Formation of Microemulsions by Amino Alkyl Alcohols

Schulman, J. H.; Montagne, J. B.

doi:10.1111/j.1749-6632.1961.tb44987.x

Cited by 151 publications

(41 citation statements)

References 6 publications

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“…Surfactant and co-surfactant get preferentially adsorbed at the interface, reducing the interfacial energy as well as providing a mechanical barrier to coalescence. Decrease in the free energy required for emulsion formation consequently improves the thermodynamic stability of the microemulsion for- mulation (34,35). Therefore, the selection of oil and surfactant, and the mixing ratio of oil to S/CoS, play an important role in the microemulsion formation.…”

Section: Construction Of a Pseudo-ternary Phase Diagrammentioning

confidence: 99%

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Meena¹,

Sharma

Kandaswamy

et al. 2012

Acta Pharmaceutica

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Most of the new chemical entities (NCEs) are poorly water-soluble and pose a challenge to developing an optimum solid oral dosage form. Oral route has been the major route of drug delivery for the treatment of various diseases. Delivery of poorly water--soluble molecules by oral route is difficult because approximately 40 % of drug compounds are limited to low aqueous solubility, which leads to restricted oral bioavailability, high intra-and inter-subject variability and lack of dose proportionality (1).To increase the oral bioavailability of poorly water-soluble compounds and eliminate the discussed drawbacks, various other formulation strategies have been adopted, including the use of cyclodextrins, nanoparticles, solid dispersions and permeation en- The aim of the study was to develop and evaluate a self--emulsifying drug delivery system (SEDDS) formulation to improve solubility and dissolution and to enhance systemic exposure of a BCS class II anthelmetic drug, albendazole (ABZ). In the present study, solubility of ABZ was determined in various oils, surfactants and co-surfactants to identify the microemulsion components. Pseudoternary phase diagrams were plotted to identify the microemulsification existence area. SEDDS formulation of ABZ was prepared using oil (Labrafac Lipopfile WL1349) and a surfactant/co-surfactant (Tween 80/PEG 400) mixture and was characterized by appropriate studies, viz., microemulsifying properties, droplet size measurement, in vitro dissolution, etc. Finally, PK of the ABZ SEDDS formulation was performed on rats in parallel with suspension formulation. It was concluded that the SEDDS formulation approach can be used to improve the dissolution and systemic exposure of poorly water-soluble drugs such as ABZ.

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Section: Construction Of a Pseudo-ternary Phase Diagrammentioning

confidence: 99%

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Meena¹,

Sharma

Kandaswamy

et al. 2012

Acta Pharmaceutica

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“…Lipids, however, are highly insoluble in water (their critical micelle concentration is typically in the < 10 −6 M range [1]), which makes the above interpretation for the surface tension largely irrelevant as there is almost no exchange of lipids between the bilayer membrane and the embedding aqueous medium. More commonly, the surface tension is considered as a measure for the elastic response of a membrane with a fixed number of lipids to area variations [9,10]. This view clearly differs from the meaning of the term "surface tension" for fluid/fluid interfaces, where it serves as a measure for the free energy penalty resulting from an exchange of molecules between the "bulk" phases and the "interface" [11].…”

Section: Introductionmentioning

confidence: 99%

Small membranes under negative surface tension

Avital

Farago

2015

The Journal of Chemical Physics

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We use computer simulations and a simple free energy model to study the response of a bilayer membrane to the application of a negative (compressive) mechanical tension. Such a tension destabilizes the long wavelength undulation modes of giant vesicles, but it can be sustained when small membranes and vesicles are considered. Our negative tension simulation results reveal two regimes -(i) a weak negative tension regime characterized by stretching-dominated elasticity, and (ii) a strong negative tension regime featuring bending-dominated elastic behavior. This resembles the findings of the classic Evans and Rawicz micropipette aspiration experiment in giant unilamellar vesicles (GUVs) [Phys, Rev. Lett. 64, 2094(1990]. However, while in GUVs the crossover between the two elasticity regimes occurs at a small positive surface tension, in smaller membranes it takes place at a moderate negative tension. Another interesting observation concerning the response of a small membrane to negative surface tension is related to the relationship between the mechanical and fluctuation tensions, which are equal to each other for non-negative values. When the tension decreases to negative values, the fluctuation tension γ drops somewhat faster than τ in the small negative tension regime, before it saturates (and becomes larger than τ ) for large negative tensions. The bending modulus exhibit an "opposite" trend. It remains almost unchanged in the stretchingdominated elastic regime, and decreases in the bending-dominated regime. Both the amplitudes of the thermal height undulations and the projected area variations diverge at the onset of mechanical instability.

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“…The decrease in the free energy required for the emulsion formation consequently improves the thermodynamic stability of the microemulsion formulation (Groves, 1976;Schulman and Montagne, 1961). Therefore, the selection of oil and surfactant and the ratio of oil to S/Co-S, are important in the formation of microemulsion.…”

Section: Construction Of Pseudo-ternary Phase Diagramsmentioning

confidence: 99%

Preparation and Evaluation of Novel Fenofibrate-loaded Self-Microemulsifying Drug Delivery System (SMEDDS)

2010

Journal of Pharmaceutical Investigation

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− Fenofibrate has been used for many years to lower cholesterol levels and its pharmacokinetic profile is well understood. However, due to its low solubility in water, it has low bioavailability after oral administration. In order to improve the dissolution rate, fenofibrate was formulated into a self-microemulsifying drug delivery systems (SMEDDS). We used pseudo-ternary phase diagrams to evaluate the area of microemulsification, and an in vitro dissolution test was used to investigate the dissolution rate of fenofibrate. The optimized formulation for in vitro dissolution assessment consisted of Lauroglycol FCC (60%), Solutol HS 15 (27%), and Transcutol-P (13%). The mean droplet size of the oil phase in the microemulsion formed from the SMEDDS was about 130 nm. The dissolution rate of fenofibrate from SMEDDS was significantly higher than that of the reference tablet. Our studies suggested that the fenofibrate containing SMEDDS composition can effectively increase the solubility and oral bioavailability of poorly water-soluble drugs.

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Formation of Microemulsions by Amino Alkyl Alcohols

Cited by 151 publications

References 6 publications

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Small membranes under negative surface tension

Preparation and Evaluation of Novel Fenofibrate-loaded Self-Microemulsifying Drug Delivery System (SMEDDS)

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