Design and Evaluation of Microemulsions for Improved Parenteral Delivery of Propofol

Date, Abhijit A.; Nagarsenker, Mangal S.

doi:10.1208/s12249-007-9023-7

Cited by 56 publications

(25 citation statements)

References 39 publications

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“…1 Among others, block copolymers containing Poly(Ethylene Oxide) (PEO) have been widely studied 2-7 both due to their relatively simple chemical structure and their bio-compatibility that permits to use them as drug carriers. [8][9][10] 3…”

Section: Introductionmentioning

confidence: 99%

Core Freezing and Size Segregation in Surfactant Core–Shell Micelles

et al. 2015

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Nonionic surfactants containing poly(ethylene oxide) are chemically simple and biocompatible and form core-shell micelles at a wide range of conditions. For those reasons, they and their aggregates have been widely investigated. Recently, irregularities that were observed in the low-temperature behavior of surfactants of the kind [CH3(CH2)(n)O(CH2CH2O)(m)H], (abbreviated CnEm) were assigned to a freezing-melting phase transition in the micellar core. In this work we expand the focus from the case of single component systems to binary surfactant systems at temperatures between 1 and 15 °C. By applying small-angle X-ray scattering (SAXS), differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), and density measurements in pure C18E20 and C18E100 solutions and their mixtures, we show that core freezing/melting is also present in mixtures. Additionally, comparing SAXS data obtained from the mixture with those from the single components, it was possible to demonstrate that the phase transition leads to a reversible segregation of the surfactants from mixed micelles to distinct kinds of micelles of the two components.

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Section: Introductionmentioning

confidence: 99%

Core Freezing and Size Segregation in Surfactant Core–Shell Micelles

et al. 2015

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“…Even though the mean droplet diameter of Diprivan ® was about 170 nm, the number of particles larger than 5 µm was 120-200 (Han et al, 2001). Intravenous infusion of lipid particles exceeding 5 µm in diameter might cause a risk of embolism (Driscoll et al, 1995;Koster et al, 1996;Baker and Naguib, 2005;Date and Nagarsenker, 2008a). Because all the particles in the newly developed propofol microemulsion were less than 100 nm, however, the potency of embolism can be evaded.…”

Section: Discussionmentioning

confidence: 99%

“…Either polyethylene glycol 660 hydroxystearate or poloxamers has been mainly used as a novel surfactant for the development of propofol microemulsions. The microemulation formulations based on polyethylene glycol 660 hyd-roxystearate or poloxamers have additionally employed cosolvents or cosurfactants, and have been evaluated with respect to stability, safety, in vivo efficacy and so on (Ryoo et al, 2005;Morey et al, 2006aMorey et al, , 2006bKim et al, 2007;Date and Nagarsenker, 2008a).…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

Cho

Lee

et al. 2010

Arch. Pharm. Res.

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A new triglyceride-free propofol microemulsion for intravenous injection was formulated using nonionic surfactants, poloxamers and polyethylene glycol 660 hydroxystearate. The aim of this investigation was to evaluate the formulation for storage stability, antimicrobial activity, toxicity and preclinical efficacy. The results were compared to the characteristics obtained for the most commonly used formulation of propofol (Diprivan®). The mean particle diameter of the microemulsion was less than 100 nm so that it could be readily sterilized using a 0.22 μm membrane at room temperature. The microemulsion formulation demonstrated enhanced stability compared to the marketed macroemulsion formulation. In a stress storage condition, it was physicochemically stable for at least 40 months. This new formulation showed higher antimicrobial activity, lower risk of hyperlipidemia and better tolerability than Diprivan®. In preclinical studies, the efficacy and pharmacokinetic profile of the microemulsion were similar to those of Diprivan®. Nevertheless, the administration of the microemulsion caused considerably low histamine release compared to the macroemulsion. Based on these results, the newly developed microemulsion of propofol appeared to have several advantages and, thus, could be an alternative to the fat macroemulsions of propofol.

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“…The ease of emulsification was judged by the number of flask inversions required to yield homogeneous emulsion. The emulsions were allowed to stand for 24 hrs and then % transmittance was evaluated by using UV spectrophotometer 11,12 . They were also observed for turbidity or phase separation visually the surfactant chosen must be able to lower the interfacial tension during the formation of nanoemulsion.…”

Section: Screening Of Surfactantsmentioning

confidence: 99%

Untitled

2017

IJPSR

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Self nano-emulsifying system drug delivery system (SNEDDS) is promising for drugs of BCS class II. The objective of present study to develop self nano-emulsifying drug delivery system for Lipophillic drug Telmisartan (antihypertensive drug), labrafil 1944, Kolliphor ELP: Span 80 (1:1) and PEG 400: Ethanol (1:1) was chosen as oil, Surfactant and Co-surfactant as they show higher solubility for Telmisartan. Screening of Surfactant, Co-surfactant done by percent transmittance and were also observed for turbidity or phase separation visually. Pseudo ternary phase diagram were constructed to identify the self emulsifying regions and also to establish the optimum concentration of oil, surfactant and co-surfactant. Box bhenken desine applied for optimization of formulation. Prepared formulation further Characterization done. Percent Drug Content found 99.71, thermodynamic stability studies show homogenous and no phase separation, Emulsifying Study performed transparent appearance after 24 hr, for robustness Dilutability in water and 0.1N HCl give Percentage Transmittance 99.5 and 100, conducting in vitro dissolution test compared with marketed preparation in stimulated gastric (S.G.F) pH 1.2 showed Percent Drug Release 93.98 with in 30 min, compared by pure drug which was 14.26. Particle size found 164.9 nm which is under nano size range, performing Poly Dispersity Index (PDI) 0.228, Zeta Potential found to be -26.0 mV, by using particle size analyzer.TEM study shows uniform spherical nano emulsion droplets. From the present study it is clear that SNEDDS can be formulated to improve the dissolution and oral bioavailability of poorly water soluble drug Telmisartan.

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Design and Evaluation of Microemulsions for Improved Parenteral Delivery of Propofol

Cited by 56 publications

References 39 publications

Core Freezing and Size Segregation in Surfactant Core–Shell Micelles

Core Freezing and Size Segregation in Surfactant Core–Shell Micelles

Formulation and evaluation of an alternative triglyceride-free propofol microemulsion

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