Rheological behavior of drug suspensions in Gelucire® mixtures and proxyphylline release from matrix hard gelatin capsules

Ratsimbazafy, V.; Bourret, E.; Duclos, R.; Brossard, C.

doi:10.1016/s0939-6411(99)00042-9

Cited by 18 publications

(4 citation statements)

References 17 publications

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“…[21][22][23] Fatty acid esters of PEGs, commonly known as macrogolglycerides are produced industrially and used in a variety of lipid-based formulations in cosmetic and pharmaceutical applications. Currently, these lipidic excipients are used as bioavailability enhancers in, for example, proxyphylline release from matrix hard gelatin capsules, 24 oral formulation of nicotine, 25 and dermal application of cyclosporin A. 26 The present work reports the synthesis, self-assembly, and interaction study of new amphiphiles targeting lectins prepared by click-chemistry grafting of propargylated carbohydrates onto azido-PEG900-stearate.…”

Section: Introductionmentioning

confidence: 99%

Self-assembled carbohydrate-based micelles for lectin targeting

et al. 2011

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Biocompatible low-polydispersity micelles designed for lectin targeting have been prepared by spontaneous self-assembly in water of macromolecular glycosylated amphiphiles. Propargyl-blactoside and N-acetyl-b-D-glucosaminide were conjugated by copper-catalyzed Huisgen cycloaddition to azide-terminated PEG 900 stearate. Upon dissolution in water, the resulting amphiphiles immediately self-assemble into highly regular micelles having a mean diameter of 10 nm. Dynamic Light Scattering (DLS), Transmission Electron Microscopy (TEM) and Small-Angle X-ray Scattering (SAXS) were used to investigate the structure of the self-assembled saccharidic amphiphiles micelles. The presence of the carbohydrate epitopes on the surface of the micelles and their bioavailability for lectin targeting were also demonstrated by light scattering measurements. Specific interaction of the GlcNac and Lac residues with Wheat Germ Agglutinin (WGA) and Peanut Agglutinin (PNA) respectively, unveils potential applications of such carbohydrate-derived surfactants as simple and site-specific vectorization systems for drug delivery.

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Section: Introductionmentioning

confidence: 99%

Self-assembled carbohydrate-based micelles for lectin targeting

et al. 2011

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“…More recently glyceride based materials, particularly gelucires, have been used as extended release matrices for encapsulation [15][16][17]. Gelucires are a group of essentially inert excipients derived from natural hydrogenated food grade fats and oils.…”

Section: Introductionmentioning

confidence: 99%

Design and In Vitro Evaluation of a Novel Vaginal Drug Delivery System Based on Gelucire

Manordas

2009

CDD

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Carbamazepine indicated for the control of epilepsy, undergoes extensive hepatic first-pass metabolism after oral administration. A vaginal dosage form of carbamazepine is not commercially available. Conventional suppository having poor retention in the vaginal tract, as they are removed in a short time by the tract's self-cleansing action, having poor patient compliance. To overcome such problems, delivery system with mucoadhesive polymers polyox WSR N-60K and Ucarflock 302 that prolong drug permanence on the vaginal mucosa were developed. In the present study the suitability of gelucires to formulate vaginal pesseries was investigated. The possible modification of carbamazepine release kinetics by using gelucires blends and hydrophilic additives in the pesseries was evaluated. It was observed that among gelucire grades melting point higher than 37 ˚C, the release rate proved to be highly dependant on HLB value and matrix composition. In most of the formulations carbamazepine release occurred by disintegration and erosion of the matrices which is depending upon the vehicle employed. The aging study revealed that the formulations containing G50/13 and G50/13-G44/14 blends undergo some changes during one year of shelf aging. From the results obtained it can be concluded that different gelucire grades and their blends along with hydrophilic polymer could be successesively used to formulate prolong release carbamazepine pesseries.

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“…These materials are classified by two numbers, the first referring to the approximate melting point of the base and the second to the hydrophile-lipophile balance (HLB) number that reflects the proportion of watersoluble to lipid-soluble moieties in each material. Gelucires have been widely studied as controlled-release matrices, particularly with respect to two such materials, G 50/13 and G 44/14 (Sutananta et al 1995;Ratsimbazafy et al 1999;Khan & Craig 2003). Moreover, Compritol 888 ATO (atomized glyceryl behenate) consists of about 28-32% tribehenate, 52-54% dibehenate and 12-18% monobehenate, and Precirol ATO 5 is synthesized by esterification of glycerol by palmitostearic acid.…”

Section: Introductionmentioning

confidence: 99%

Controlled release tamsulosin hydrochloride from alginate beads with waxy materials

Kim

Park

Jun

et al. 2005

Journal of Pharmacy and Pharmacology

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The objective of this study was to develop oral controlled release delivery systems for tamsulosin hydrochloride (TSH) using alginate beads with various waxy materials, such as Compritol 888 ATO, Precirol ATO 5 and Gelucires. The beads were prepared from sodium alginate-waxy material-TSH slurry dropped onto calcium chloride to form spherical beads. The effects of the addition of various waxy materials to alginate beads on the drug encapsulation efficiency, bead size and morphology were investigated. The drug encapsulation efficiency significantly increased with the addition of waxy materials. The TSH-loaded alginate beads with and without waxy materials were almost spherical particles with an average diameter of 1.44 and 1.22 mm, respectively. In dissolution study, the TSH-loaded alginate beads with waxy materials exhibited controlled release behaviour over a 6-h period, while beads without waxy materials showed release of 100% TSH within 2 h. These results may be attributed to the formation of a more rigid alginate matrix structure due to incorporated waxy materials. From the Dunnett's t-test and the f2 factor, the release of TSH from alginate beads, a similar dissolution pattern to that of the marketed product (Harunal capsules) could be achieved by adding Gelucire 50/13 into TSH-loaded alginate beads. From these results, oral controlled release of TSH could be achieved with loading in alginate beads with waxy materials, such as Compritol 888 ATO, Precirol ATO 5 and Gelucires.

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Rheological behavior of drug suspensions in Gelucire® mixtures and proxyphylline release from matrix hard gelatin capsules

Cited by 18 publications

References 17 publications

Self-assembled carbohydrate-based micelles for lectin targeting

Self-assembled carbohydrate-based micelles for lectin targeting

Design and In Vitro Evaluation of a Novel Vaginal Drug Delivery System Based on Gelucire

Controlled release tamsulosin hydrochloride from alginate beads with waxy materials

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