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Journal ArticleDOI

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) of darunavir for improved dissolution and oral bioavailability: In vitro and in vivo evaluation.

TL;DR: Investigation of solid self-nanoemulsifying drug delivery system (S-SNEDDS) composed of Capmul MCM C8, Tween 80 and Transcutol P found presence of drug in non-crystalline amorphous state without any significant interaction of drug with the components of S- SNEDDS.
About: This article is published in European Journal of Pharmaceutical Sciences.The article was published on 2015-07-10. It has received 111 citations till now. The article focuses on the topics: Darunavir & Drug delivery.
Citations
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Journal ArticleDOI
13 Nov 2019
TL;DR: In this article, a review of food grade nanoemulsions using high-energy methods and low-energy approaches and their characterization for physical properties, stability and microstructure is presented.
Abstract: Nanoemulsions have small droplet size and are kinetically stable colloidal systems. They have enhanced functional properties in comparison to conventional emulsions. The composition and structure of the nanoemulsions can be controlled for the encapsulation and effective delivery of bioactive lipophilic compounds. Nanoemulsions have potential application in the food industry for the delivery of nutraceuticals, coloring and flavoring agents, and antimicrobials. The nanoemulsion formulations of active ingredients can be used for developing biodegradable coating and packaging films to enhance the quality, functional properties, nutritional value and shelf life of foods. This review focuses on preparation of food grade nanoemulsions using high-energy methods and low-energy approaches and their characterization for physical properties, stability and microstructure. The application of nanoemulsion formulations for sustainable food processing and improving the delivery of functional compounds, such as colorants, flavouring agents, nutraceuticals and preservatives or antimicrobial agents in foods has been discussed.

231 citations

Journal ArticleDOI
TL;DR: This review includes the conflict between the influences of droplet size, variation in correlation between in vitro lipolysis or ex-vivo intestinal permeation and pharmacokinetic parameters, variations in in vivo results of solid and liquid SEDDS, and potential challenges or limitation of pharmacokinetics studies on human volunteers with orally administered SED DS.
Abstract: Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of lipid, surfactant and co-surfactant, which forms a fine emulsion when comes in contact of an aqueous medium with mild agitation. SEDDS is considered as a potential platform for oral delivery of hydrophobic drug in order to overcome their poor and irregular bioavailability challenges. In spite of fewer advantages like improved solubility of drug, bypassing lymphatic transport etc., SEDDS faces different controversial issues such as the use of appropriate terminology (self-microemulsifying drug delivery system; SMEDDS or self-nanoemulsifying drug delivery system; SNEDDS), presence of high amount of surfactant, correlation of in vitro model to in vivo studies, lack of human volunteer study and effect of conversion of SEDDS to final administrable dosage form on pharmacokinetic behavior of the drug. In this review, potential issues or questions on SEDDS are identified and summarized from the pharmacokinetic point of view. Primarily this review includes the conflict between the influences of droplet size, variation in correlation between in vitro lipolysis or ex-vivo intestinal permeation and pharmacokinetic parameters, variation in in vivo results of solid and liquid SEDDS, and potential challenges or limitation of pharmacokinetic studies on human volunteers with orally administered SEDDS. In the past decades, hundreds of in vivo studies on SEDDS have been published. In the present study, only the relevant article on in vivo pharmacokinetic studies with orally administered SEDDS published in past 5-6 years are analyzed for an up to date compilation.

109 citations


Cites methods from "Solid self-nanoemulsifying drug del..."

  • ...But, the reason behind higher extent of absorption and bioavailability from S-SNEDDS compared to L-SNEDDS is not clear from the authors view other than general hypothesized mechanisms of improved pharmacokinetics from SNEDDS that have been already explained in this review earlier....

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  • ...The in vivo studies showed 2–2.5 times higher Cmax and 2–3 times higher AUC0– values obtained after oral administration of L-SNEDDS and S-SNEDDS to Wistar albino rats compared to normal drug suspension....

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  • ...Darunavir, a poorly soluble drug was formulated as liquid SNEDDS (L-SNEDDS) containing Capmul MCM (a medium chain triglyceride) followed by conversion to a solid powder (S-SNEDDS) (Inugala et al., 2015)....

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  • ...…Transcutol P 101 ± 4 SNEDDS (Kang et al., 2012) Diclofenac Sodium NR 137 SNEDDS (Kumar et al., 2015) Darunavir Capmul MCM C8, tween 80, transcutol P 144 ± 2.3 SNEDDS (Inugala et al., 2015) MCT: Medium chain triglyceride; TPGS: D-alpha-tocopheryl polyethylene glycol 1000 succinate; NR: Not reported....

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  • ...The initial rate of Darunavir absorption was higher in the case of L-SNEDDS, but the AUC0– value was higher in the case of S-SNEDDS (32.28 ± 2.5 mg.h/ml) than L-SNEDDS (22.9 ± 2.1 mg.h/ml)....

