Solid self-microemulsifying dispersible tablets of celastrol: Formulation development, charaterization and bioavailability evaluation

Qi, Xiaole; Qin, Jiayi; Ma, Ning; Chou, Xiaohua; Wu, Zhenghong

doi:10.1016/j.ijpharm.2014.06.019

Cited by 122 publications

(70 citation statements)

References 23 publications

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“…The ODT-SR of domperidone was administered orally at a single dose of 1.64 mg/ 200 g body weight after dispersing it in normal saline 36 . Necessary corrections were made and the animal dosage was determined from the human dose using the conversion factor 37 .…”

Section: Ii) Drug Administration and Collection Of Plasmamentioning

confidence: 99%

Formulation and development of orodispersible sustained release tablet of domperidone

Patil

Tiwari

Repka

et al. 2015

Drug Development and Industrial Pharmacy

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Abstract:Commercially available domperidone orodispersible tablets (ODT) are intended for immediate release of the drug but none of them have been formulated for sustained action. The aim of the present research work was to develop and evaluate orodispersible sustained release tablet (ODT-SR) of domperidone, which has the convenience of ODT and benefits of controlled release product combined in one. The technology comprised of developing sustained release microspheres (MS) of domperidone, followed by direct compression of MS along with suitable excipients to yield ODT-SR which rapidly disperses within 30 seconds and yet the dispersed MS maintain their integrity to have a sustained drug release. The particle size of the MS was optimized to be less than 200 μm to avoid the grittiness in the mouth. The DSC thermograms of MS showed the absence of drug-polymer interaction within the microparticles, while SEM confirmed their spherical shape and porous nature. Angle of repose, compressibility and Hausner's ratio of the blend for compression showed good flowability and high percent compressibility. The optimised ODT-SR showed disintegration time of 21 seconds and matrix controlled drug release for 9 h. Invivo pharmacokinetic studies in Wistar rats showed that the ODT-SR had a prolonged MRT of 11.16 h as compared 3.86 h of conventional tablet. The developed technology is easily scalable and holds potential for commercial exploitation.

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Section: Ii) Drug Administration and Collection Of Plasmamentioning

confidence: 99%

Formulation and development of orodispersible sustained release tablet of domperidone

Patil

Tiwari

Repka

et al. 2015

Drug Development and Industrial Pharmacy

View full text Add to dashboard Cite

show abstract

“…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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“…10 Despite its potential in cancer treatment, further therapeutic application of CL is affected by the poor water solubility, low oral bioavailability, and multiple side effects. 11,12 Furthermore, harmful solvents such as dimethyl sulfoxide (DMSO) need to be used to solubilize the hydrophobic CL, and this limits its clinical use. 13,14 In spite of this, to overcome these physicochemical and pharmacokinetic deficiencies, and to reduce the amount of the effective dose, the nanoencapsulation of CL can represent a useful strategy.…”

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confidence: 99%

Nanoencapsulation of natural triterpenoid celastrol for prostate cancer treatment

Sanna¹,

Chamcheu²,

Pala³

et al. 2015

IJN

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Celastrol (CL), a triterpenoid extracted from the Chinese herb Tripterygium wilfordii , has recently attracted interest for its potential antitumor effects. However, unfavorable physicochemical and pharmacokinetics properties such as low solubility, poor bioavailability, and systemic toxicity, are limiting its therapeutic application. In this context, the development of innovative nanocarriers can be useful to overcome these issues, and nanoencapsulation would represent a powerful strategy. In this study, we developed novel CL-loaded poly( ε -caprolactone) nanoparticles (NPs), and investigated their antiproliferative efficacy on prostate cancer cells. CL-NPs were prepared using a nanoprecipitation method and fully characterized by physicochemical techniques. The antiproliferative effects on LNCaP, DU-145, and PC3 cell lines of CL-NPs, compared to those of free CL at different concentrations (0.5, 1.0, and 2.0 µM), were investigated. Moreover, fluorescence microscopy was utilized to examine the cellular uptake of the nanosystems. Furthermore, to elucidate impact of nanoencapsulation on the mechanism of action, Western analyses were conducted to explore apoptosis, migration, proliferation, and angiogenesis alteration of prostate cancer cells. The results confirmed that CL-NPs inhibit proliferation dose dependently in all prostate cancer cells, with inhibitory concentration 50 less than 2 µM. In particular, the NPs significantly increased cytotoxicity at lower/medium dose (0.5 and 1.0 µM) on DU145 and PC3 cell lines with respect to free CL, with modulation of apoptotic and cell cycle machinery proteins. To date, this represents the first report on the development of biocompatible polymeric NPs encapsulating CL. Our findings offer new perspectives for the exploitation of developed CL-NPs as suitable prototypes for prostate cancer treatment.

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Solid self-microemulsifying dispersible tablets of celastrol: Formulation development, charaterization and bioavailability evaluation

Cited by 122 publications

References 23 publications

Formulation and development of orodispersible sustained release tablet of domperidone

Formulation and development of orodispersible sustained release tablet of domperidone

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

Nanoencapsulation of natural triterpenoid celastrol for prostate cancer treatment

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