Preparation and evaluation of self-microemulsifying drug delivery system of baicalein

Liu, Wenli; Tian, Rui; Hu, Wenjing; Jia, Yuntao; Jiang, Huiming; Zhang, Jingqing; Zhang, Liangke

doi:10.1016/j.fitote.2012.08.021

Cited by 87 publications

(40 citation statements)

References 26 publications

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“…The ratio of surfactant to co-surfactant was taken as 1:1, 2:1. Oil and Smix were mixed properly in different weight ratios (1:9 to 9:1) [24] . Then each mixture titrated with distilled water until they exhibited turbidity.…”

Section: Construction Of Pseudo-ternary Phase Diagramsmentioning

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: Construction Of Pseudo-ternary Phase Diagramsmentioning

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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“…Much more attention is now focused on SMEDDS due to its excellent efficiency in improving the solubility and oral absorption of poorly water-soluble drugs. [10][11][12][13][14] Thus, SMEDDS could be a valuable approach in solving the delivery problems associated with 25-OCH 3 -PPD. The selection of a suitable self-emulsifying formulation requires assessment of the solubility of the compound in various components, the area of the self-emulsifying region as obtained in the pseudoternary phase diagrams, and the droplet size distribution of the subsequent self-emulsification.…”

Section: (S)mentioning

confidence: 99%

Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation

Cai¹,

Shi²,

Zhang³

et al. 2014

IJN

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The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of the poorly water-soluble compound 20(S)-25-methoxydammarane-3β;12β;20-triol (25-OCH 3 -PPD). Optimized SMEDDS formulations for 25-OCH 3 -PPD contained Cremophor® EL (50%) as the surfactant, glycerin (20%) as the cosurfactant, and Labrafil® M1944 (30%) as the oil. The SMEDDS were characterized by morphological observation and mean droplet size. The pharmacokinetics and bioavailability of the 25-OCH 3 -PPD suspension and SMEDDS were evaluated and compared in rats. The plasma concentrations of 25-OCH 3 -PPD and its main metabolite, 25-OH-PPD, were determined by ultra performance liquid chromatography-tandem mass spectrometry. The relative bioavailability of SMEDDS was dramatically enhanced by an average of 9.8-fold compared with the suspension. Improved solubility and lymphatic transport may contribute to this enhanced bioavailability. Our studies highlight the promise of SMEDDS for the delivery of 25-OCH 3 -PPD via the oral route.

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“…1 BCL is also one of the active ingredients of Sho-Saiko-To, a Japanese herbal supplement believed to be able to improve the liver health. It is highly insoluble in acidic medium and soluble in alkali medium but unstable.…”

Section: Introductionmentioning

confidence: 99%

“…Poor solubility in the gastric fluid and instability in the intestinal fluid greatly limit its oral bioavailability and clinical efficacy. To improve the oral absorption of BCL, a number of novel formulation approaches have been explored, including solid dispersion, 2 cyclodextrin inclusion, 2 nanocrystal, 3 selfmicroemulsifying, 1 phospholipid complex, 4 and liposomes. 5 Nevertheless, these approaches still have some shortcomings to be used as oral delivery vehicles due to inadequate drug protection, poor biocompatibility, and larger particle size.…”

Section: Introductionmentioning

confidence: 99%

Biocompatible nanoemulsions based on hemp oil and less surfactants for oral delivery of baicalein with enhanced bioavailability

Yin¹,

Xiang²,

Wang³

et al. 2017

IJN

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Baicalein (BCL) possesses high pharmacological activities but low solubility and stability in the intestinal tract. This study aimed to probe the potential of nanoemulsions (NEs) consisting of hemp oil and less surfactants in ameliorating the oral bioavailability of BCL. BCL-loaded NEs (BCL-NEs) were prepared by high-pressure homogenization technique to reduce the amount of surfactants. BCL-NEs were characterized by particle size, entrapment efficiency (EE), in vitro drug release, and morphology. Bioavailability was studied in Sprague-Dawley rats following oral administration of BCL suspensions, BCL conventional emulsions, and BCL-NEs. The obtained NEs were ~90 nm in particle size with an EE of 99.31%. BCL-NEs significantly enhanced the oral bioavailability of BCL, up to 524.7% and 242.1% relative to the suspensions and conventional emulsions, respectively. BCL-NEs exhibited excellent intestinal permeability and transcellular transport ability. The cytotoxicity of BCL-NEs was documented to be low and acceptable for oral purpose. Our findings suggest that such novel NEs and preparative process provide a promising alternative to current formulation technologies and suitable for oral delivery of drugs with bioavailability issues.

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Preparation and evaluation of self-microemulsifying drug delivery system of baicalein

Cited by 87 publications

References 26 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

Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation

Biocompatible nanoemulsions based on hemp oil and less surfactants for oral delivery of baicalein with enhanced bioavailability

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Preparation and evaluation of self-microemulsifying drug delivery system of baicalein

Cited by 87 publications

References 26 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

Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3&beta;, 12&beta;, 20-triol: preparation and evaluation

Biocompatible nanoemulsions based on hemp oil and less surfactants for oral delivery of baicalein with enhanced bioavailability

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Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation