Development of tamoxifen-phospholipid complex: Novel approach for improving solubility and bioavailability

Jena, Sunil Kumar; Singh, Charan; Dora, Chander Parkash; Suresh, Sarasija

doi:10.1016/j.ijpharm.2014.06.056

Cited by 99 publications

(37 citation statements)

References 26 publications

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“…3. DSC thermograms of a SCE, b Phospholipon® 90H, c physical mixture, and d CN phospholipid complexes (44,48). The disappearance of the SCE crystalline peaks thus confirmed the formation of SCEphospholipid complex.…”

Section: Differential Scanning Calorimetrymentioning

confidence: 68%

“…The disappearance of peak at 1563 cm −1 (exhibiting the aromatic ring stretching) may be due to the weakening, or removal, or shielding by the phospholipid molecule, which may further support the formation of naturosome. This phenomenon may be explained as occurring due to the entrapment/packing of the SCE in the hydrophobic cavity of the formed phospholipid vesicle, and being held by van der Waals forces, and other hydrophobic interactions (44). The presence of the peaks at 1468, 1418, and 1378 cm −1 exhibits the C-H bending and rocking.…”

Section: Fourier Transform Infrared Spectroscopymentioning

confidence: 98%

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Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Saoji

Raut

Dhore

et al. 2015

AAPS J

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Abstract. In the present study, a phospholipid-based complex of standardized Centella extract (SCE) was developed with a goal of improving the bioavailability of its phytoconstituents. The SCE-phospholipid complex was prepared by solvent evaporation method and characterized for its physicochemical and functional properties. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), photomicroscopy, and powder x-ray diffraction (PXRD) were used to confirm the formation of Centella naturosome (CN). The prepared complex was functionally evaluated by apparent solubility, in vitro drug release, ex vivo permeation, and in vivo efficacy studies. The prepared CN exhibited a significantly higher (12-fold) aqueous solubility (98.0±1.4 μg/mL), compared to the pure SCE (8.12±0.44 μg/mL), or the physical mixture of SCE and the phospholipid (13.6±0.4 μg/mL). The in vitro dissolution studies revealed a significantly higher efficiency of CN in releasing the SCE (99.2±4.7, % w/w) in comparison to the pure SCE (39.2±2.3, % w/w), or the physical mixture (42.8±2.09, % w/w). The ex vivo permeation studies with the everted intestine method showed that the prepared CN significantly improved the permeation of SCE (82.8±3.7, % w/w), compared to the pure SCE (26.8±2.4, % w/w), or the physical mixture (33.0±2.7, % w/w). The in vivo efficacy studies using the Morris Water Maze test indicated a significant improvement of the spatial learning and memory in aged mice treated with CN. Thus, drug-phospholipid complexation appears to be a promising strategy to improve the aqueous solubility and bioavailability of bioactive phytoconstituents.

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Section: Differential Scanning Calorimetrymentioning

confidence: 68%

Section: Fourier Transform Infrared Spectroscopymentioning

confidence: 98%

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Saoji

Raut

Dhore

et al. 2015

AAPS J

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“…Moreover, X‐ray diffraction study was also performed to confirm the physical state of the drug in optimized TMX‐SLNs. TMX exhibited sharp and distinctive peaks at 2θ angles of 5.55°, 9.79°, 14.95°, 16.49°, 19.20° and 21.05° indicating its crystalline nature . The characteristic peaks of TMX were evident in PM, while absent in optimized TMX‐SLNs (Figure S6f).…”

Section: Resultsmentioning

confidence: 97%

“…The plasma concentration–time profile of TMX and optimized formulation of TMX‐SLNs exhibited biphasic profile indicating TMX undergoes enterohepatic circulation (Figure a) . The relative bioavailability of the optimized formulation of TMX‐SLNs was approximately 1.59‐fold higher than that of TMX suspension.…”

Section: Resultsmentioning

confidence: 99%

Alpha-lipoic acid–stearylamine conjugate-based solid lipid nanoparticles for tamoxifen delivery: formulation, optimization, in-vivo pharmacokinetic and hepatotoxicity study

Dhaundiyal

Jena

Samal

et al. 2016

Journal of Pharmacy and Pharmacology

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“…The significant difference of DSC graphs among four samples indicated that the AmB and phospholipids in the complex were amorphous. All the results suggested that some weak interactions, such as the hydrogen bonds or Vander Waals force are formed between AmB and phospholipid molecules [22][23][24][25][26] . o indicating its crystalline characteristics.…”

Section: Stability Of Suspension Of Amb Lipid Complexmentioning

confidence: 99%

A facile microfluidic method for production of amphotericin B lipid complex

Yen¹,

Duong²,

L³

et al. 2017

Pharm Sci Asia

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Amphotericin B (AmB) is a large amphiphilic molecule, which is a drug of choice in therapy of systemic fungal infection because of its board-spectrum antifungal activity. However, conventional formulation of AmB is micelles, which is unstable in the bloodstream and releases drug to form toxic aggregates. Lipid complex of AmB has been developed to reduce toxicity while retaining activity. Microfluidic method is mixing technique, which permits millisecond mixing at the nano/microliter scale, can reproducibly generate limit size of particles of drug delivery system. In this study, microfluidic hydrodynamic focusing method was used to produce AmB lipid complex. It was obtained of two synthetic phospholipids: hydrogenated soy phosphatidylcholine (HSPC), distearoylphosphatidylglycerol (DSPG) and AmB in the molar ratio of 1:1:2.The lipid complex of AmB was characterized using differential scanning calorimetry (DSC), X -ray diffraction, Fourier-transform infrared spectroscopy (FTIR) and Field Emission Scanning Electron Microscopy(FESEM).The results showed that AmB lipid complex, prepared by microfluidic method, had smallest size at the flow rate ratio (FRR) of 5:1. The distinct phase transition temperature, the crystal peak of phospholipid, the characteristic band of-P-O-group of phospholipid were not observed in the DSC curve, X-ray diffraction diagram and FTIR spectra, respectively, of AmB lipid complex.

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Development of tamoxifen-phospholipid complex: Novel approach for improving solubility and bioavailability

Cited by 99 publications

References 26 publications

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Alpha-lipoic acid–stearylamine conjugate-based solid lipid nanoparticles for tamoxifen delivery: formulation, optimization, in-vivo pharmacokinetic and hepatotoxicity study

A facile microfluidic method for production of amphotericin B lipid complex

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