The influence of surfactants on drug release from a hydrophobic matrix

Efentakis, M.; Alhmoud, Hassan A.; Buckton, Graham; Rajan, Z.

doi:10.1016/0378-5173(91)90175-n

Cited by 34 publications

(22 citation statements)

References 4 publications

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“…Also, it is possible that the surfactant lowers the interfacial tension between the polymer matrix and the dissolution medium; hence it will increase the dispersability of the polymer matrix containing the drug and will also increase the release rate. Perhaps the surfactant acts as a wicking agent, causing the fluid to enter the matrix, the surfactant may then dissolve and form channels from which the drug release may be affected [9]. At surfactant concentration above the cmc, the solubility increases linearly with the concentration of surfactant indicating that solubilization is related to micellization [2].…”

Section: Effect Of Solubilizing Agents On the Rate Of Nystatin Releasementioning

confidence: 99%

“…The increase in micelles enhances the solubilization of the drug. It was also speculated that increasing amounts of surfactants in the copolymer system together with the drug, increases the porosity facilitating the enhanced diffusion of drug molecules through the channels present in the matrix (EVA matrix), leading to an increase in the rate of drug release [9].…”

Section: Effect Of Solubilizing Agents On the Rate Of Nystatin Releasementioning

confidence: 99%

“…The addition of surfactants promoted a far higher release of nystatin. There are other reports that have demonstrated an increase in drug release due to the addition of surfactants [7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

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Effects of solubilizing surfactants and loading of antiviral, antimicrobial, and antifungal drugs on their release rates from ethylene vinyl acetate copolymer

Tallury¹,

K.²,

Thaw³

et al. 2007

Dental Materials

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Objectives-This study investigates the effects of surfactants and drug loading on the drug release rate from ethylene vinyl acetate (EVA) copolymer. The release rate of nystatin from EVA was studied with addition of non-ionic surfactants Tween 60 and Cremophor RH 40. In addition, the effect of increasing drug load on the release rates of nystatin, chlorhexidine diacetate and acyclovir is also presented.Method-Polymer casting solutions were prepared by stirring EVA copolymer and nystatin (2.5 wt %) in dichloromethane. Nystatin and surfactants were added in ratios of (1:1), (1:2) and (1:3). Drug loading was studied with 2.5, 5.0, 7.5, and 10.0% wt. proportions of nystatin, chlorhexidine diacetate and acyclovir incorporated into a separate polymer. Three drug loaded polymer square films (3cm × 3cm × 0.08 cm) were cut from dry films to follow the kinetics of drug release at 37°C. 10 ml of either distilled water or PBS was used as the extracting medium that was replaced daily. PBS was used for nystatin release with addition of surfactants and water was used for the study on drug loading and surfactant release. The rate of drug release was measured by UVspectrophotometer. The amount of surfactant released was determined by HPLC.Results-The release of nystatin was low in PBS and its release rate increased with the addition of surfactants. Also, increasing surfactant concentrations resulted in increased drug release rates. The release rates of chlorhexidine diacetate (p<0.0001), acyclovir (p<0.0003) and nystatin (p<0.0017) linearly increased with increasing drug loads. The amount of surfactants released was above the CMC.Significance-This study demonstrates that the three therapeutic agents show a sustained rate of drug release from EVA copolymer over extended periods of time. Nystatin release in PBS is low owing to its poor solubility. Its release rate is enhanced by addition of surfactants and increasing the drug load as well.

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Section: Effect Of Solubilizing Agents On the Rate Of Nystatin Releasementioning

confidence: 99%

Section: Effect Of Solubilizing Agents On the Rate Of Nystatin Releasementioning

confidence: 99%

See 1 more Smart Citation

Effects of solubilizing surfactants and loading of antiviral, antimicrobial, and antifungal drugs on their release rates from ethylene vinyl acetate copolymer

Tallury¹,

K.²,

Thaw³

et al. 2007

Dental Materials

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“…25,27,28 Wetting can also be an influential factor in the release of drugs from inert matrices. [29][30][31] Luner et al 32 demonstrated that the wettability of a hydrophobic drug varied greatly with different surfactants at the same surface tension. It is likely that the wettability of pharmaceutical materials may be different for bile salts compared to other surfactants.…”

Section: Introductionmentioning

confidence: 98%

Wetting Properties of Bile Salt Solutions and Dissolution Media

Luner

2000

Journal of Pharmaceutical Sciences

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“…Stability studies of the prepared formulations were performed at ambient humidity conditions, at room temperature, at 250C ± 20C & 60% RH, 40oC ± 20C & 75% RH and 600C for a period up to 30 days. The samples were withdrawn after periods of 15 days, and 30 days and were analyzed for their appearance, hardness, friability, drug content and in vitro drug release [7][8][9]. The results revealed that no significant changes in appearance, drug content, hardness, friability, and in vitro release were observed for F10 formulation (Table 5).…”

Section: Stability Studiesmentioning

confidence: 99%

Formulation Development and Evaluation of Gabapentin Controlled Release Tablets

Dembla¹

2015

PPIJ

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The objective of the present study was to develop a pharmaceutically equivalent, stable, robust, cost effective and quality improved formulation of Gabapentin controlled release tablets by using different grades of controlled release polymer. The design of dosage form was performed by choosing Hydroxypropyl Methyl Cellulose (HPMC K100MCR), Hydroxypropyl Methyl Cellulose (HPMC K15MCR), Microcrystalline Cellulose (MCC) and Di-calcium phosphate polymers as matrix builders. The drug-polymer compatibility studies were performed. Blend Uniformity was studied and accordingly the flowability was optimized for the powder blend. Tablets were prepared by direct compression with free flowing powder. The network formed by HPMC, MCC and DCP had been coupled satisfactorily with the controlled resistance, in vitro release and FT-IR. Mean dissolution time was also reported to compare various dissolution profiles. The formula was finalized by comparing the in vitro dissolution with that of the innovator SR and IR tablets. Optimized formulation of Gabapentin was formulated using 23% HPMC K100MCR and 10% of DCP. In vitro drug release profile was examined 98.69% within 12h. The releases of the formulation were fitting to Hixson Crowell model suggesting controlled zero order release from the formulation. The results suggested that direct compression is a suitable method to formulate controlled release Gabapentin tablets and it can perform therapeutically better than conventional immediate release dosage form.

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The influence of surfactants on drug release from a hydrophobic matrix

Cited by 34 publications

References 4 publications

Effects of solubilizing surfactants and loading of antiviral, antimicrobial, and antifungal drugs on their release rates from ethylene vinyl acetate copolymer

Effects of solubilizing surfactants and loading of antiviral, antimicrobial, and antifungal drugs on their release rates from ethylene vinyl acetate copolymer

Wetting Properties of Bile Salt Solutions and Dissolution Media

Formulation Development and Evaluation of Gabapentin Controlled Release Tablets

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