Controlled Release of Oral Tetrahydrocurcumin from a Novel Self-Emulsifying Floating Drug Delivery System (SEFDDS)

Setthacheewakul, Saipin; Kedjinda, Wichan; Maneenuan, Duangkhae; Wiwattanapatapee, Ruedeekorn

doi:10.1208/s12249-010-9568-8

Cited by 60 publications

(23 citation statements)

References 25 publications

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“…Until now, solid self-emulsifying systems have been already produced by loading liquid self-emulsifying systems on solid carriers using different technologies: extrusion/spheronization (Newton et al, 2001), co-extrusion (Iosi et al, 2011), wet granulation in high shear mixer (Franceschinis et al, 2005) and spray drying (Christensen et al, 2001;Dollo et al, 2003;Yi et al, 2008). The extrusion/spheronization process is commonly used in the pharmaceutical industry to make uniformly sized pellets (Setthacheewakul et al, 2011). Pellet, as a multiple unit dosage form, possess many advantages such as flexibility of manufacture, reducing intrasubject and intersubject variability of plasma profiles and minimizing GI irritation without lowering drug bioavailability (Gandhi et al, 1999;Bolcskei et al, 2013).…”

Section: Single-pass Intestinal Perfusionmentioning

confidence: 99%

Self-emulsifying drug delivery system and the applications in herbal drugs

Zhang

et al. 2013

Drug Delivery

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Herbal drugs have been used for thousands of years in the east and have had a recent resurgence in popularity among consumers in the west. However, most of herbal drug are poorly soluble and have hydrophobic properties and poor distribution, leading to reduced bioavailability and hence decreased treatment efficacy, requiring repeated administration or increased dose. In the past few decades, considerable attention has been focused on the development of self-emulsifying drug delivery system (SEDDS) for herbal drugs. SEDDS is isotropic and thermodynamically stable solutions consisting of oil, surfactant, co-surfactant and drug that can spontaneously form oil-in-water micro/nanoemulsion when mixed with water under gentle stirring. The formulation can be a viable alternative to classical formulations to take advantage of their lipophilic nature and to solve their problems of poor solubility, poor bioavailability, low oral absorption and instability. The mechanism of self-emulsification, solubility studies, construction of phase diagram, optimization and characterization of herbal drugs-loaded SEDDS formulation and in situ absorption evaluation of herbal drugs in rat intestine are presented in our article.

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Section: Single-pass Intestinal Perfusionmentioning

confidence: 99%

Self-emulsifying drug delivery system and the applications in herbal drugs

Zhang

et al. 2013

Drug Delivery

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“…The formulations of liquid THC-SMEDDS (mixtures of Labrasol, Cremophor EL, Capryol 90 and Labrafac PG) were optimized by solubility assay and pseudo-ternary phase diagram analysis according to our previous study (11). Briefly, the solubility of THC in various vehicles, including oils, surfactants and co-surfactants was determined by the shake-flask method.…”

Section: Preparation Of Liquid Thc-smeddsmentioning

confidence: 99%

“…Moreover, the cost of the manufacturing process is high. Recently, several research groups have successfully developed solid SMEDDS by incorporating SMEDDS into pharmaceutical excipients to produce different solid dosage forms, such as microcapsules (9), pellets (10,11) and tablets (12). The advantages of SMEDDS in tablet formulations are their low cost of manufacture, and ease of production on a large scale.…”

Section: Introductionmentioning

confidence: 99%

Development, Characterization and Permeability Assessment Based on Caco-2 Monolayers of Self-Microemulsifying Floating Tablets of Tetrahydrocurcumin

et al. 2013

Self Cite

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Abstract. Novel self-microemulsifying floating tablets were developed to enhance the dissolution and oral absorption of the poorly water-soluble tetrahydrocurcumin (THC). Their physicochemical properties and THC permeability across Caco-2 cell monolayers were assessed. The self-microemulsifying liquid containing THC was adsorbed onto colloidal silicon dioxide, mixed with HPMC, gas-generating agents (sodium bicarbonate and tartaric acid), lactose and silicified-microcrystalline cellulose and transformed into tablets by direct compression. The use of different types/concentrations of HPMC and sodium bicarbonate in tablet formulations had different effects on the floating characteristics and in vitro THC release. The optimum tablet formulation (F2) provided a short floating lag time (∼23 s) together with a prolonged buoyancy (>12 h). About 72% of THC was released in 12 h with an emulsion droplet size in aqueous media of 33.9±1.0 nm while that of a self-microemulsifying liquid was 29.9±0.3 nm. The tablet formulation was stable under intermediate and accelerated storage conditions for up to 6 months. The THC released from the self-microemulsifying liquid and tablet formulations provided an approximately three-to fivefold greater permeability across the Caco-2 cell monolayers than the unformulated THC and indicated an enhanced absorption of THC by the formulations. The self-microemulsifying floating tablet could provide a dosage form with the potential to improve the oral bioavailability of THC and other hydrophobic compounds.

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“…It combines the advantages of liquid SEDDS (improved solubility and bioavailability) with those of solid dosage forms (storage stability and patient compliance). 8,9 SSEDDS are supposed to maintain the self-emulsifying ability and capable of forming fine oil-in-water emulsions under gentle agitation provided by 11,12 In our previous study, solid self-emulsifying matrix combined with mesoporous silica was successfully prepared. When introduced to aqueous media under gentle agitation, the solid matrix exhibited excellent self-emulsifying properties of forming a uniform microemulsion.…”

Section: Introductionmentioning

confidence: 99%

Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement

Quan¹,

Niu²,

Singh³

et al. 2017

IJN

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Solid self-emulsifying drug delivery system (SSEDDS), which incorporates liquid SEDDS into a solid dosage form, has been recently introduced to improve the oral bioavail-ability of poorly water-soluble drugs. However, supersaturated drug generated by SSEDDS is thermodynamically unstable and tends to precipitate rapidly prior to absorption, resulting in compromised bioavailability. The aim of this study was to construct a novel supersaturated SSEDDS (super-SSEDDS) by combining SSEDDS with appropriate precipitation inhibitor. Fenofibrate (FNB), a sparingly soluble drug, was selected as a model drug in this study. An optimized SSEDDS was prepared by solvent evaporation by using mesoporous silica Santa Barbara Amorphous-15 as the inert carrier. Supersaturation assay was conducted to evaluate the precipitation inhibition capacity of different polymers, and the results showed that Soluplus ® could retard the FNB precipitation more effectively and sustain a higher apparent concentration for ~120 min. This effect was also clearly observed in the dissolution profiles of FNB from SSEDDS under supersaturated condition. The study of the mechanism suggested that the inhibition effect might be achieved both thermodynamically and kinetically. The area under the concentration–time curve of the super-SSEDDS was 1.4-fold greater than that of SSEDDS in the absence of Soluplus, based on an in vivo pharmacokinetic study conducted in beagle dogs. This study has demonstrated that the approach of combining SSEDDS with Soluplus as a supersaturation stabilizer constitutes a potential tool to improve the absorption of poorly water-soluble drugs.

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Controlled Release of Oral Tetrahydrocurcumin from a Novel Self-Emulsifying Floating Drug Delivery System (SEFDDS)

Cited by 60 publications

References 25 publications

Self-emulsifying drug delivery system and the applications in herbal drugs

Self-emulsifying drug delivery system and the applications in herbal drugs

Development, Characterization and Permeability Assessment Based on Caco-2 Monolayers of Self-Microemulsifying Floating Tablets of Tetrahydrocurcumin

Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement

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