Development and Permeability Testing of Self-Emulsifying Atorvastatin Calcium Pellets and Tablets of Compressed Pellets

Diril, Mine; Karasulu, H. Yeşim; Toskas, Miltiadis; Nikolakakis, Ioannis

doi:10.3390/pr7060365

Cited by 12 publications

(4 citation statements)

References 48 publications

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“…As the loading amount can be influenced by the solubility and miscibility of the drug in the lipid matrix, therefore, higher EE% due to a reduction in the HLB could be as a result of the high solubility of atorvastatin in Span 80 (solubility of atorvastatin calcium in span 80 is 47.47 mg/ml) (31). Reduction in the HLB value is accompanied by increasing the amount of Span 80 which can help to load atorvastatin (log p = 6.98 and water solubility is 0.00063 mg/ml) into the solid lipid (14).…”

Section: Effect Of Hlb Of Surfactants On Nanoparticles Propertiesmentioning

confidence: 99%

Atorvastatin Solid Lipid Nanoparticles as a Promising Approach for Dermal Delivery and an Anti-inflammatory Agent

et al. 2020

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In the current research, the main focus was to overcome dermal delivery problems of atorvastatin. To this end, atorvastatin solid lipid nanoparticles (ATR-SLNs) were prepared by ultra-sonication technique. The prepared SLNs had a PDI value of ≤ 0.5, and the particle size of nanoparticles was in the range 71.07 ± 1.72 to 202.07 ± 8.40 nm. It was noticed that, when the concentration of lipid in ATR-SLNs increased, the size of nanoparticles and drug entrapment efficiency were also increased. Results showed that a reduction in the HLB of surfactants used in the preparation of SLN caused an increase in the particle size, zeta potential (better stability), and drug entrapment efficiency. Despite Tween and Span are non-ionic surfactants, SLNs containing these surfactants showed a negative zeta potential, and the absolute zeta potential increased when the concentration of Span 80 was at maximum. DSC thermograms, FTIR spectra, and x-ray diffraction (PXRD) pattern showed good incorporation of ATR in the nanoparticles without any chemical interaction. In vitro skin permeation results showed that SLN containing atorvastatin was capable of enhancing the dermal delivery of atorvastatin where a higher concentration of atorvastatin can be detected in skin layers. This is a hopeful promise which could be developed for clinical studies of the dermal delivery of atorvastatin nanoparticles as an anti-inflammatory agent.

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Section: Effect Of Hlb Of Surfactants On Nanoparticles Propertiesmentioning

confidence: 99%

Atorvastatin Solid Lipid Nanoparticles as a Promising Approach for Dermal Delivery and an Anti-inflammatory Agent

et al. 2020

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“…This is a program-based in silico simulation and prediction software used for pharmaceutical products (dosage form) in various animal models (rodents, primates, and animals). The software uses various models based on drug characteristics, formulation properties, and biopharmaceutics of the model drug. − There are several data sets in the input tab as default values. The program offered three different tabs such as the compound tab for physicochemical properties of the model compound, the physiological tab to set the physiological condition for the outcome, and the pharmacokinetics tab for the pharmacokinetic profile of the drug.…”

Section: Methodsmentioning

confidence: 99%

Preferential Solvation Study of Rosuvastatin in the {PEG400 (1) + Water (2)} Cosolvent Mixture and GastroPlus Software-Based In Vivo Predictions

