Enhanced absorption and drug targeting by positively charged submicron emulsions

Yang, Shi Cheng; Benita, Simon

doi:10.1002/1098-2299(200007/08)50:3/4<476::aid-ddr31>3.0.co;2-6

Cited by 64 publications

(24 citation statements)

References 59 publications

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“…The high positive charge may contribute to its high intestinal absorption. 24 The w/o microemulsion could be transformed to a o/w emulsion or a w/o/w multiemulsion after it is diluted.…”

Section: Discussionmentioning

confidence: 99%

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Zhuang²,

Wu³

et al. 2011

IJN

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Background: A microemulsion is an effective formulation for improving the oral bioavailability of poorly soluble drugs. In this paper, a water-in-oil (w/o) microemulsion was investigated as a system for enhancing the oral bioavailability of Biopharmaceutic Classification System (BCS) III drugs. Methods: The microemulsion formulation was optimized using a pseudoternary phase diagram, comprising propylene glycol dicaprylocaprate (PG), Cremophor ® RH40, and water (30/46/24 w/w). Results: The microemulsion increased the oral bioavailability of hydroxysafflor yellow A which was highly water-soluble but very poorly permeable. The relative bioavailability of hydroxysafflor yellow A microemulsion was about 1937% compared with a control solution in bile duct-nonligated rats. However, the microemulsion showed lower enhanced absorption ability in bile duct-ligated rats, and the relative bioavailability was only 181%. In vitro experiments were further employed to study the mechanism of the enhanced effect of the microemulsion. In vitro lipolysis showed that the microemulsion was digested very quickly by pancreatic lipase. About 60% of the microemulsion was digested within 1 hour. Furthermore, the particle size of the microemulsion after digestion was very small (53.3 nm) and the digested microemulsion had high physical stability. An everted gut sac model demonstrated that cumulative transport of the digested microemulsion was significantly higher than that of the diluted microemulsion. Conclusion: These results suggested that digestion of the microemulsion by pancreatic lipase plays an important role in enhancing oral bioavailability of water-soluble drugs.

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“…The high positive charge may contribute to its high intestinal absorption. 24 The w/o microemulsion could be transformed to a o/w emulsion or a w/o/w multiemulsion after it is diluted.…”

Section: Discussionmentioning

confidence: 99%

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Zhuang²,

Wu³

et al. 2011

IJN

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“…The use of lecithin, which is the reference emulsifying agent used in the submicron emulsion (Yang and Benita 2000), was not dispersible in the SCT oil, and the blend of nonionic surfactants was unable to form an emulsion giving an immediate phase disruption at the end of the emulsification process. The strategy followed was then to reduce the amount of triacetin by mixing it with conventional oily phases.…”

Section: Optimization Of the Formulation With Regard To The Oily Phasementioning

confidence: 99%

“…Finally, only a 40% oil phase with a blend of triacetin/MCT (1:3) including 2.4% lecithin and 2% polysorbate 85 was able to form a submicron emulsion with a potential sufficient amount of incorporable drug. The formulation of a 40% oil phase submicron emulsion including nonconventional lipids is of interest with regard to the formulations of submicron emulsion of 10-20% of oil phase currently available, including mainly natural or hemisynthetic lipids, fatty acids, and oils such as medium-or long-chain triglycerides (Yang and Benita 2000).…”

Section: Optimization Of the Formulation With Regard To The Oily Phasementioning

confidence: 99%

Effect of Oil-in-Water Submicron Emulsion Surface Charge on Oral Absorption of a Poorly Water-Soluble Drug in Rats

et al. 2008

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The effect of oil-in-water submicron emulsion (SE) droplet surface charge on absolute bioavailability of a poorly watersoluble drug (griseofulvin, as model drug) after oral administration was studied in conscious rat. Positively, negatively, and neutrally charged SE were designed and characterized (size, polydispersity index, zeta potential, and pH). Three emulsion formulations, whose compositions included 40% oil phase and differed only in the nature of the emulsifying agent, were retained. Only the positively charged SE showed a higher area under the plasma concentrationtime curve (AUC 0→∞ ) in comparison with the tablet and with the other SE.

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“…The enhanced interaction of oil droplets with the mucosal surface, resulting in increased adhesion of the positively charged droplets to rat intestinal mucosa, and thus increased mucosal uptake of the drug, may be explained in part by their electrostatic interaction with negatively charged sites existing in the epithelial surface (Gershanik, Benzeno, and Benita 1998). The cationic submicron emulsion bearing cationic charge has been reported in various literature preferable for ocular delivery (Yang and Benita 2000). However, the efficacy and safety of submicron emulsion using different cationic charge inducers like chitosan, protamine, and stearylamine for oral delivery has not been studied so far.…”

Section: Introductionmentioning

confidence: 99%

Preparation and performance evaluation of saquinavir laden cationic submicron emulsions

et al. 2009

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Enhanced absorption and drug targeting by positively charged submicron emulsions

Cited by 64 publications

References 59 publications

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Effect of Oil-in-Water Submicron Emulsion Surface Charge on Oral Absorption of a Poorly Water-Soluble Drug in Rats

Preparation and performance evaluation of saquinavir laden cationic submicron emulsions

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