Formulation and development of solid self micro-emulsifying drug delivery system (S-SMEDDS) containing chlorthalidone for improvement of dissolution

Dangre, Pankaj V.; Gilhotra, Ritu Mehra; Dhole, Shashikant

doi:10.1007/s40005-016-0243-2

Cited by 34 publications

(9 citation statements)

References 22 publications

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“…In the gastrointestinal (GI) tract, they can form oil-in-water (o/w) microemulsions spontaneously, thus allowing rapid dissolution of drugs and enhancing permeation of the drugs across the intestinal membrane. 7 In addition, a formed o/w microemulsion could be delivered by lymphatic transport to avoid first-pass metabolism in the liver, thus improving BA of the drug. 8 Nevertheless, SMEDDS have several shortcomings for practical drug product development.…”

Section: Introductionmentioning

confidence: 99%

Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

Yeom¹,

Chae²,

Son³

et al. 2017

IJN

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A novel, supersaturable self-microemulsifying drug delivery system (S-SMEDDS) was successfully formulated to enhance the dissolution and oral absorption of valsartan (VST), a poorly water-soluble drug, while reducing the total quantity for administration. Poloxamer 407 is a selectable, supersaturating agent for VST-containing SMEDDS composed of 10% Capmul ® MCM, 45% Tween ® 20, and 45% Transcutol ® P. The amounts of SMEDDS and Poloxamer 407 were chosen as formulation variables for a 3-level factorial design. Further optimization was established by weighting different levels of importance on response variables for dissolution and total quantity, resulting in an optimal S-SMEDDS in large quantity (S-SMEDDS_LQ; 352 mg in total) and S-SMEDDS in reduced quantity (S-SMEDDS_RQ; 144.6 mg in total). Good agreement was observed between predicted and experimental values for response variables. Consequently, compared with VST powder or suspension and SMEDDS, both S-SMEDDS_LQ and S-SMEDDS_RQ showed excellent in vitro dissolution and in vivo oral bioavailability in rats. The magnitude of dissolution and absorption-enhancing capacities using quantity-based comparisons was in the order S-SMEDDS_RQ > S-SMEDDS_LQ > SMEDDS > VST powder or suspension. Thus, we concluded that, in terms of developing an effective SMEDDS preparation with minimal total quantity, S-SMEDDS_RQ is a promising candidate.

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Section: Introductionmentioning

confidence: 99%

Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

Yeom¹,

Chae²,

Son³

et al. 2017

IJN

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“…Despite its attractive therapeutic effects, the low solubility and bioavailability of genistein have limited its potential as a medicine (Dixon and Ferreira, 2002). Diverse pharmaceutical formulations such as self-emulsifying drug delivery systems, mixed micelles, polymeric particulate systems, and liposomes (Takeuchi et al ., 2003; Mathot et al ., 2006; Munish et al ., 2016; Pankaj et al ., 2016) have been investigated as strategies to increase the solubility and bioavailability of poorly soluble drugs such as genistein. In particular, solid lipid particulate systems (SLPS) are very promising because they increase the solubility of poorly soluble drugs, improve drug stability by protecting them from enzymatic or chemical degradation, and release incorporated drugs at a controlled rate, thereby enhancing drug bioavailability (Luo et al ., 2006; Muller et al ., 2006).…”

Section: Introductionmentioning

confidence: 99%

Absorption Study of Genistein Using Solid Lipid Microparticles and Nanoparticles: Control of Oral Bioavailability by Particle Sizes

