Sustained-Release and Swelling Characteristics of Xanthan Gum/Ethylcellulose-Based Injection Moulded Matrix Tablets: in Vitro and in Vivo Evaluation

Quinten, T.; Beer, Thomas De; Onofre, Fernanda O.; Méndez‐Montealvo, Guadalupe; Wang, Y.J.; Remon, Jean Paul; Vervaet, Chris

doi:10.1002/jps.22480

Cited by 22 publications

(10 citation statements)

References 29 publications

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“…As a commonly used alternative plasticizer, dibutyl sebacate has been well documented. [2][3][4]19) However, our previous studies on phthalate esters demonstrated that not only DBP but also phthalate esters with short chain alcohol exhibited adjuvant effect. 6,7) As to sebacate esters, there is a report of Twenty-four hours after skin application of 0.5% FITC in acetone alone, or in acetone containing 50% DBP (positive control) or 20% DIPS, cells in the draining lymph nodes were analyzed as to the levels of FITC (abscissa) and CD11c (ordinate) by flow cytometry.…”

Section: )mentioning

confidence: 96%

“…Another type of aliphatic plasticizers is sebacate esters, which are applied for medical devices as well as drug formulation. [2][3][4] We have been investigating phthalate esters from an immuno-toxicological point of view. We showed that contact sensitization to fluorescein isothiocyanate (FITC) is enhanced in the presence of certain types of phthalate esters in mouse models.…”

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confidence: 99%

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An Aliphatic Ester Diisopropyl Sebacate Exhibited an Adjuvant Effect on Fluorescein Isothiocyanate-Induced Contact Hypersensitivity Mouse Models

Kurohane

Kimura

Terasawa

et al. 2018

Biological & Pharmaceutical Bulletin

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Alternative plasticizers have become more popular due to health concerns about phthalate esters. We demonstrated that phthalate esters enhanced skin sensitization to fluorescein isothiocyanate (FITC) in mouse contact hypersensitivity models. Alternative plasticizers have not been well studied as to their effect on the immune system. We previously found that diisopropyl adipate (DIPA), an aliphatic dicarboxylic acid ester, enhanced skin sensitization to FITC. Sebacate esters are also widely used as alternative plasticizers. Here we tested diisopropyl sebacate (DIPS), which has the same alcohol with an aliphatic dicarboxylic acid of longer chain, using BALB/c mice. The results showed that DIPS facilitated skin sensitization to FITC and increased FITC-presenting dendritic cell trafficking from the skin to draining lymph nodes. Furthermore, DIPS activated transient receptor potential ankyrin 1 (TRPA1). The latter feature has been commonly observed for phthalate esters and DIPA, which have adjuvant effects. In summary, the adjuvant effect of a sebacate ester was demonstrated in a mouse model. Key words sebacate ester; adjuvant; alternative plasticizer; contact hypersensitivity; mouse Due to health concerns about phthalate esters, expectation of the use of alternative plasticizers in consumer products has been increasing. 1) Phthalate esters are made up of an aromatic dicarboxylic acid and two alcohols. One group of alternative plasticizers is the adipate esters, which consist of an aliphatic dicarboxylic acid. Another type of aliphatic plasticizers is sebacate esters, which are applied for medical devices as well as drug formulation. 2-4)We have been investigating phthalate esters from an immuno-toxicological point of view. We showed that contact sensitization to fluorescein isothiocyanate (FITC) is enhanced in the presence of certain types of phthalate esters in mouse models. 5,6) Thus, phthalate esters with short chain alcohols, such as dibutyl phthalate (DBP) and di-n-propyl phthalate (DPP), exhibited strong activities among phthalate esters. 6)Those phthalate esters were shown to exhibit agonist activity toward transient receptor potential ankyrin 1 (TRPA1) cation channels, TRPA1 being used as a nociceptor by sensory neurons.7) The results may suggest a close relationship between the adjuvant activity on skin sensitization and TRPA1 agonistic activity.As to alternative plasticizers, we previously showed that diisopropyl adipate (DIPA) facilitated skin sensitization to FITC in vivo. TRPA1 agonist activity of DIPA was also shown in vitro. 8) In the present study, we investigated the activity of diisopropyl sebacate (DIPS), in which isopropyl alcohol is a shared component with DIPA. As a positive control, we employed DBP to check each experimental system. The results clearly demonstrated that DIPS also activated TRPA1 and enhanced FITC-induced contact hypersensitivity (CHS). (Osaka, Japan), FITC and Fluo 4-AM from Dojindo Laboratories (Kumamoto, Japan), dimethyl sulfoxide (DMSO) from Nacalai Tesque (Kyoto, Japan), a...

