Role of excipients in successful development of self-emulsifying/microemulsifying drug delivery system (SEDDS/SMEDDS)

Rahman, Arafatur; Hussain, Arshad; Hussain, Md. Sarfaraj; Mirza, Mohd. Aamir; Iqbal, Zeenat

doi:10.3109/03639045.2012.660949

Cited by 132 publications

(81 citation statements)

References 124 publications

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“…As a result, enhancement of the effect of SEDDS was depend on the forming small size of emulsions droplet which is provided a large interfacial surface area for drug absorption not only the alone role of complementary (Rahman et al, 2013).…”

Section: In Situ Intestinal Absorption Studiesmentioning

confidence: 99%

“…In addition, it indicated that the SEDDS formulation did not change the absorption segment of piperine. Numerous reports indicated that the surfactants could increase drug absorption by reversible injury in biological cell membranes (Neslihan Gursoy & Benita, 2004;Rahman et al, 2013). So Transcutol P and Tween 80 were selected for next study.…”

Section: In Situ Intestinal Absorption Studiesmentioning

confidence: 99%

See 1 more Smart Citation

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Lei

Cui

et al. 2014

Drug Delivery

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(2015) Enhanced oral bioavailability of piperine by selfemulsifying drug delivery systems: invitro,invivo and insitu intestinal permeability studies, Drug Delivery, 22:6, 740-747, DOI: 10.3109/10717544.2014 AbstractThe main purpose of this work was to develop and evaluate a self-emulsifying drug delivery system (SEDDS) of piperine to enhance its solubility and bioavailability. The formulation was optimized by solubility test and ternary phase diagrams. Then physiochemical properties and in vitro release of SEDDS were characterized. In vivo pharmacokinetics study and in situ singlepass intestinal perfusion were performed to investigate the effects of SEDDS on the bioavailability and intestinal absorption of piperine. The optimized formulation was composed of ethyl oleate, Tween 80 and Transcutol P (3:5.5:1.5, w/w), with the level of the piperine reached 2.5% (w/w). The in vitro dissolution rates of piperine SEDDS were significantly higher than the self-prepared capsules. In vivo pharmacokinetic study showed C max1 , C max2 and area under the curve of piperine after oral administration of SEDDS in rats were 3.8-, 7.2-and 5.2-fold higher than the self-prepared capsules, respectively, and the relative bioavailability of SEDDS was 625.74%. The in situ intestinal absorption study revealed that the effective permeability and the effective absorption rate values of piperine for SEDDS were significantly improved comparing to solutions (p50.01). So SEDDS formulation could improve the oral bioavailability and intestinal absorption of piperine effectively.

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Section: In Situ Intestinal Absorption Studiesmentioning

confidence: 99%

Section: In Situ Intestinal Absorption Studiesmentioning

confidence: 99%

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Lei

Cui

et al. 2014

Drug Delivery

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“…The accelerated digestion of lipid not only improves absorption but also reduces food effect. But in any cases, compatibility and stability of drug with oils should be asserted during the formulation stages (Rahman et al 2013).In this study, we formulated MGA nanoemulsion (MGA NE) which can reduce dosage size by three to four folds, and achieved stable and enhanced oral bioavailability of MGA regardless of food-intake. Droplet size of MGA NE was confirmed via dynamic light scattering (DLS) and TEM imaging analysis.…”

Section: Electronic Supplementary Materialsmentioning

confidence: 99%

Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect

Song

Kim

et al. 2015

Arch. Pharm. Res.

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Megestrol acetate (MGA) belongs to the BCS class II drugs with low solubility and high permeability, and its oral absorption in conventional dosage form MGA microcrystal suspension (MGA MS) is very limited and greatly affected by food. In this study, MGA nanoemulsion (MGA NE) was formulated based on solubility, phase-diagram and release studies. Then oral bioavailability of MGA NE and MGA MS was evaluated. A randomized two-way crossover trial was conducted on six male dogs under fed and fasting conditions. Blood concentrations of MGA were analyzed using LC-MS/MS. MGA NE yielded 5.00-fold higher oral bioavailability in fasting conditions and displayed more stable absorption profiles after food intake compared with MGA MS.

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“…Enabling formulation-approaches include the use of co-solvents, complexing agents, (non-ionic) surfactants, self-(micro-or nano-) emulsifying drug delivery systems, liposomes, amorphous solid dispersions and mesoporous carriers. For recent reviews see (Rahman et al, 2013;Singh et al, 2011;Van Hoogevest et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Biopharmaceutical classification of poorly soluble drugs with respect to “enabling formulations”

Buckley

Frank

Fricker

et al. 2013

European Journal of Pharmaceutical Sciences

173

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The large number of drug candidates with poor dissolution characteristics seen in the past decade, has fostered interest in so-called "enabling formulations", i.e., formulations which shall make such drugs bio-available. Development of enabling formulations is currently being guided by the following (simplified) hypothesis: If a poorly soluble drug (BCS class II drug) can be transferred into a solubilized state, one can achieve an absorption profile close to that of a soluble drug (BCS class I drug). Thus, formulation development typically endeavors to achieve the most robust solubility enhancement. Here we critically review both common in vitro approaches and experimental data available in literature pertaining to the solubility and permeability of poorly soluble drugs from enabling formulations, and discuss their interplay. Recent in vitro data indicate, that commonly employed surfactants as well as endogenous surfactants present in the intestine, although enhancing drug solubility, mostly hamper drug permeation. Mechanistic studies demonstrate a direct correlation between passive transcellular diffusion and the concentration of molecularly dissolved drug. The latter may be reduced due to partitioning into micelles or other solubilizing carriers, but enhanced in supersaturating formulations. We conclude thus that biopharmaceutical assessment approaches that rely on the amount of molecularly dissolved drug should guide us towards successful enabling formulations.

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Role of excipients in successful development of self-emulsifying/microemulsifying drug delivery system (SEDDS/SMEDDS)

Cited by 132 publications

References 124 publications

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems:in vitro, in vivoandin situintestinal permeability studies

Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect

Biopharmaceutical classification of poorly soluble drugs with respect to “enabling formulations”

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