Development of self emulsifying lipid formulations of BCS class II drugs with low to medium lipophilicity

Jannin, Vincent; Chevrier, Stéphanie; Michenaud, Matthieu; Dumont, Camille; Belotti, Silvia; Chavant, Yann; Demarne, Frédéric

doi:10.1016/j.ijpharm.2015.09.009

Cited by 44 publications

(13 citation statements)

References 33 publications

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“…Pancreatin solution was prepared fresh each time before the experiment as described previously [26]. In brief, 1.0 g of pancreatin was dispersed in 5 mL of cold digestion medium free of bile salt and phospholipid (8 C, 1000 rpm; Eppendorf ThermoMixer C, Eppendorf AG, Hamburg, Germany) and pH was adjusted to 6.5 with 2 M NaOH.…”

Section: Sedds Lipolysismentioning

confidence: 99%

“…In brief, 1.0 g of pancreatin was dispersed in 5 mL of cold digestion medium free of bile salt and phospholipid (8 C, 1000 rpm; Eppendorf ThermoMixer C, Eppendorf AG, Hamburg, Germany) and pH was adjusted to 6.5 with 2 M NaOH. After 10 min, the enzyme suspension was centrifuged at 2800g and 5 C for 10 min (ROTINA 380 R, Andreas Hettich GmbH & Co.KG, Tuttlingen, Germany) [26] and the recovered supernatant was used for lipolysis experiments. Lipolysis was performed as follows: 1.0 g of SEDDS were emulsified in 36 mL of digestion medium (37 C) in a thermostat-jacketed glass reaction vessel (Metrohm V R AG, Herisau, Switzerland).…”

Section: Sedds Lipolysismentioning

confidence: 99%

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Development and in vitro characterization of self-emulsifying drug delivery system (SEDDS) for oral opioid peptide delivery

Zupančič¹,

Rohrer²,

Lam

et al. 2017

Drug Development and Industrial Pharmacy

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Section: Sedds Lipolysismentioning

confidence: 99%

Section: Sedds Lipolysismentioning

confidence: 99%

Development and in vitro characterization of self-emulsifying drug delivery system (SEDDS) for oral opioid peptide delivery

Zupančič¹,

Rohrer²,

Lam

et al. 2017

Drug Development and Industrial Pharmacy

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“…The concentration of drug was quantified by measuring the absorbance at specific wave length (238.73 nm) using UVvisible spectrophotometer. The content of drug was calculated from the standard calibration curve (Jannin et al 2015). Percent transmission measurement can be used to reflect clarity and micron size of globules.…”

Section: Characterization Of Liquid Smeddsmentioning

confidence: 99%

D-Optimal Mixture Design for Optimization of Self Microemulsifying Drug Delivery System of Simvastatin: Characterization and in Vitro Evaluation

Kg¹,

AT²,

JR³

et al. 2018

Bull. Pharm. Res.

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The objective of present research work was to develop self-micro emulsifying drug delivery system to improve the in vitro dissolution of a Biopharmaceutical Classification System Class II lipid lowering agent, simvastatin. Solubility study was performed to identify the potent oil, surfactant and co-surfactant showing highest solubility of simvastatin. The ternary phase diagrams were constructed for selected components to identify the area of microemulsion formation. D-optimal mixture design was applied for optimization using three formulation variables namely, oleic acid, Tween 80 and Cremophore EL. The liquid self-micro emulsifying drug delivery systems (SMEDDS) were evaluated for droplet size, self-emulsification time, percent transmittance and drug solubility. The optimized batch showed self-emulsification time and solubility. The optimized liquid formulation was solidified using Aerosil 200 to prepare solid SMEDDS. Solid SMEDDS showed good flow property and uniform drug content. Solid state characterization was performed by differential scanning calorimetry, X-ray diffraction study and scanning electron microscopy. The zeta potential and globule size was-3.66mV and 755.3 nm, respectively. The rate and extent of drug dissolution from solid SMEDDS was significantly higher than tablet formulation. The optimized formulation was found to be stable. These results demonstrate the potential of SMEDDS as a means of improving solubility and dissolution.

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“…In contrast, a significant increase (p50.05) of log P (DES/SDS) and log P (DES/AOT) to a positive value of 0.33 was observed ( Figure 3B). Although a positive log P value was reached, DES/AOT and DES/SDS are still considered hydrophilic in comparison with low lipophilic drugs like nifedipine (log P ¼ 2.20) (Jannin et al, 2015) and highly lipophilic drugs like atorvastatin (log P ¼ 6.36) (Belhadj et al, 2013), which were already successfully incorporated into SEDDS (Belhadj et al, 2013;Jannin et al, 2015).…”

Section: Partitioning Coefficient Log P (Capmul 907 P/water)mentioning

confidence: 99%

Development andin vitroevaluation of an oral SEDDS for desmopressin

et al. 2016

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Context: Self-emulsifying drug delivery systems (SEDDS) are among most promising tools for improving oral peptide bioavailability. Objective: In this study, in vitro protective effect of SEDDS containing desmopressin against presystemic inactivation by glutathione and a-chymotrypsin was evaluated. Materials and methods: The partitioning coefficient (log P) of desmopressin was increased via hydrophobic ion pairing using anionic surfactants. Solubility studies were performed to select the appropriate solvents for SEDDS preparation. Subsequently, droplet size and emulsification properties of 22 SEDDS formulations were evaluated. Moreover, the peptide-surfactant complex was dissolved in two chosen SEDDS formulations. Finally, SEDDS containing desmopressin were characterized regarding lipase stability, toxicity, and in vitro protective effect toward glutathione and a-chymotrypsin. Results: Desmopressin log P was increased from initial À6.13 to 0.33 using sodium docusate. The resulting desmopressin docusate complex (DES/AOT) was incorporated in two different SEDDS formulations, containing Capmul 907 P as main solvent. DES/AOT-SEDDS-F4 (containing 0.07% w/w DES/AOT) was composed of 50% Capmul 907P, 40% Cremophor RH40, and 10% Transcutol. The comparatively more hydrophilic formulation DES/AOT-SEDDS-F15 (containing 0.25% w/w DES/AOT) consisted of 20% Capmul 907P, 40% Acconon MC8-2, and 40% Tween 20. Both formulations were stable toward digestion by lipase and protected desmopressin toward a-chymotrypsin degradation. Moreover, DES/AOT-SEDDS-F4 also protected the peptide from thiol/disulfide exchange reactions with glutathione and was not cytotoxic at a concentration of 0.375% (w/w). Conclusion: DES/AOT-SEDDS-F4 protected desmopressin from in vitro glutathione and a-chymotrypsin degradation. DES/AOT-SEDDS-F4 was metabolically stable and nontoxic. Therefore, it could be considered as a potential delivery system for oral desmopressin administration.

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Development of self emulsifying lipid formulations of BCS class II drugs with low to medium lipophilicity

Cited by 44 publications

References 33 publications

Development and in vitro characterization of self-emulsifying drug delivery system (SEDDS) for oral opioid peptide delivery

Development and in vitro characterization of self-emulsifying drug delivery system (SEDDS) for oral opioid peptide delivery

D-Optimal Mixture Design for Optimization of Self Microemulsifying Drug Delivery System of Simvastatin: Characterization and in Vitro Evaluation

Development andin vitroevaluation of an oral SEDDS for desmopressin

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