Effect of combined use of nonionic surfactant on formation of oil-in-water microemulsions

Li, Ping; Ghosh, Anasuya A.; Wagner, Robert F.; Krill, Steve; Joshi, Yatindra M.; Serajuddin, Abu T.M.

doi:10.1016/j.ijpharm.2004.08.024

Cited by 172 publications

(83 citation statements)

References 17 publications

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“…Tween 80 (T80) was found to improve microemulsification of SHS 15 to greatest extent. Literature indicates that mixture of surfactants can yield stable microemulsions (33) and observations in the current investigation are in line with it and the resultant propofol dispersion was absolutely transparent. This could be due to additional stabilization of propofol at interface due to surfactant nature of T80.…”

Section: Screening Of Cosurfactantssupporting

confidence: 86%

Design and Evaluation of Microemulsions for Improved Parenteral Delivery of Propofol

Date

Nagarsenker

2008

AAPS PharmSciTech

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Abstract. The objective of this investigation was to evaluate the potential of the microemulsions to improve the parenteral delivery of propofol. Pseudo-ternary phase diagrams were plotted to identify microemulsification region of propofol. The propofol microemulsions were evaluated for globule size, physical and chemical stability, osmolarity, in vitro hemolysis, pain caused by injection using rat paw-lick test and in vivo anesthetic activity. The microemulsions exhibited globule size less than 25 nm and demonstrated good physical and chemical stability. Propofol microemulsions were slightly hypertonic and resulted in less than 1% hemolysis after 2 h of storage with human blood at 37°C. Rat paw-lick test indicated that propofol microemulsions were significantly less painful as compared to the marketed propofol formulation. The anesthetic activity of the microemulsions was similar to the marketed propofol formulation indicating that they do not compromise the pharmacological action of propofol. The stability studies indicated that the microemulsions were stable for 3 months when stored at 5±3°C. Thus, microemulsions appeared to be an interesting alternative to the current propofol formulations.

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Section: Screening Of Cosurfactantssupporting

confidence: 86%

Design and Evaluation of Microemulsions for Improved Parenteral Delivery of Propofol

Date

Nagarsenker

2008

AAPS PharmSciTech

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“…A water titration method was employed in present investigation to construct phase diagrams (15). Briefly, mixtures of Capryol 90 and Tween-20+Transcutol P were prepared at ratios (in percent w/w) of 9:1, 8:2, 7:3, 6:4, 5:5, 4:6, 3:7, 2:8, and 1:9 into different vials.…”

Section: Phase Diagramsmentioning

confidence: 99%

SMEDDS of Glyburide: Formulation, In Vitro Evaluation, and Stability Studies

Bachhav

Patravale

2009

AAPS PharmSciTech

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Abstract. The objective of the present investigation was to develop and evaluate self-microemulsifying drug delivery system (SMEDDS) for improving the delivery of a BCS class II antidiabetic agent, glyburide (GLY). The solubility of GLY in oils, cosurfactants, and surfactants was evaluated to identify the components of the microemulsion. The ternary diagram was plotted to identify the area of microemulsion existence. The in vitro dissolution profile of GLY SMEDDS was evaluated in comparison to the marketed GLY tablet and pure drug in pH 1.2 and pH 7.4 buffers. The chemical stability of GLY in SMEDDS was determined as per the International Conference on Harmonisation guidelines. The area of microemulsion existence increased with the increase in the cosurfactant (Transcutol P) concentration. The GLY microemulsion exhibited globule size of 133.5 nm and polydispersity index of 0.94. The stability studies indicated that GLY undergoes significant degradation in the developed SMEDDS. This observation was totally unexpected and has been noticed for the first time. Further investigations indicated that the rate of GLY degradation was highest in Transcutol P.

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“…Physical integrity of microemulsion formed and drug solublization capacity after dilution of SMEDDS must be assessed and ensured as it gives an idea about its performance in vivo (22,23). In view of this, FK 506 SMEDDS were diluted with aqueous phases differing in pH.…”

Section: Effect Of Dilution and Ph Of Dilution Media On Fk 506 Smeddsmentioning

confidence: 99%

“…4. Drug Incorporation can have significant influence on mean globule size and needs to be investigated (22,23). Because of hydrophobic nature of FK 506, it may affect globule size of microemulsions or may precipitate upon dilution.…”

Section: Effect Of Fk 506 Loadingmentioning

confidence: 99%

Design and Evaluation of Self-Microemulsifying Drug Delivery System (SMEDDS) of Tacrolimus

2008

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Abstract. The objective of present investigation was to formulate self-microemulsifying drug delivery systems (SMEDDS) of tacrolimus (FK 506), a poorly water soluble immunosuppressant that exhibits low and erratic bioavailability. Solubility of FK 506 in various oils, surfactants cosurfactants and buffers was determined. Phase diagrams were constructed at different ratios of surfactant/cosurfactant (K m ) to determine microemulsion existence region. The effect of oil content, pH of aqueous phase, dilution, and incorporation of drug on mean globule size of resulting microemulsions was studied. The optimized SMEDDS formulation was evaluated for in vitro dissolution profile in comparison to pure drug and marketed formulation (Pangraf capsules). The in vivo immunosuppressant activity of FK 506 SMEDDS was evaluated in comparison to Pangraf capsules. Area of o/w microemulsion region in phase diagram was increased with increase in K m . The SMEDDS yielded microemulsion with globule size less than 25 nm which was not affected by the pH of dilution medium. The SMEDDS was robust to dilution and did not show any phase separation and drug precipitation even after 24 h. Optimized SMEDDS exhibited superior in vitro dissolution profile as compared to pure drug and Pangraf capsules. Furthermore, FK 506 SMEDDS exhibited significantly higher immunosuppressant activity in mice as compared to Pangraf capsules.

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Effect of combined use of nonionic surfactant on formation of oil-in-water microemulsions

Cited by 172 publications

References 17 publications

Design and Evaluation of Microemulsions for Improved Parenteral Delivery of Propofol

Design and Evaluation of Microemulsions for Improved Parenteral Delivery of Propofol

SMEDDS of Glyburide: Formulation, In Vitro Evaluation, and Stability Studies

Design and Evaluation of Self-Microemulsifying Drug Delivery System (SMEDDS) of Tacrolimus

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