Resveratrol Loaded Self-Microemulsifying Drug Delivery System (SMEDDS): Development and Optimization

2014 ◽  
Vol 936 ◽  
pp. 763-769
Author(s):  
Guo Qing Liu ◽  
Hua Feng Zhou ◽  
Jing Zhang ◽  
Ze Min Yan ◽  
Ming Xing Duan ◽  
...  

We developed a SMEDDS to enhance the oral delivery of resveratrol by using high performance liquid chromatography, a pseudo ternary phase diagram and a central composite design (CCD). We found that the optimal formulation of 12.69% greoil gtcc, 62.29% Cremophor EL, and 25.02% Labrasol. We characterized the particle size and zeta potential of the final SMEDDS.

2013 ◽  
Vol 11 (2) ◽  
pp. 83-91
Author(s):  
Fariba Khan ◽  
Md Saiful Islam ◽  
Reza-ul Jalil

Self-emulsifying drug delivery system (SEDDS) is successfully used to improve the aqueous solubility and oral bioavailability of the poorly aqueous soluble drugs. Atorvastatin calcium (ATV), a poorly aqueous soluble drug having low oral bioavailability, was the model drug for this study. The aim of this study was to find out the suitable lipid and surfactant which can be used in formulation of ATV-SEDDS and this was done using ternary phase diagram, an important tool used very essentially in optimizing SEDDS formulations. Ternary phase diagrams of lipid/surfactant/ATV mixture were constructed to generate the solubility data of ATV. Two lipids namely Capmul PG 8, Oleic acid and seven different surfactants namely Tween 20, Tween 80, Cremophor CO 40, Cremophor CO 60, Cremophor EL, Cremophor RH 40 and Cremophor RH 60 were used. For Capmul PG 8/surfactant mixture, solubilizing efficiency order was: Cremophor RH 40 > Tween 80 > Tween 20 > Cremophor CO 60 > Cremophor RH 60 > Cremophor EL > Cremophor CO 40. For Oleic acid/surfactant mixture, solubilizing efficiency order was: Cremophor RH 40 > Tween 80 > Tween 20 > Cremophor RH 60 > Cremophor CO 60 > Cremophor EL > Cremophor CO 40. Considering the solubility phase diagrams of the drug, both Oleic acid and Capmul PG 8 can be used as lipid in combination with any of the surfactants, Cremophor RH40 or Tween 80 or Tween 20 for the development of SEDDS formulations of ATV having enhanced solubility and dissolution property. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14507 Dhaka Univ. J. Pharm. Sci. 11(2): 83-91, 2012 (December)


Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 247 ◽  
Author(s):  
Rae Kim ◽  
Dong-Jin Jang ◽  
Yu Kim ◽  
Jin-Ha Yoon ◽  
Kyoung Min ◽  
...  

The aim of this work was to prepare and optimize a solid self-nanoemulsifying drug delivery system pre-concentrate (SSP) containing water-insoluble flurbiprofen (FL) using a novel pseudo-ternary phase diagram. The pseudo-ternary phase diagram, composed of FL as the drug and dispersion core, Kollisolv MCT 70 as the oil phase, and TPGS (tocopherol polyethylene glycol 1000 succinate) as the surfactant, was constructed for the determination of the SSP region. SSP was investigated in terms of particle size, physical state by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), in vitro dissolution and oral pharmacokinetics in rats. The determined SSP (FL/Kollisolv MCT 70/TPGS = 10/10/80, weight %) in the pseudo-ternary phase diagram had the melting point of 32.37 °C and uniform mean particle size of below 30 nm without any precipitation of FL in the dispersion. In the dissolution test, the SSP exhibited 95.70 ± 3.40% of release at 15 min, whereas the raw FL showed poor dissolution (i.e., 6.75 ± 1.30%) at that time point. In addition, the SSP showed the enhanced oral absorption (i.e., 1.93-fold increase in AUCinfinite) as compared to the suspension group of raw FL. Therefore, the developed SSP would be a promising drug delivery system with excellent solubilization, dissolution, and bioavailability for FL.


Author(s):  
Priyal Patel ◽  
Shilpa Solanki ◽  
Ashok Mahajan ◽  
Falgun Mehta ◽  
Kautuk Shah

The aim of research was to develop self nanoemulsifying drug delivery technology containing low aqueous soluble drug allopurinol for improving solubility, dissolution and bioavaibility. Preliminary screening were carried on the basis of maximum solubility of allopurinol in oil, surfactant, co-surfactant and pseudo-ternary phase diagram was constructed to identify the ratio of surfactant and co-surfactant for nanoemulsion formulation using water titration method. Based on the solubility study, Labrafil M 1944 CS, Cremophor RH 40, Transcutol used as oil, surfactant, and co-surfactant respectively. Pseudo-ternary phase diagram was constructed to identify the ratio of surfactant and co-surfactant for nanoemulsion formation by water titration method. As per the ternary phase diagram ratio of Smix in 2:1 was identified with maximum emulsification area. SNEDDS composed of 35 % Labrafil M 1944 CS, 43.34% Cremophor RH 40, 21.66% Transcutol. Globule size was found to be 25.42 nm, and zeta potential value was -9.26 mV. Prepared SNEDDS were evaluated for globule size, viscosity, emulsification time, cloud point, dilution test and thermodynamic stability study. Prepared liquid SNEDDS then converted into solid SNEDDS via extrusion/spheronization technique using Aerosil 200, lactose monohydrate and Croscarmellose sodium. The pellets containing SNEDDS possessed good flow properties and mechanical strength and other rheological parameters. Self nanoemulsifying pellet exhibited uniform size and shape. Friability, dissolution time and disintegration of pellets formulation shown promising results. Time required for 80% drug release of self nanoemulsifying pellet was found to be 26 min, which was significantly lower than liquid SNEDDS, plain drug containing pellet and marketed preparation of Allopurinol (ZYRIK).


