Enteric Controlled-Release Pantoprazole-Loaded Microparticles Prepared by Using Eudragit S100 and Poly(ε-caprolactone) Blend

Raffin, Renata Platcheck; Colomé, Letícia Marques; Guterres, Sílvia Stanisçuaski; Pohlmann, Adriana Raffin

doi:10.1080/10837450701556933

Cited by 22 publications

(9 citation statements)

References 37 publications

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“…When delivering acid sensitive bioactives orally there are often problems associated with the low pH of the stomach adversely affecting the administration. Examples of such bioactives include acid-labile drugs, such as penicillin G, antigens, or microorganisms, such as live bacterial vaccines or probiotic bacteria. , Although the entrapment of these species in enteric dosage forms has been shown to improve drug stability, or reduce cell death, , the mechanisms of protection are usually hypothesized and very rarely demonstrated or quantified dynamically. These mechanisms are likely to be either a result of the polymer’s insolubility in acid, halting penetration of acid into the polymer matrix, or the buffering capacity of the polymers in the formulation raising the pH inside the matrices to a level which is no longer harmful to the encapsulated material. , …”

Section: Introductionmentioning

confidence: 99%

CLSM Method for the Dynamic Observation of pH Change within Polymer Matrices for Oral Delivery

Cook¹,

Saratoon

Tzortzis

et al. 2013

Biomacromolecules

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If acid-sensitive drugs or cells are administered orally, there is often a reduction in efficacy associated with gastric passage. Formulation into a polymer matrix is a potential method to improve their stability. The visualization of pH within these materials may help better understand the action of these polymer systems and allow comparison of different formulations. We herein describe the development of a novel confocal laser-scanning microscopy (CLSM) method for visualizing pH changes within polymer matrices and demonstrate its applicability to an enteric formulation based on chitosan-coated alginate gels. The system in question is first shown to protect an acid-sensitive bacterial strain to low pH, before being studied by our technique. Prior to this study, it has been claimed that protection by these materials is a result of buffering, but this has not been demonstrated. The visualization of pH within these matrices during exposure to a pH 2.0 simulated gastric solution showed an encroachment of acid from the periphery of the capsule, and a persistence of pHs above 2.0 within the matrix. This implies that the protective effect of the alginate-chitosan matrices is most likely due to a combination of buffering of acid as it enters the polymer matrix and the slowing of acid penetration.

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Section: Introductionmentioning

confidence: 99%

CLSM Method for the Dynamic Observation of pH Change within Polymer Matrices for Oral Delivery

Cook¹,

Saratoon

Tzortzis

et al. 2013

Biomacromolecules

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“…Their advantages include the ability to improve the stability and bioavailability of the drug substance, modification and control of its release site and rate. The most common methods of microparticle production are the solvent evaporation or emulsification method [ 51 , 52 , 198 , 199 , 200 , 201 , 202 , 203 , 204 , 205 , 206 , 207 , 208 , 209 , 210 , 211 , 212 , 213 , 214 ] and spray-drying [ 199 , 200 , 215 , 216 , 217 , 218 , 219 , 220 ]. The advantage of the latter over the other methods is the ease of process scale-up [ 215 ].…”

Section: Development Of New Formulations With Ppismentioning

confidence: 99%

“…Raffin et al [ 209 ] developed double-walled microparticles using the two-step emulsification method. Pantoprazole was microencapsulated using biodegradable polymer poly(ε-caprolactone) and subsequently coated with Eudragit S100 to provide the colonic delivery of the drug substance.…”

Section: Development Of New Formulations With Ppismentioning

confidence: 99%

Formulation of Dosage Forms with Proton Pump Inhibitors: State of the Art, Challenges and Future Perspectives

2022

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Since their introduction to pharmacotherapy, proton pump inhibitors (PPIs) have been widely used in the treatment of numerous diseases manifested by excessive secretion of gastric acid. Despite that, there are still unmet needs regarding their availability for patients of all age groups. Their poor stability hinders the development of formulations in which dose can be easily adjusted. The aim of this review is to describe the discovery and development of PPIs, discuss formulation issues, and present the contemporary solutions, possibilities, and challenges in formulation development. The review outlines the physicochemical characteristics of PPIs, connects them with pharmacokinetic and pharmacodynamic properties, and describes the stability of PPIs, including the identification of the most important factors affecting them. Moreover, the possibilities for qualitative and quantitative analysis of PPIs are briefly depicted. This review also characterizes commercial preparations with PPIs available in the US and EU. The major part of the review is focused on the presentation of the state of the art in the development of novel formulations with PPIs covering various approaches employed in this process: nanoparticles, microparticles, minitablets, pellets, bilayer, floating, and mucoadhesive tablets, as well as parenteral, transdermal, and rectal preparations. It also anticipates further possibilities in the development of PPIs dosage forms. It is especially addressed to the researchers developing new formulations containing PPIs, since it covers the most important formulary issues that need to be considered before a decision on the selection of the formula is made. It may help in avoiding unnecessary efforts in this process and choosing the best approach. The review also presents an up-to-date database of publications focused on the pharmaceutical technology of formulations with PPIs.

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“…Microparticles were prepared by the simple emulsion-solvent evaporation technique, widely employed to produce particles from different polymers [22]. The optimized morphology of the microparticles was obtained using a polymer concentration of 10% w/v and a PVA concentration in the aqueous phase of 1.5% w/v.…”

Section: Preparation and Characterization Of Microparticlesmentioning

confidence: 99%

Development of Novel Controlled Release Gliclazide-Loaded poly(ε- caprolactone) Microparticles: Effect of Polymer Blends

Barakat¹,

Al-Shazli²,

Almedany³

2012

Pharm Anal Acta

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Gliclazide-loaded microparticles made with a polymeric blend were prepared by a solvent evaporation technique. Organic solutions of two polymers, poly (epsilon-caprolactone) (PCL) and Eudragit RS (E RS) or ethyl cellulose (EC), in different weight ratios, and 33.3% of GLZ were prepared and dropped into aqueous solution of poly vinyl alcohol, in different experimental conditions, achieving drug-loaded microparticles. The obtained microparticles were characterized in terms of yield of production, shape, size, surface properties, drug content, and in vitro drug release behavior. The physical state of the drugs and the polymer was determined by scanning electron microscopy (SEM), Fourier transform infra red and differential scanning calorimetry (DSC). Following the in vitro release studies microparticles made from blends of polymer, PCL/E RS or EC showed slower drug release than microparticles made from single PCL polymer. Surface morphology also revealed presence of porous and spherical structure of microparticles. Microparticles showing sustained release of GLZ were examined in rabbit and serum GLZ concentrations were calculated using HPLC method of assay.

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Enteric Controlled-Release Pantoprazole-Loaded Microparticles Prepared by Using Eudragit S100 and Poly(ε-caprolactone) Blend

Cited by 22 publications

References 37 publications

CLSM Method for the Dynamic Observation of pH Change within Polymer Matrices for Oral Delivery

CLSM Method for the Dynamic Observation of pH Change within Polymer Matrices for Oral Delivery

Formulation of Dosage Forms with Proton Pump Inhibitors: State of the Art, Challenges and Future Perspectives

Development of Novel Controlled Release Gliclazide-Loaded poly(ε- caprolactone) Microparticles: Effect of Polymer Blends

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