Effect of different dispersing agents on the characteristics of Eudragit microspheres prepared by a solvent evaporation method

Horoz, B. Bahar; Kiliçarslan, Müge; Yüksel, Nilüfer; Baykara, Tamer

doi:10.1080/02652040310001637893

Cited by 19 publications

(17 citation statements)

References 17 publications

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“…Expectedly, this manner of release is related to the pH responsiveness of Eudragit RL100 (Pignatello et al, 2000;Philip et al, 2010). Similar result was observed when Eudragit RS 100 was used in the formulation of a certain drug molecule (Horoz et al, 2004). In another study by Philip et al (2010), the author presented a similar effect when a pH responsiveness material such as sodium alginate was used in oral delivery of insulin.…”

Section: Release Studysupporting

confidence: 67%

Microspheres of insulin-Eudragit complex: Formulation, characterization and in vivo studies

Momoh¹,

Jackson²,

Musiliu³

et al. 2017

Afr. J. Pharm. Pharmacol.

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Insulin, a hormonal drug for the management of diabetes mellitus has continued to attract attention of many researchers and pharmaceutical formulators for more than a decade. However, its low oral bioavailability due to the activities of intestinal enzymes restricts its route of administration to only the parenteral route. This study was designed to evaluate the capacity of mucoadhesive microspheres formulated with varying blends of Eudragit ® RL 100 and Eudragit ® RS 100 to protect insulin for oral administration. Microspheres containing varying blends of Eudragit ® RL 100/RS100 loaded insulin was prepared by solvent evaporation method and were characterized in vitro and in vivo. Results showed that stable formulation with high encapsulation efficiency, positive zeta potential and high bioadhesion were obtained in all the formulations. In vitro release showed a maximum release of 9 and 87% release in pH 1.2 and 7.2, respectively. Single oral studies showed a decreased in blood glucose level comparably equal to that of subcutaneous (sc) administration. The results of this study indicate that insulin-loaded Eudragit RL100/RS100 microspheres could be a promising drug delivery system to improve oral absorption of insulin.

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Section: Release Studysupporting

confidence: 67%

Microspheres of insulin-Eudragit complex: Formulation, characterization and in vivo studies

Momoh¹,

Jackson²,

Musiliu³

et al. 2017

Afr. J. Pharm. Pharmacol.

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“…The solvent evaporation method of microencapsulation involves the use of emulsification of a solution containing polymer and drug with an additional medium in which the drug and polymer cannot dissolve [8].…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Perindopril Microencapsules by Using Different Polymer

Jacob¹,

Tv²,

Abraham³

2017

Asian J Pharm Clin Res

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Objective: The study was conducted with an objective to achieve a potential sustained release oral drug delivery system of an antihypertensive drug, perindopril which is a angiotensin converting enzyme inhibitor having half-life of 2 hrs. Perindopril is water-soluble drug, so we can control or delay the release rate of drug using release retarding polymers. This may also decrease the toxic side effects by preventing the high initial concentration in the blood.Methods: Microcapsules were prepared by solvent evaporation technique using Eudragit L100 and ethyl cellulose as a retarding agent to control the release rate and magnesium stearate as an inert dispersing carrier to decrease the interfacial tension between lipophilic and hydrophilic phase.Results: Prepared microcapsules were evaluated for the particle size, percentage yield, drug entrapment efficiency, flow property, and in vitro drug release for 12 hrs. Results indicated that the percentage yield, mean particle size, drug entrapment efficiency, and the micrometric properties of the microcapsules were influenced by various drug:polymer ratio. The release rate of microcapsules could be controlled as desired by adjusting the combination ratio of dispersing agents to retarding agents. Conclusion:Perindopril microcapsules can be successfully designed to develop sustained drug delivery that reduces the dosing frequency and their by one can increase the patient compliance.

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“…13 Eudragit RLPO and RSPO are pH-independent polymers, inert to the digestive tract, impermeable to water, as well as capable of swelling and release active ingredients by diffusion. 14 As a result microspheres of Metformin HCl using Eudragit RSPO or Eudragit RLPO will give a time dependent controlled release which will ultimately potentiate the pharmacologic efficacy of the drug.…”

Section: Introductionmentioning

confidence: 99%

Evaluation and Optimization of Influence of Permeability Property and Concentration of Polymethacrylic Polymers on Microspheres of Metformin HCl

Hasan

Paul

Akhter

et al. 2014

Dhaka Univ. J. Pharm. Sci

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Metformin HCl microspheres were prepared with the aim of increasing its bioavailability and decreasing gastrointestinal side effects by means of sustained action. Eudragit RSPO and Eudragit RLPO, polymers of different permeability characteristics were used to prepare different microspheres. Emulsification solvent evaporation technique using acetone as the internal phase and liquid paraffin as the external phase was the method of choice. Six formulations were prepared using two polymers. The effect of drug loading and polymeric property on the surface morphology, entrapment efficiency, particle size and release characteristics of the microspheres were examined. FTIR and DSC studies established compatibility of the drug with the polymers. SEM studies clearly revealed the effect of drug loading and polymeric nature on the surface morphology of the microspheres.Entrapment efficiencies were within 77.09-97.11% and particle size of all the batches were in the acceptable range.Release data were treated with different mathematical kinetic models. The drug release profile showed that Eudragit RSPO and Eudragit RLPO have opposite effect on drug release. On the other hand, increase in drug loading results in increased drug release. Kinetic modeling of in vitro dissolution profiles revealed that the drug release mechanism varies from diffusion controlled to anomalous type.

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Effect of different dispersing agents on the characteristics of Eudragit microspheres prepared by a solvent evaporation method

Cited by 19 publications

References 17 publications

Microspheres of insulin-Eudragit complex: Formulation, characterization and in vivo studies

Microspheres of insulin-Eudragit complex: Formulation, characterization and in vivo studies

Formulation and Evaluation of Perindopril Microencapsules by Using Different Polymer

Evaluation and Optimization of Influence of Permeability Property and Concentration of Polymethacrylic Polymers on Microspheres of Metformin HCl

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