Solubility of simvastatin: A theoretical and experimental study

Aceves-Hernández, Juan Manuel; Hinojosa-Torres, J.; Nicolás–Vázquez, María Inés; Ruvalcaba, René Miranda; García, Rosa María Lima

doi:10.1016/j.molstruc.2011.03.048

Cited by 19 publications

(25 citation statements)

References 26 publications

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“…The particle size distribution, PDI, and ZP of simvastatin loaded SLNs were measured using a Malvern Zetasizer (Nano ZS90, UK). About 100 L of the prepared SLN dispersion was diluted to 5 mL with double distilled water and analyzed with Zetasizer [13].…”

Section: Measurement Of Particle Size Polydispersity Index (Pdi) Anmentioning

confidence: 99%

“…The solid lipid nanoparticles along with the encapsulated drug remain in the outer chamber and the aqueous phase is moved into the sample recovery chamber through membrane. The amount of drug in the aqueous phase is estimated by HPLC [13,14].…”

Section: Entrapment Efficiencymentioning

confidence: 99%

“…Excess dispersion was blotted from the grid with filter paper to form a thin-film specimen. The sample was then stained with 2% uranyl acetate, airdried, and examined under transmission electron microscope (Hitachi, H-7500) at a magnification of 50KX [13].…”

Section: Visualization By Transmission Electron Microscopymentioning

confidence: 99%

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Factorial Design Studies and Biopharmaceutical Evaluation of Simvastatin Loaded Solid Lipid Nanoparticles for Improving the Oral Bioavailability

Raju

Sudhakar

Murthy

2014

ISRN Nanotechnology

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Statins are HMG-CoA reductase inhibitors, which lower the cholesterol level through reversible and competitive inhibition; they are involved in the biosynthesis of cholesterol and other sterols. Simvastatin exhibits poor oral bioavailability (<5%) and undergoes extensive microsomal metabolism by CYP enzymes. CYP3A4 is the major metabolizing enzyme that metabolizes lactone form of simvastatin and significantly lowers intestinal uptake. The hydrophobic properties of simvastatin prevent complete dissolution of the drug in the intestinal fluid which also contributes to its lower bioavailability. SLNs are alternative carrier system to polymeric nanoparticles. SLNs are in submicron size range (1–1000 nm). To overcome the hepatic first pass metabolism and to enhance the bioavailability, intestinal lymphatic transport of drugs can be exploited. In the present study, attempt has been made to prepare solid lipid nanoparticles of simvastatin to improve the bioavailability. SLNs of simvastatin were prepared with Trimyristin by hot homogenization followed by ultrasonication method. The SLNs were characterized for various physicochemical properties and analytical techniques like PXRD, DSC to study thermal nature and morphology of formulation and excipients. Promising results of the study indicated the applicability of simvastatin solid lipid nanoparticles as potential tools for improvement of bioavailability of poorly soluble drugs.

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Section: Measurement Of Particle Size Polydispersity Index (Pdi) Anmentioning

confidence: 99%

Section: Entrapment Efficiencymentioning

confidence: 99%

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Factorial Design Studies and Biopharmaceutical Evaluation of Simvastatin Loaded Solid Lipid Nanoparticles for Improving the Oral Bioavailability

Raju

Sudhakar

Murthy

2014

ISRN Nanotechnology

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“…The reported octanol solubilities and melting points of 224 compounds were taken from the literature (see Table S1) 1,9,12–35. The molar volumes and solubility parameters were taken from literature36–50 or calculated using Fedors' group contribution method 51.…”

Section: Data Collectionmentioning

confidence: 99%

Predicting the Octanol Solubility of Organic Compounds

Admire

Yalkowsky

2013

Journal of Pharmaceutical Sciences

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“…Simvastatin (SIM) {molecular structure: Fig 1 ; chemical name: [(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] 2,2-dimethylbutanoate; molecular formula: C 25 H 38 O 5 ; molar mass: 418.57 g mol -1 and CASRN: 79902-63-9) occurs as a white to off-white crystalline powder [ 1 , 2 ]. It is a lipid lowering agent which belongs to statins family and powerful inhibitor of (3,5)-hydroxy-3-methylglutaryl coenzyme A (HMGr-CoA) reductase [ 3 , 4 ].…”

Section: Introductionmentioning

confidence: 99%

Solubilization and thermodynamic properties of simvastatin in various micellar solutions of different non-ionic surfactants: Computational modeling and solubilization capacity

et al. 2021

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The aim of this work was to solubilize simvastatin (SIM) using different micellar solutions of various non-ionic surfactants such as Tween-80 (T80), Tween-20 (T20), Myrj-52 (M52), Myrj-59 (M59), Brij-35 (B35) and Brij-58 (B58). The solubility of SIM in water (H2O) and different micellar concentrations of T80, T20, M52, M59, B35 and B58 was determined at temperatures T = 300.2 K to 320.2 K under atmospheric pressure p = 0.1 MPa using saturation shake flask method. The experimental solubility data of SIM was regressed using van’t Hoff and Apelblat models. The solubility of SIM (mole fraction) was recorded highest in M59 (1.54 x 10−2) followed by M52 (6.56 x 10−3), B58 (5.52 x 10−3), B35 (3.97 x 10−3), T80 (1.68 x 10−3), T20 (1.16 x 10−3) [the concentration of surfactants was 20 mM in H2O in all cases] and H2O (1.94 x 10−6) at T = 320.2 K. The same results were also recorded at each temperature and each micellar concentration of T80, T20, M52, M59, B35 and B58. “Apparent thermodynamic analysis” showed endothermic and entropy-driven dissolution/solubilization of SIM in H2O and various micellar solutions of T80, T20, M52, M59, B35 and B58.

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Solubility of simvastatin: A theoretical and experimental study

Cited by 19 publications

References 26 publications

Factorial Design Studies and Biopharmaceutical Evaluation of Simvastatin Loaded Solid Lipid Nanoparticles for Improving the Oral Bioavailability

Factorial Design Studies and Biopharmaceutical Evaluation of Simvastatin Loaded Solid Lipid Nanoparticles for Improving the Oral Bioavailability

Predicting the Octanol Solubility of Organic Compounds

Solubilization and thermodynamic properties of simvastatin in various micellar solutions of different non-ionic surfactants: Computational modeling and solubilization capacity

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