Parenteral emulsions stabilized with a mixture of phospholipids and PEG-660-12-hydroxy-stearate: evaluation of accelerated and long-term stability

Jumaa, Muhannad; Müller, Bernd W.

doi:10.1016/s0939-6411(02)00057-7

Cited by 55 publications

(19 citation statements)

References 21 publications

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“…Various formulation factors (type and concentration of oils and emulsifiers), preparation conditions (homogenization temperature, pressure and number of cycles) as well as the way of drug incorporation in the inner phase of the nanoemulsion may profoundly affect its physicochemical properties and stability, and consequently, the in vivo pharmacokinetic behavior and efficacy (Benita and Levy, 1993;Nordén et al, 2001;Jumaa and Müller, 2002;Đorđević et al, 2013). Hence, it is highly desirable to have a good understanding and control of these complex parameters.…”

Section: Introductionmentioning

confidence: 99%

Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation

Đorđević

Cekić

Savić

et al. 2015

International Journal of Pharmaceutics

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This paper describes design and evaluation of parenteral lecithin-based nanoemulsions intended for brain delivery of risperidone, a poorly water-soluble psychopharmacological drug. The nanoemulsions were prepared through cold/hot high pressure homogenization and characterized regarding droplet size, polydispersity, surface charge, morphology, drug-vehicle interactions, and physical stability. To estimate the simultaneous influence of nanoemulsion formulation and preparation parameters--co-emulsifier type, aqueous phase type, homogenization temperature--on the critical quality attributes of developed nanoemulsions, a general factorial experimental design was applied. From the established design space and stability data, promising risperidone-loaded nanoemulsions (mean size about 160 nm, size distribution <0.15, zeta potential around -50 mV), containing sodium oleate in the aqueous phase and polysorbate 80, poloxamer 188 or Solutol(®) HS15 as co-emulsifier, were produced by hot homogenization and their ability to improve risperidone delivery to the brain was assessed in rats. Pharmacokinetic study demonstrated erratic brain profiles of risperidone following intraperitoneal administration in selected nanoemulsions, most probably due to their different droplet surface properties (different composition of the stabilizing layer). Namely, polysorbate 80-costabilized nanoemulsion showed increased (1.4-7.4-fold higher) risperidone brain availability compared to other nanoemulsions and drug solution, suggesting this nanoemulsion as a promising carrier worth exploring further for brain targeting.

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Section: Introductionmentioning

confidence: 99%

Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation

Đorđević

Cekić

Savić

et al. 2015

International Journal of Pharmaceutics

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“…It is well known that both formulation parameters and processing conditions, as well as the way of the drug incorporation into the internal oil phase of the nanoemulsion may affect its physicochemical properties and stability [6,[8][9][10][11]. In order to efficiently investigate a simultaneous effect of different variables that are critical for obtaining nanoemulsions with desired/required characteristics, a design of experiments approach could be a useful tool.…”

Section: Introductionmentioning

confidence: 99%

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

Cekić¹,

Đorđević²,

Savić³

et al. 2015

Savr tehnol

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Using the experimental design methodology, we have developed and characterized nanoemulsions for a parenteral delivery using diazepam as a model drug. The formulations containing 20 or 30% (w/w) of medium chain triglycerides or the mixture of medium chain triglycerides and soybean oil as the oil phase, soybean lecithin and polysorbate 80 as emulsifiers, and a phosphate buffer solution as the aqueous phase were prepared by cold high pressure homogenization. The obtained nanoemulsions were evaluated in terms of droplet size, size distribution, surface charge, drug-vehicle interactions and physical stability. To evaluate the effects of the oil phase type, oil content and drug presence, as well as their interactions on critical quality attributes of nanoemulsions, a three-factor two-level full factorial design was applied. After the preparation, all nanoemulsions revealed small spherical droplets in the range 170-210 nm, with the narrow droplet size distribution (< 0.15) and the surface charge about -60 mV. The experimental design results indicated that not only factors alone (oil type, oil content, presence of drug), but their interactions also had a significant effect on the nanoemulsion droplet size, polydispersity index, and zeta potential. During two months of storage at 25 °C, all nanoemulsions formulated with the medium chain triglycerides-soybean oil mixture (4:1, w/w) remained physically stable, without considerable changes in monitored parameters. Physicochemical characteristics and stability of these nanoemulsions demonstrated their suitability for parenteral drug delivery.

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“…In our study the formulation showed sufficient resistance to the destabilization phenomenon over the defined period at low and moderate temperatures. This might be because of either less density difference between the oil and aqueous phase or it may be because of strong interfacial film at the interface [19]. At higher temperatures slight phase separation might be because of lowering of viscosity of oil phase that resulted in the sedimentation of the heavier phase under centrifugal force [20][21][22].…”

Section: Discussionmentioning

confidence: 99%

Formulation and stability of topical water in oil emulsion containing corn silk extract

Mohsin¹,

Akhtar²,

Mahmood³

et al. 2016

Trop. J. Pharm Res

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Parenteral emulsions stabilized with a mixture of phospholipids and PEG-660-12-hydroxy-stearate: evaluation of accelerated and long-term stability

Cited by 55 publications

References 21 publications

Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation

Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

Formulation and stability of topical water in oil emulsion containing corn silk extract

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