2021 ◽  
Vol 1162 ◽  
pp. 119-128
Author(s):  
Yandi Syukri ◽  
Siti Asmaliah ◽  
Lutfi Chabib ◽  
Annisa Fitria

Propolis is a poorly water-soluble substance contain natural resinous produced by honey bees. Self-nanoemulsifying (SNE) play a role not only to increase the solubility of propolis but also to improve the pharmacological activity. The aim of the present study is to fabrication and characterization self-nanoemulsifying of propolis extract (SNEPE) using virgin coconut oil (VCO) as the lipid-based vehicle. VCO (lipid-based), cremophor RH 40 (surfactant) and polyethylene glycol (PEG) 400 with concentration 10-50; 10-80; 10-40% respectively was used to construction pseudo ternary phase diagram. The formulations that selected in the pseudo ternary phase diagram is continued for the fabrication of SNEPE. The formation of SNEPE was characterized include transmittance, particle size, zeta potential, thermodynamic stability test, robustness to dilution test, and accelerated stability test. The result showed that eight formulas using 10-20% of VCO, 40-80% of cremophor RH40, and 10-40% of PEG 400 were selected for the fabrication of SNEPE. SNEPE demonstrated the transmittance more than 90%, particle size with range 9,00±0,00 to 34,10±0,30 nm, and less than-30 mV of zeta potential. The formulation passed the thermodynamic stability test. The robustness to dilution test showed that three formulas with a ratio of 20: 70: 10, 20: 60: 20, and 20: 50: 30 are the most stable formulations in various dilution. The formulas are also stable during accelerated stability study. The results can be concluded that VCO, cremophor RH40, and PEG 400 as a vehicle to produce stable SNEPE.


Author(s):  
Rachel Orenstein ◽  
James P. Male ◽  
Michael Toriyama ◽  
Shashwat Anand ◽  
G. Jeffrey Snyder

A new understanding of the MgSi–MgSn miscibility gap is reached through phase boundary mapping the Mg–Si–Sn ternary phase diagram.


1984 ◽  
Vol 62 (3) ◽  
pp. 457-474 ◽  
Author(s):  
A. D. Pelton ◽  
C. W. Bale ◽  
P. L. Lin

Phase diagrams and thermodynamic properties of five additive molten salt ternary systems and nine reciprocal molten salt ternary systems containing the ions Li+, Na+, [Formula: see text], OH− are calculated from the thermodynamic properties of their binary subsystems which were obtained previously by a critical assessment of the thermodynamic data and the phase diagrams in these binary systems. Thermodynamic properties of ternary liquid phases are estimated from the binary properties by means of the Conformal Ionic Solution Theory. The ternary phase diagrams are then calculated from these thermodynamic properties by means of computer programs designed for the purpose. It is found that a ternary phase diagram can generally be calculated in this way with a maximum error about twice that of the maximum error in the binary phase diagrams upon which the calculations are based. If, in addition, some reliable ternary phase diagram measurements are available, these can be used to obtain small ternary correction terms. In this way, ternary phase diagram measurements can be smoothed and the isotherms drawn in a thermodynamically correct way. The thermodynamic approach permits experimental data to be critically assessed in the light of thermodynamic principles and accepted solution models. A critical assessment of error limits on all the calculated ternary diagrams is made, and suggestions as to which composition regions merit further experimental study are given.


2014 ◽  
Vol 59 (4) ◽  
pp. 1393-1404 ◽  
Author(s):  
W. Wołczynski ◽  
Z. Pogoda ◽  
G. Garzeł ◽  
B. Kucharska ◽  
A. Sypien ◽  
...  

Abstract A mathematical description for the (Zn) - coating formation with the presence of flux in the zinc bath is presented. This description includes the progressive vanishing of the products of the flux disintegration. A function which expresses the flux vanishing is formulated. The solidification of some phase sub-layers in the (Zn) - coating is considered with the use of a hypothetical pseudo-ternary phase diagram Fe-Zn-flux. Some relationships are formulated to define the varying Zn - solute redistribution as observed across the sub-layers. The relationships are based on the mass balance analyzed for the coating / bath / flux system. An amount of the growing phase in a given sub-layers is also defined mathematically.


2015 ◽  
Vol 38 (6) ◽  
pp. 1073-1080 ◽  
Author(s):  
Kyeong-Sill Lee ◽  
Kwang-Joo Kim ◽  
Joachim Ulrich

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