Kim

Barua

Kim

et al. 2017

Biomolecules & Therapeutics

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In this study, the effect of particle size of genistein-loaded solid lipid particulate systems on drug dissolution behavior and oral bioavailability was investigated. Genistein-loaded solid lipid microparticles and nanoparticles were prepared with glyceryl palmitostearate. Except for the particle size, other properties of genistein-loaded solid lipid microparticles and nanoparticles such as particle composition and drug loading efficiency and amount were similarly controlled to mainly evaluate the effect of different particle sizes of the solid lipid particulate systems on drug dissolution behavior and oral bioavailability. The results showed that genistein-loaded solid lipid microparticles and nanoparticles exhibited a considerably increased drug dissolution rate compared to that of genistein bulk powder and suspension. The microparticles gradually released genistein as a function of time while the nanoparticles exhibited a biphasic drug release pattern, showing an initial burst drug release, followed by a sustained release. The oral bioavailability of genistein loaded in solid lipid microparticles and nanoparticles in rats was also significantly enhanced compared to that in bulk powders and the suspension. However, the bioavailability from the microparticles increased more than that from the nanoparticles mainly because the rapid drug dissolution rate and rapid absorption of genistein because of the large surface area of the genistein-solid lipid nanoparticles cleared the drug to a greater extent than the genistein-solid lipid microparticles did. Therefore, the findings of this study suggest that controlling the particle size of solid-lipid particulate systems at a micro-scale would be a promising strategy to increase the oral bioavailability of genistein.

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“…7 Poorly water-soluble drugs involve many difficulties in the development of pharmaceutical dosage forms for oral delivery systems due to their low bioavailability. 8 During the past few years, there has been a great pace in using solubility enhancement techniques for the improvement of the dissolution rate and subsequently the bioavailability of poorly water soluble drugs. Several techniques like nanomaterialization, 9 salt formation, 10 hydrotropy, 11 liposome formation, 12 liquisolid compaction, 13 solid dispersion, 14 SMEDDS, 15 and many other significant techniques have been reported for improving bioavailability of poorly water soluble drugs of class BCS-II and BCS-IV.…”

Section: Introductionmentioning

confidence: 99%

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

Dangre¹,

Godbole²,

Ingale³

et al. 2016

IJPER

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Background: Eprosartan mesylate (EM) is a poorly aqueous soluble drug belonging to BCS-class II suffers from low bioavailability (13%). The present study involves an effort for improving dissolution and thus the bioavailability of EM using solid dispersion approach. Methods: Solid dispersion (SD) was prepared by melting, solvent evaporation and kneading method using different ratios of drug and polymers (PEG-4000, Eudragit E-100, PVP K-30, Poloxamer-407, and Eudragit L-100). Phase solubility study revealed highest solubility in PVP K-30 at 1:2 ratios. The solid state characterizations of selected solid dispersion formulation (SD-15) were performed by infrared spectroscopy, differential scanning calorimeter, X-ray diffraction study and scanning electron microscopy. In vitro dissolution was carried out in phosphate buffer (pH 7.4) at 50 rpm in 900 ml of volume. The in vivo pharmacokinetic study of selected formulation (SD-15) was carried out in male Wistar rats using non-compartment analysis by linear trapezoidal method after a single oral dose of 10 mg/kg of EM. Results: The solid state characterization revealed no such drug-polymer interactions and rapid transformation of crystalline drug in an amorphous state, which amplifies the aqueous solubility and hence the dissolution rate. The in vitro dissolution study of the dispersions prepared by PVP K-30 (1:2) was found to be 95.5% after 1 hr. In vivo pharmacokinetic study in Wistar rats showed significant improvement in oral bioavailability of EM in SD-15 with the 2.4 fold increments than the pure drug. Conclusion: The solid dispersion prepared using PVP K-30 by kneading method showed improved dissolution and bioavailability. Therefore, solid dispersion formulation can be sorted as a promising approach for improving the dissolution and bioavailability of Eprosartan mesylate.

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Formulation and development of solid self micro-emulsifying drug delivery system (S-SMEDDS) containing chlorthalidone for improvement of dissolution

Cited by 34 publications

References 22 publications

Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

Absorption Study of Genistein Using Solid Lipid Microparticles and Nanoparticles: Control of Oral Bioavailability by Particle Sizes

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

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