturally isoflavone C-glycoside which was isolated from Pueraria lobota. It is traditionally used to reduce febrile symptoms and decrease myocardial consumption of oxygen, and it also can increase coronary artery blood flow and improve microcirculation. [1][2][3] Due to poor oral bioavailability, the commercial product puerarin i.v. is widely used in clinical. It is used for treatment of coronary artery disease, ischemic heart disease, cerebrovascular disease, coronarism and cerebral angio spasm in clinic. 4,5) But the clinical efficacy of puerarin i.v. is limited by severe and acute toxic side effects, such as intravenous hemolysis. So it is very necessary to seek a novel delivery system for puerarin in order to reduce its side effects. 6,7) Submicron emulsion, also referred to as lipid emulsions or lipid microspheres, is potentially interesting drug delivery system.8) It can reduce drug hydrolysis and increase drug bioavailability.9) By means of incorporating drug into the lipophilic core (of the oil droplets or in the core of micelles) or in the interface, direct contact of the drug with the body fluid and tissues can also be avoided in order to minimize the drug possible side effects. The reports about the ability of these systems to enhance the efficacy and to reduce side effects have appeared in the literature. 10) And there are some drug loaded emulsions for i.v. injection on the market such as amphotericin B, 11) prostaglandin E 1 . 12)Puerarin is slightly soluble in water (the aqueous solubility of about 4 mg/ml) and poorly soluble in oil.13) So it would be very difficult to incorporate puerarin into oil phase of emulsion by the traditional homogenization method. The puerarin emulsions are not possibly prepared by applying the simple method which was to dissolve the drug in the oil in order to prepare the emulsion. The objectives of this study are: (a) puerarin emulsion was firstly prepared by novel complexphase inversion-homogenization (CPIH) technology which was a technology basically combining drug phospholipid complex with the phase inversion-homogenization technology, and to investigate if it was possible to decrease the particle size, span of dispersity and to increase entrapment efficiency of puerarin emulsion; (b) to optimize preparative parameters which powerfully affect the characteristics of puerarin emulsion by central composite design; (c) to evaluate the physicochemical character of puerarin emulsion such as morphology and stability. ExperimentalMaterials Puerarin was obtained from Xian-guochui Ltd., purity 99.5% (Xi-AN, China). Egg lecithin was purchased from Hua-qing-mei-hen Ltd. (Beijing, China); Purified soybean oil for parenteral use (Tieling BeiYa Pharmaceutical Co., Tieling, China). Synperonic F68 (BASF AG, Ludwigshafen, Germany), All other chemicals and reagents were of analytical or chromatographic grade.Component of Preparation Formula Puerarin, 1 g; soybean lecithin, 1.2 g; soybean oil, 12 g; synperonic F68, 0.2 g; glycerol, 2.5 g; a-tocopherol, 300 mg; double disti...

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An NMR and DSC study of the interaction of phospholipid vesicles with some anti-inflammatory agents

Cited by 58 publications

References 17 publications

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

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

Characterization and Antioxidant Activity of the Complex of Phloridzin and Hydroxypropyl-β- cyclodextrin

Development and Optimization of Intravenous Puerarin Emulsions Formation by a Novel Complex-Phase Inversion-Homogenization Technology

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