et al. 2023

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Rosuvastatin (RST) is a poorly water-soluble drug responsible for limited in vivo dissolution and subsequently low oral systemic absorption (poor bioavailability). The mole fraction solubility values of RST in various ratios of binary mixtures “{PEG400 (1) + water (2)}” at 298.15 K were employed to investigate the preferential solvation (PS) of RST (3) by the binary components. Moreover, the GastroPlus program predicted the drug dissolution/absorption rates, plasma drug concentration, and compartmental regional drug absorbed from a conventional tablet as compared to the RST-loaded (PEG400 + water) mixture (at x 1 = 0.5) in healthy subjects (considering the fast condition). Fedors’ method was adopted to estimate the values of molar volume (314.8 cm3·mol–1) and Hildebrand solubility parameter (28.08 MPa1/2) of RST. The results of inverse Kirkwood–Buff integrals showed the PS of RST by PEG400 as observed in all studied ratios of the binary mixture. The highest PS value (δx 1,3 = 1.65 × 10–2) for RST by PEG400 was attained at x 1 = 0.5. Finally, the GastroPlus program predicted the maximum dissolution rate [20 mg within 15 min as compared to pure RST (1.5 mg within 15 min)]. Moreover, the program predicted increased in vivo oral absorption (1.2 μg/mL) and enhanced regional absorption (95.3%) of RST from upper segments of the gastrointestinal tract for the RST-loaded PEG400 + water mixture in humans as compared to conventional tablets (87.5% as total regional absorption and 0.88 μg/mL as in vivo absorption). Hence, the present binary system ferrying RST can be a promising strategy to control systemic dyslipidemia after oral or subcutaneous administration.

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“…Samples of 200 µl were collected at 0, 30, 60, 90, and 120 minutes (n=3). The apparent permeability coefficient (Papp, cm s −1 ) was calculated from the slope (dQ/t) of the linear portion of the plots depicting the cumulative amounts of permeated VST (Q) over time (t), as per Equation 1 [14]. The quantity of drug remaining on the surface and inside of the polycarbonate membrane was also determined to assess the method's validity.…”

Section: In Vitro Permeability Studiesmentioning

confidence: 99%

Liquid and Solid Self-Emulsifying Drug Delivery Systems (Sedds) Containing Valsartan: Stability Assessment and Permeability Studies

Yıldız Türkyılmaz,

Diril,

Gülmezoğlu

et al. 2024

Ankara Ecz. Fak. Derg.

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Objective: Valsartan (VST) is a Biopharmaceutical classification system (BSC) class II active ingredient with a bioavailability of approximately 25% and is utilized to treat high blood pressure (hypertension). This study aimed was to showcase the stability and increase the permeability of VST by developing self-emulsifying drug delivery systems (SEDDS) and solidified SEDDS (S-SEDDS) formulations. Material and Method: The ratios of the components were determined by the pseudo-ternary phase diagram, and the characterization studies were conducted in the previous study. Stability was performed in long-term (25±2˚C, 60±5% relative humidity) and accelerated (40±2˚C, 75±5% relative humidity) conditions. The intestinal permeability of SEDDS formulations was evaluated by Caco-2 cells. Result and Discussion: Formulations for 12 month, droplet sizes were found to be 67.52 ± 5.26 nm and 176.93 ± 17.34 nm for SEDDS of VST (VST-SEDDS) and S-SEDDS of VST (VST-S-SEDDS), respectively. During this period, polydispersity indexes were: VST-SEDDS, 0.56±0.1; VST-S-SEDDS, 0.58±0.05. Both formulations increased VST permeability across Caco-2 cells: VST-SEDDS by 2.32x (powder) and 2.18x (commercial); VST-S-SEDDS by 1.38x (powder) and 1.30x (commercial). The formulation components did not have cytotoxic effects. These results demonstrated that newly developed VST-SEDDS and VST-S-SEDDS formulations with high permeability may be a desirable approach for antihypertensive therapy.

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Development and Permeability Testing of Self-Emulsifying Atorvastatin Calcium Pellets and Tablets of Compressed Pellets

Cited by 12 publications

References 48 publications

Atorvastatin Solid Lipid Nanoparticles as a Promising Approach for Dermal Delivery and an Anti-inflammatory Agent

Atorvastatin Solid Lipid Nanoparticles as a Promising Approach for Dermal Delivery and an Anti-inflammatory Agent

Preferential Solvation Study of Rosuvastatin in the {PEG400 (1) + Water (2)} Cosolvent Mixture and GastroPlus Software-Based In Vivo Predictions

Liquid and Solid Self-Emulsifying Drug Delivery Systems (Sedds) Containing Valsartan: Stability Assessment and Permeability Studies

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