scholarly journals Study of Solubility of Atorvastatin using Ternary Phase Diagram for the Development of Self-Emulsifying Drug Delivery Systems (SEDDS)

2013 ◽  
Vol 11 (2) ◽  
pp. 83-91
Author(s):  
Fariba Khan ◽  
Md Saiful Islam ◽  
Reza-ul Jalil
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Oleic Acid ◽  
Oral Bioavailability ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Tween 80 ◽  
Tween 20 ◽  
Surfactant Mixture ◽  
Cremophor El

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)

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 ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Particle Size ◽  
High Performance Liquid Chromatography ◽  
Oral Delivery ◽  
High Performance ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Cremophor El ◽  
Central Composite

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.

Preparation and Characterization of Novel Self Nano Emulsifying Drug Delivery System of Allopurinol

2021 ◽  
pp. 2108-2114
Author(s):  
Priyal Patel ◽  
Shilpa Solanki ◽  
Ashok Mahajan ◽  
Falgun Mehta ◽  
Kautuk Shah
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Stability Study ◽  
Rheological Parameters ◽  
Dissolution Time ◽  
Titration Method ◽  
Uniform Size ◽  
Globule Size

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).

Design and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Rosuvastatin

2018 ◽  
Vol 11 (2) ◽  
pp. 4042-4052
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Priya Keerthi
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Oral Bioavailability ◽  
Drug Delivery Systems ◽  
Ternary Phase Diagram ◽  
Delivery Systems ◽  
Water Soluble ◽  
Lipid Lowering ◽  
Tween 20 ◽  
Onset Of Action

Development of self-emulsifying drug delivery systems (SEDDS) are becoming more popular to improve the oral bioavailability of poorly water-soluble drugs. Rosuvastatin is a lipid-lowering agent used in patients suffering from dyslipidemia. It is a competitive inhibitor of 3-hydroxy 3-methyl glutaryl coenzyme A, which converts mevalonate to cholesterol. Rosuvastatin is a BCS class II (poor solubility) drug; hence, SNEDDS are being formulated to enhance oral bioavailability of the drug. In the present study, rosuvastatin SNEDDS were formulated using different oils, surfactant and co-surfactant. The optimized formulation F9 has composition of Las (PEG-8-Caprylic glycerides), Maisine 35-1 and Tween 20 as oil phase, surfactant and co-surfactant respectively. Composition of SNEDDS was optimized using Pseudo-ternary phase diagram, where the formulations showed increased self-emulsification with increased concentration of surfactants. Formulation F9 was found to be best formulation based on evaluation parameters. The particle size of the optimized SNEDDS formulation was found to be 10.9 nm & Z-Average of 55.6 nm indicating all the particles were in the nanometer range. The zeta potential of the optimized SNEDDS formulation was found to be -11.2 mV, which comply with the requirement of the zeta potential for stability. The developed rosuvastatin SNEDDS have the potential to minimize the variability in absorption and provide rapid onset of action of the drug.   

scholarly journals New Approach for Administration of Doxazosin Mesylate: Comparative Study between Liquid and Solid Self-nanoemulsifying Drug Delivery Systems

2021 ◽  
Vol 12 (2) ◽  
pp. 1095-1101
Author(s):  
Al Zahraa G. Al Ashmawy ◽  
Noura G. Eissa ◽  
Gehan F. Balata ◽  
Hanan M. El Nahas
Keyword(s):  
Drug Delivery ◽  
Oleic Acid ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Tween 80 ◽  
Delivery Systems ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Surfactant Mixture ◽  
Doxazosin Mesylate

