Solubility and stability of tetrazepam in mixed micelles

Hammad, Mohamed A.; Müller, Bernd W.

doi:10.1016/s0928-0987(98)00006-2

Cited by 49 publications

(29 citation statements)

References 14 publications

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“…Bile salts (BS), detergent-like chemicals produced by the liver and stored in the gall bladder, are able to solubilize phosphatidylcholine www.chinaphar.com Duan RL et al Acta Pharmacologica Sinica npg (PC) to a large extent, forming a clear mixed micellar solution that is able to solubilize substances with poor water solubility [20] . Previous studies have shown that the hemolytic effect of bile salts can be neutralized by solubilized phospholipids [21] .…”

Section: Introductionmentioning

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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Section: Introductionmentioning

confidence: 99%

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

et al. 2010

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“…Hydrophilic parts of the molecules form the micelle corona. Micelle encapsulation increases bioavailability of poorly soluble drugs, protects them from destruction in biological surroundings, and beneficially modifies their pharmacokinetics and biodistribution (11). Because of their small size (usually 5-50 nm), micelles demonstrate spontaneous accumulation in pathological areas with leaky vasculature, such as infarct zones (12) and tumors (13,14).…”

mentioning

confidence: 99%

Immunomicelles: Targeted pharmaceutical carriers for poorly soluble drugs

Torchilin

Lukyanov

Gao

et al. 2003

Proc. Natl. Acad. Sci. U.S.A.

524

309

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“…Based on its physiological compatibility and solubilizing capacity, a phosphatidylcholine (PC)-bile salts (BS)-mixed micelle (MM) formulation is an attractive candidate for the intravenous administration of poorly soluble drugs. [14][15][16][17][18][19][20] This simple approach of combining a water-soluble surfactant with a water-insoluble phospholipid results in an isotropically clear solution. 21,22 Many studies have been published regarding the preparation and characterization of PC-BS-MMs.…”

Section: Introductionmentioning

confidence: 99%

“…21,22 Many studies have been published regarding the preparation and characterization of PC-BS-MMs. 16,[23][24][25][26] BS present in bile with a high concentration can solubilize PC to a large extent, forming a kind of clear mixed-micellar solution that in turn can solubilize substances with poor water solubility. 16,19 With the solubilized phospholipids, the hemolytic effects of BS can be neutralized.…”

Section: Introductionmentioning

confidence: 99%

“…16,[23][24][25][26] BS present in bile with a high concentration can solubilize PC to a large extent, forming a kind of clear mixed-micellar solution that in turn can solubilize substances with poor water solubility. 16,19 With the solubilized phospholipids, the hemolytic effects of BS can be neutralized. 27 Most importantly, PC-BS-MMs have been proven to be locally and systemically well tolerated, with no embryotoxic, teratogenic, or mutagenic effects after administration.…”

Section: Introductionmentioning

confidence: 99%

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Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study

Jiang²,

Ren³

et al. 2012

IJN

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Background:The clinical application of nimodipine (NIM) is limited by several unfavorable properties, which are induced by its low aqueous solubility. In the present study, nimodipineloaded egg phosphatidylcholine-sodium glycocholate mixed micelles (NIM-EPC-SGC-MMs) were prepared to improve the water solubility of NIM, thus allowing it to be more applicable for clinical use. Methods: NIM-EPC-SGC-MMs were prepared using the coprecipitation method and the factors influencing formulation quality were optimized. After formulation, water solubility, solubilizing efficiency, drug loading, particle size, physical compatibility, pharmacokinetics, and vascular irritability were determined. Results: The mean size of the NIM-EPC-SGC-MMs was 6.099 ± 0.048 nm under optimized conditions. The water solubility of NIM in EPC-SGC-MMs was enhanced 250-fold compared with free NIM. The physical compatibility, pharmacokinetic, and vascular irritability studies showed that, in comparison to the commercially available NIM injections, NIM-EPC-SGCMMs presented better physical compatibility, the same pharmacokinetic profile, and less risk of local vascular irritation and phlebitis. Conclusion: EPC-SGC-MMs represent a promising new formulation suitable for the intravenous delivery of NIM.

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Solubility and stability of tetrazepam in mixed micelles

Cited by 49 publications

References 14 publications

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

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

Immunomicelles: Targeted pharmaceutical carriers for poorly soluble drugs

Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study

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