Development of a solidified self-microemulsifying drug delivery system (S-SMEDDS) for atorvastatin calcium with improved dissolution and bioavailability

Yeom, Dong Woo; Son, Ho Yong; Kim, Jin Han; Kim, Dae Jung; Lee, Sang Gon; Song, Seh Hyon; Chae, Bo Ram; Choi, Young Wook

doi:10.1016/j.ijpharm.2016.04.059

Cited by 67 publications

(41 citation statements)

References 36 publications

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“…For one capsule 160 mg of Neusilin US2 was mixed with 160 mg of L-SMEDDS and filled in hard gelatin capsule size '0' [21] . S-SMEDDS formulations were evaluated for angle of repose, Carr's compressibility index and Hausner's ratio [31][32][33] .…”

Section: Characterization Of L-smeddsmentioning

confidence: 99%

Development and Optimization of Piroxicam-loaded Solid Self-micro emulsifying Drug Delivery System

Pattewar¹,

Kasture²,

Pande³

et al. 2018

pharmaceutical-sciences

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The aim of present study was to formulate and evaluate self-microemulsifying drug delivery system containing piroxicam and to use the ability of porous magnesium alumina metasilicate as a solid carrier for self-microemulsifying drug delivery system. It was developed to resolve the problems of piroxicam such as low water solubility, low bioavailability and gastrointestinal irritation. Self-microemulsifying drug delivery system containing varying proportions of Capmul MCM, Cremophor EL and Transcutol-P were prepared and optimized using response surface methodology of Design-Expert ® software version 10. Liquid selfmicroemulsifying drug delivery systems were subjected to in vitro evaluation, including self-emulsification efficiency study, droplet size, zeta potential measurement and in vitro drug release studies. Solid selfmicroemulsifying drug delivery system was prepared by adding liquid self-microemulsifying drug delivery system with Neusilin US2 and filled in hard gelatin capsule. The optimized formulation consists of 28.26 % of Capmul MCM, 44.16 % of Cremophor EL and 27.58 % of Transcutol-P. The results showed that the drug release profile of piroxicam from the self-microemulsifying drug delivery formulations was higher than the pure piroxicam powder. The release of piroxicam was rapid and complete. Solid self-microemulsifying drug delivery systems after filled in hard gelatin capsule, predicted to be a promising technique to deliver a liquid formulation in solid dosage form.

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Section: Characterization Of L-smeddsmentioning

confidence: 99%

Development and Optimization of Piroxicam-loaded Solid Self-micro emulsifying Drug Delivery System

Pattewar¹,

Kasture²,

Pande³

et al. 2018

pharmaceutical-sciences

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“…3) In order to increase the probability of success, solubilized formulation technology is expected to improve the bioavailability of highly water-insoluble compound classified into the biopharmaceutical classification (BCS) class II or class IV. Representative solubilized formulation technology implies crystal engineering, 4) prodrug, 5) self-micro emulsifying drug delivery system (SMEDDS), [6][7][8] cyclodextrin inclusion, 9) solid dispersion, 10) liposome 11) and micellar system. 12) Particle size reduction of active pharmaceutical ingredients (API) is also effective as solubilized formulation technology.…”

Section: Introductionmentioning

confidence: 99%

Development of Universal Formulation with Superior Re-dispersion Using Nanocrystal Approach with Simultaneous Identification of API Physicochemical Properties

Fujii

Watano

2019

Chem. Pharm. Bull.

