Design and Evaluation of Self-Emulsifying Drug Delivery System (SEDDS) Of Carvedilol to Improve the Oral Absorption

Salimi, Anayatollah; Makhmalzadeh, Behzad Sharif; Hemati, Ali Asghar; Birgani, Sanaz Akbari

doi:10.17795/jjnpp-16125

Cited by 22 publications

(14 citation statements)

References 13 publications

(20 reference statements)

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“…[56,57] Cinacurcumin ® is an oral polymeric micelle formulation containing curcumin, with the indications including kidney function improvement, repairing of the damaged tissues, decreasing the chemical therapy adverse effects.…”

Section: Polymeric Micelle Preparation Methodsmentioning

confidence: 99%

“…As it is added to a hydrophilic liquid, amphiphilic monomers start to locate on the surface of the liquid and decrease the surface tension. [7] A threshold at which surface tension remains constant while the surfactant concentration is increasing is called critical micelle concentration (CMC). At CMC, surfactant monomers self-assemble and form a micelle.…”

Section: Micelle Formation Mechanismmentioning

confidence: 99%

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Untitled

Esfahani¹

2017

AJP

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Almost half of the orally administered drugs are poorly soluble in water; therefore they have low absorption in the gastrointestinal (GI) tract. In addition, drugs which are administered orally must remain stable during passing the GI tract, despite different physiologic challenges such as pH changes, and dilution effect. Hence, new methods are needed to increase the solubility of these drugs while making them more stable in the physiologic environment. Polymeric micelles are one of the new nanocarriers which are able to increase the solubility of these drugs while protecting them from pH changes, dilution effect, and biological barriers such as filtration in the spleen or scavenging by the phagocytic system. This article provides some important and basic information including polymeric micelles characteristics, structure, and preparation.

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Section: Polymeric Micelle Preparation Methodsmentioning

confidence: 99%

Section: Micelle Formation Mechanismmentioning

confidence: 99%

Untitled

Esfahani¹

2017

AJP

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“…A significant number of drugs suffer from the problem of low oral absorption, [10][11][12] and thus poor oral efficiency. Different strategies have been investigated to enhance the bioavailability of poorly absorbed drugs in order to increase their clinical efficacy when administered orally.…”

Section: Introductionmentioning

confidence: 99%

“…[12; 14-17] SEEDS are drug delivery systems based on a mixture of oils, surfactants, co-solvents and drugs, which results in entropy-favoured spontaneous emulsification on in situ exposure, and can sometimes emulsify under conditions of gentle agitation, similar to those that would be encountered in the gastrointestinal tract. [13; 18-21] The ability of SEDDS to improve oral bioavailability has been shown for curcumin, [22] mitotane, [23] mefenamic acid, [24] Valsartan, [25] to improve the oral absorption of carvediol, [11] inhibition of human efflux transporter ABCC2, [26] and transformation of the crystalline form of the drug to the amorphous form in the SEDDS. [16] SEDDS are among the methods used to improve the oral bioavailability of poorly soluble drugs by presenting and maintaining the drug in a dissolved state, in small droplets of oil, and all over its transit through the gastrointestinal tract.…”

Section: Introductionmentioning

confidence: 99%

Design and Development of Self-Emulsifying Drug Delivery Systems Novel Cardioactive N-Acylhydrazone Compound

Zanchetta¹,

Chaud²,

Santana³

2016

IJNN

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In this study, the emphasis is placed on a strategy for enhancing the drug/carrier interaction for improved drug solubility, drug-loading capacity, self-emulsification and stability.Preliminary solubility of L294 was determined in various oils, surfactants and cosurfactants. A ternary phase diagram was constructed to identify the self-emulsifying region for the selected systems, using series concentrations of Labrafac PG, Labrasol and Transcutol HP. Self-emulsifying properties, particle size, polydispersibility, and zeta potential were studied after dilution of formulations in water.The results demonstrated the development of a self-emulsifying formulation of L294 in liquid form, which upon contact with aqueous media spontaneously forms a clear nanoemulsion having a small droplet size (around 100 nm). The zeta potential of the selected SEDDS formulation was between −11.09 and −20.50 with a viscosity around 40-60 cP. The optimum formulation consisted of a mixture of Labrafac PG, Labrasol and Transcutol HP.The L294 showed extremely low water solubility (0,006 mg.mL -1 ), and when formulated in SEDDS, its solubility increased over than 33,000 fold.This study demonstrate that SEDDS can be considered as a very good candidate to optimize the peroral administration of L294.

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“…It has been loaded in self-emulsifying (SEDDS) [17][18][19], self-microemulsifying (SMEDDS) [17,20] and self-nanoemulsifying drug delivery systems (SNEDDS) [6,21,22], as well as in solid lipid nanoparticles (SLN) [3,7,13,23,24]. For instance, Singh et al [6] observed an improvement in CARV pharmacokinetic parameters C max (134.2 %) and AUC (85.2 %) by loading it in SNEDDS.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of carvedilol compatibility with lipid excipients for the development of lipid-based drug delivery systems

Silva

Teixeira

Serpa

et al. 2015

J Therm Anal Calorim

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Carvedilol (CARV) is a widely used non-selective b-blocker, which has shown low bioavailability after oral administration (20 %) due to its low water solubility and intense first-pass metabolism. Lipid-based drug delivery systems have been proposed to improve CARV oral bioavailability. An evaluation of drug-excipient compatibility is needed to clarify potential physical and chemical interactions between them and therefore guarantee a correct selection of excipients. However, to date there are no reports on the systematic evaluation of CARV-lipid excipient compatibility. Thus, the aim of this study was to evaluate the compatibility of CARV with the lipid excipients commonly used for the development of lipid-based formulations. Thermal analysis techniques (DTA and TG/DTG), Fourier transform infrared spectroscopy and isothermal stress testing (IST) were used for this purpose. The results of this study showed that 4 of the 10 lipid excipients studied were incompatible with CARV. The strongest thermal and spectroscopic modifications were observed in CARV mixtures with oleic acid, lauric acid, lauroyl polyoxylglycerides (Gelucire Ò 44/14) and glyceryl caprylate/caprate (Capmul Ò MCM). In addition, these mixtures resulted in significant decreases in drug content after aging. On the other hand, palmitic acid, stearic acid, glyceryl behenate (Compritol ATO Ò 188), tribeheninPEG (Emulium Ò 22), polyglyceryl-6-isostearate (Plurol Isostearique Ò ) and diethylene glycol monoethyl ether (Transcutol HP Ò ) were considered good candidates for developing self-emulsifying drug delivery systems and for preparing lipid microparticle or nanoparticle containing CARV. These findings denote the relevance of combining thermal and spectroscopic techniques with thermal stress testing for the accurate determination of druglipid excipient compatibility.

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Design and Evaluation of Self-Emulsifying Drug Delivery System (SEDDS) Of Carvedilol to Improve the Oral Absorption

Cited by 22 publications

References 13 publications

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Design and Development of Self-Emulsifying Drug Delivery Systems Novel Cardioactive N-Acylhydrazone Compound

Evaluation of carvedilol compatibility with lipid excipients for the development of lipid-based drug delivery systems

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