Self-nanoemulsifying drug delivery systems (SNEDDS) in both liquid and solid forms were suggested to improve water solubility of Doxazosin mesylate (DOX) a poorly water- soluble antihypertensive drug. Oleic acid: Smix (1:9 w/w) and Tween 80: co-surfactant mixture (Ethanol and PEG 400) (1:1, 2:1, 3:1 and 4:1) were chosen to prepare a liquid and solid forms of SNEDDS according to their solubility. TEM images revealed change in the  crystalline nature of DOX into uniform particles with smooth surface. Characterization studies revealed droplet size ranges from  79.80±14.39 to 273.10±4.17 nm, zeta potential ranges from -5.57±0.10 to -21.13±0.46 mV and dissolution enhancement of more than two folds with more favorable properties for the solid forms. FTIR demonstrated significant physical changes in DOX crystalline structure. In conclusion, the solid SNEDDS containing oleic acid: Smix (1:9 w/w) and Tween 80: co-surfactant mixture (3:1 w/w) and adsorbent mixture of Avicel 101 and Aerosil 200 (40:1 w/w) might be a promising formula for better management of hypertension with expected shelf stability.

scholarly journals Formulation and evaluation of atorvastatin calcium niosomes

2021 ◽  
Vol 2 (1) ◽  
pp. 116-126
Author(s):  
Neha Rani ◽  
Rupali Rana ◽  
Reena Thakur ◽  
Shivali Singla ◽  
Sachin Goyal
Keyword(s):  
Drug Delivery ◽  
Oral Bioavailability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Drug Carriers ◽  
Tween 20 ◽  
Atorvastatin Calcium ◽  
Span 60

Atorvastatin calcium is a HMG-CoA reductase inhibitor used for the treatment of hyperlipidaemia. It has oral bioavailability of ≤12 %. It also undergoes high first pass metabolism. It is highly soluble in acidic pH and absorbed more in the upper part of the gastrointestinal tract. In order, to improve the absorption and its oral bioavailability, niosomes of Atorvastatin calcium have been formulated and evaluated on different parameters. Niosomes play an increasingly important role in drug delivery as they can reduce toxicity and 000000000modify pharmacokinetic and bio-availability. Niosomes formulations of Atorvastatin calcium were successfully developed by thin film hydration technique using nonionic surfactant i.e. Span 40, Span 60 Span 80, Tween 20, Tween 40, Tween 80 and cholesterol at different concentrations. The formulations were evaluated for size, shape, and entrapment efficiency. In-vitro release and stability studies also performed. Results indicated that Niosomes were prepared succesfully work as promising drug carriers and promising drug delivery module.

scholarly journals Preparation and Characterization of Topical Letrozole Nanoemulsion for Breast Cancer

2020 ◽  
Vol 29 (1) ◽  
pp. 195-206
Author(s):  
Ihab D. Hammodi ◽  
Shaimaa N. Abd Alhammid
Keyword(s):  
Breast Cancer ◽  
Phase Diagram ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Enzyme System ◽  
Tween 80 ◽  
Deionized Water ◽  
Water Based ◽  
Solubility Studies

Letrozole (LZL) is a non-steroidal competitive aromatase enzyme system inhibitor. The aim of this study is to improve the permeation of LZL through the skin by preparing as nanoemulsion using various numbers of oils, surfactants and co-surfactant with deionized water. Based on solubility studies, mixtures of oleic acid oil and tween 80/ transcutol p as surfactant/co-surfactant (Smix) in different percentages were used to prepare nanoemulsions (NS). Therefore, 9 formulae of (o/w) LZL NS were formulated, then pseudo-ternary phase diagram was used as a useful tool to evaluate the NS domain at Smix ratios: 1:1, 2:1 and 3:1.

scholarly journals Flurbiprofen-Loaded Solid SNEDDS Preconcentrate for the Enhanced Solubility, In-Vitro Dissolution and Bioavailability in Rats

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 247 ◽  
Author(s):  
Rae Kim ◽  
Dong-Jin Jang ◽  
Yu Kim ◽  
Jin-Ha Yoon ◽  
Kyoung Min ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Particle Size ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
In Vitro Dissolution ◽  
Enhanced Solubility

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.

Using phase boundary mapping to resolve discrepancies in the Mg2Si–Mg2Sn miscibility gap

2021 ◽  
Author(s):  
Rachel Orenstein ◽  
James P. Male ◽  
Michael Toriyama ◽  
Shashwat Anand ◽  
G. Jeffrey Snyder
Keyword(s):  
Phase Diagram ◽  
Phase Boundary ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Miscibility Gap ◽  
Boundary Mapping

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

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