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Universal nanocrystal formulation which can be applied to water-insoluble compounds was proposed and the criteria of its physicochemical properties as an active pharmaceutical ingredients (API) were investigated. Nanocrystal suspension was prepared by a wet-beads milling method. An acceptable Critical Quality Attributes (CQA) of nanocrystal suspension was defined by Z-average less than 500 nm and Polydispersity index (PDI) less than 0.3. Screening studies of dispersing and wetting agents were conducted using three model compounds in different pK a , melting points, etc., to find universal nanocrystal formulation. The effect of four structurally different polymer species (hydroxypropyl cellulose (HPC), hydoroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA)) and their different grades or five different surfactants (docusate sodium (DOSS), sodium lauryl sulfate (SLS), cetyl trimethyl ammonium bromide (CTAB), polysolbate80 (PS80), and polyoxyethylene castor oil (CO-35)) were studied on the redispersion stability. It was found that the combination of 4% (w/v) HPC-SSL and 0.2% (w/v) DOSS was the most robust nanocrystal formulation owing to Z-average less than 200 nm and good re-dispersion stability without aggregates at pH 1.2 and pH 6.8. API physicochemical properties were also identified using ten water-insoluble compounds. Consequently, it was found that solubility (water, pH 1.2 and pH 6.8), molecular weight, hydrogen bonding acceptor and the ratio of log D 7.4 to C Log P were critical factors.

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“…The recommended oral administration of solid dosage forms of simvastatin for primary hypercholesterolemia results in low bioavailability attributed to its low solubility, pre-systemic clearance in the gastrointestinal (GI) mucosa, and extensive firstpass metabolism in the liver (Yeom et al 2016). Hence, it poses a challenge in developing an optimum oral solid dosage form with enhanced bioavailability.…”

Section: Introductionmentioning

confidence: 99%

“…This feature makes SMEDDS a meaningful choice for oral delivery of lipophilic and low bioavailable simvastatin. Recently, numerous SMEDDS products such as Sandimmun Neoral®, Norvir®, and Fortovase® have been widely commercialized (Yeom et al 2016). Further, a systematic and structured optimization study was employed to design the self-emulsifying drug delivery system of Simvastatin by using the Design of Experiments (DoE).…”

Section: Introductionmentioning

confidence: 99%

D-Optimal Mixture Design for Optimization of Self Microemulsifying Drug Delivery System of Simvastatin: Characterization and in Vitro Evaluation

Kg¹,

AT²,

JR³

et al. 2018

Bull. Pharm. Res.

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The objective of present research work was to develop self-micro emulsifying drug delivery system to improve the in vitro dissolution of a Biopharmaceutical Classification System Class II lipid lowering agent, simvastatin. Solubility study was performed to identify the potent oil, surfactant and co-surfactant showing highest solubility of simvastatin. The ternary phase diagrams were constructed for selected components to identify the area of microemulsion formation. D-optimal mixture design was applied for optimization using three formulation variables namely, oleic acid, Tween 80 and Cremophore EL. The liquid self-micro emulsifying drug delivery systems (SMEDDS) were evaluated for droplet size, self-emulsification time, percent transmittance and drug solubility. The optimized batch showed self-emulsification time and solubility. The optimized liquid formulation was solidified using Aerosil 200 to prepare solid SMEDDS. Solid SMEDDS showed good flow property and uniform drug content. Solid state characterization was performed by differential scanning calorimetry, X-ray diffraction study and scanning electron microscopy. The zeta potential and globule size was-3.66mV and 755.3 nm, respectively. The rate and extent of drug dissolution from solid SMEDDS was significantly higher than tablet formulation. The optimized formulation was found to be stable. These results demonstrate the potential of SMEDDS as a means of improving solubility and dissolution.

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Development of a solidified self-microemulsifying drug delivery system (S-SMEDDS) for atorvastatin calcium with improved dissolution and bioavailability

Cited by 67 publications

References 36 publications

Development and Optimization of Piroxicam-loaded Solid Self-micro emulsifying Drug Delivery System

Development and Optimization of Piroxicam-loaded Solid Self-micro emulsifying Drug Delivery System

Development of Universal Formulation with Superior Re-dispersion Using Nanocrystal Approach with Simultaneous Identification of API Physicochemical Properties

D-Optimal Mixture Design for Optimization of Self Microemulsifying Drug Delivery System of Simvastatin: Characterization and in Vitro Evaluation

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