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Journal ArticleDOI
TL;DR: Considerable progress has been made in nanoemulsion design, fabrication, and testing, and this knowledge facilitates the design of new formulations to improve the bioavailability of pharmaceuticals, supplements, and nutraceuticals.
Abstract: Introduction: The efficacy of many hydrophobic bioactives (pharmaceuticals, supplements, and nutraceuticals) is limited due to their relatively low or highly variable bioavailability. Nanoemulsions consisting of small lipid droplets (r < 100 nm) dispersed in water can be designed to improve bioavailability.Areas covered: The major factors limiting the oral bioavailability of hydrophobic bioactive agents are highlighted: bioaccessibility, absorption and transformation. Two nanoemulsion-based approaches to control these processes and improve bioavailability are discussed: nanoemulsion delivery systems (NDS) and nanoemulsion excipient systems (NES). In NDS, hydrophobic bioactives are dissolved within the lipid phase of oil-in-water nanoemulsions. In NES, the bioactives are present within a conventional drug, supplement, or food, which is consumed with an oil-in-water nanoemulsion. Examples of NDS and NES utilization to improve bioactive bioavailability are given.Expert opinion: Considerable progress ...

84 citations

Journal ArticleDOI
TL;DR: The present review highlights various innovative research strategies adopted to overcome the limitations of the present treatment regimens and to enhance the efficacy of the oral ARV therapy in HIV.

81 citations

Journal ArticleDOI
TL;DR: This work provides an insight of the novel approaches in drug delivery covering the critical comparison between traditional and novel “advanced-designed” systems.

72 citations

References
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1,310 citations


"Solid self-nanoemulsifying drug del..." refers methods in this paper

  • ...%) was calculated using tapped density (Pt) and poured bulk density (Pb) of S-SNEDDS formulation (Carr, 1965)....

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Journal ArticleDOI
TL;DR: A further parameter suitable for the evaluation of in vitro dissolution has been suggested by Khan & Rhodes (1972), who introduced the idea of Dissolution Efficiency, defined as the area under the dissolution curve up to a certain time expressed as a percentage of the area of the rectangle described by 100% dissolutionin the sametime.
Abstract: The recent interest in drug availability has resulted in a proliferation of in vitro dissolution testing, now standard for many dosage forms. The usual method of evaluation is the comparison of the time taken for given proportions of the active drug to be released into solution and figures such as the t20, t50 and t90 % times are often quoted. Alternatively the fraction of drug in solution after a given time is used for comparison, i.e. 60% release in 30 min. A further parameter suitable for the evaluation of in vitro dissolution has been suggested by Khan & Rhodes (1972), who introduced the idea of Dissolution Efficiency. This is defined as the area under the dissolution curve up to a certain time, t, expressed as a percentage of the area of the rectangle described by 100% dissolutionin the sametime. The simplest case, shown in Fig. 1 where, dissolution of a tableted drug, is

928 citations


"Solid self-nanoemulsifying drug del..." refers methods in this paper

  • ...From the dissolution profiles, various dissolution parameters like dissolution efficiency (DE), mean dissolution time (MDT) and mean dissolution rate (MDR) were calculated out (Khan, 1975; Eedara et al., 2013)....

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Journal ArticleDOI
TL;DR: The mechanistic rationale which underpins the use of lipid-based delivery systems to enhance drug solubilisation is described and the available literature describing increases in oral bioavailability after the administration of lipid solution, suspension and self-emulsifying formulations is reviewed.

640 citations


"Solid self-nanoemulsifying drug del..." refers background in this paper

  • ...SNEDDS are preconcentrates composed of isotropic mixtures of oils, surfactants, co-surfactants which spontaneously form a fine oil in water (o/w) emulsion in situ upon contact with aqueous medium with a globule size in the range of 20–200 nm (Porter et al., 2008)....

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Journal ArticleDOI
TL;DR: The studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as simvastatin by the oral route, and its potential use for in vitro dissolution and bioavailability assessment.

518 citations


"Solid self-nanoemulsifying drug del..." refers methods in this paper

  • ...In vitro drug release studies In vitro drug release behaviour of drug from pure darunavir and L-SNEDDS dispersion was determined using modified dialysis method (Kang et al., 2004)....

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Journal ArticleDOI
TL;DR: The ability of polyglycolyzed glycerides (PGG) with varying fatty acid and polyethylene glycol (PEG) chain lengths to produce the self-emulsification of oil in water has been investigated in this paper.

514 citations


"Solid self-nanoemulsifying drug del..." refers background in this paper

  • ...The fatty acid composition is 70% oleic acid with several other fatty acids such as palmitic acid (Shah et al., 1994)....

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  • ...The variation in fatty acid carbon chain lengths of oil, surfactant and their degree of un-saturation plays a significant role in rapid self-emulsification with small globule size and stability of formed emulsion (Shah et al., 1994)....

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