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Section: )mentioning

confidence: 96%

mentioning

confidence: 99%

An Aliphatic Ester Diisopropyl Sebacate Exhibited an Adjuvant Effect on Fluorescein Isothiocyanate-Induced Contact Hypersensitivity Mouse Models

Kurohane

Kimura

Terasawa

et al. 2018

Biological & Pharmaceutical Bulletin

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“…The paddle speed was set at 50 rpm, while the temperature of the medium was maintained at 37±0.5°C. Samples of 5 mL were withdrawn at specific time points (0.5, 1, 2, 4,6,8,12,16,20, and 24 h without media replacement) and spectro-photometrically assessed by means of a double beam spectrophotometer (UV-1650PC, Shimadzu, Belgium; λ max MPT, MPS and MPF was 222, 222 and 220 nm respectively). The MPT, MPF or MPS content in the samples was determined by linear regression.…”

Section: In Vitro Drug Releasementioning

confidence: 99%

“…In these studies, drug release from IM tablets was sustained using ethylcellulose as matrix former and using various hydrophilic fillers (hydroxypropylmethylcellulose, lowsubstituted hydroxypropylcellulose, polyethylene oxide and xanthan gum) to control the release rate. Only the use of xanthan gum resulted in zero-order release; and for all these systems, drug was released by a combination of polymer swelling, Fickian diffusion and matrix erosion (4)(5)(6)(7). In addition, hot melt methods (i.e.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Sustained-Release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding

et al. 2012

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Abstract. Sustained-release matrix tablets based on Eudragit RL and RS were manufactured by injection moulding. The influence of process temperature; matrix composition; drug load, plasticizer level; and salt form of metoprolol: tartrate (MPT), fumarate (MPF) and succinate (MPS) on ease of processing and drug release were evaluated. Formulations composed of 70/30% Eudragit RL/MPT showed the fastest drug release, substituting part of Eudragit RL by RS resulted in slower drug release, all following first-order release kinetics. Drug load only affected drug release of matrices composed of Eudragit RS: a higher MPT concentration yielded faster release rates. Adding triethyl citrate enhanced the processability, but was detrimental to long-term stability. The process temperature and plasticizer level had no effect on drug release, whereas metoprolol salt form significantly influenced release properties. The moulded tablets had a low porosity and a smooth surface morphology. A plasticizing effect of MPT, MPS and MPF on Eudragit RS and Eudragit RL was observed via DSC and DMA. Solubility parameter assessment, thermal analysis and X-ray diffraction demonstrated the formation of a solid solution immediately after production, in which H-bonds were formed between metoprolol and Eudragit as evidenced by near-infrared spectroscopy. However, high drug loadings of MPS and MPF showed a tendency to recrystallise during storage. The in vivo performance of injection-moulded tablets was strongly dependent upon drug loading.

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“…While sustained drug release can be achieved based on the design of the dosage form (reservoir systems vs. matrices) and/or the physicochemical properties of the polymeric materials incorporated in the formulation (diffusion controlled vs. delayed polymer dissolution), hot melt extrusion (HME) (possibly in combination with injection molding) has been evaluated to manufacture sustainedrelease matrices using various polymers: ethylcellulose (EC) [1][2][3], hydroxypropyl (methyl) cellulose (HP(M)C) [4], ethylene vinyl acetate (EVA) [5][6], polyvinyl acetate (PVA) [7], poly lactic (co-glycolic) acid (PL(G)A) [8][9], silicone [10], polycaprolactone (PCL) [11][12], polyoxazolines [13], polyanhydrides [14], methacrylate copolymers (Eudragit ® RS/RL) [15][16], and several lipid materials [17][18][19]. While sustained-release dosage forms have been successfully developed via HME using these polymers, a common drawback is that the drug load in these formulations is often low, either linked to processing issues during HME of formulations with a high drug load, or due to a significant burst release when less polymeric matrix former is incorporated in the formulation.…”

Section: Introductionmentioning

confidence: 99%

Thermoplastic polyurethanes for the manufacturing of highly dosed oral sustained release matrices via hot melt extrusion and injection molding

Claeys

Vervaeck

Hillewaere

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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This study evaluated thermoplastic polyurethanes (TPUR) as matrix excipients for the production of oral solid dosage forms via hot melt extrusion (HME) in combination with injection molding (IM). We demonstrated that TPURs enable the production of solid dispersions -crystalline API in a crystalline carrier -at an extrusion temperature below the drug melting temperature (Tm) with a drug content up to 65% (wt.%). The release of metoprolol tartrate was controlled over 24h, whereas a complete release of diprophylline was only possible in combination with a drug release modifier: polyethylene glycol 4000 (PEG 4000) or Tween 80. No burst release nor a change in tablet size and geometry was detected for any of the formulations after dissolution testing. The total matrix porosity increased gradually upon drug release. Oral administration of TPUR did not affect the GI ecosystem (pH, bacterial count, short chain fatty acids), monitored via the Simulator of the Human Intestinal Microbial Ecosystem (SHIME). The high drug load (65wt.%) in combination with (in-vitro and in-vivo) controlled release capacity of the formulations, is noteworthy in the field of formulations produced via HME/IM.

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Sustained-Release and Swelling Characteristics of Xanthan Gum/Ethylcellulose-Based Injection Moulded Matrix Tablets: in Vitro and in Vivo Evaluation

Cited by 22 publications

References 29 publications

An Aliphatic Ester Diisopropyl Sebacate Exhibited an Adjuvant Effect on Fluorescein Isothiocyanate-Induced Contact Hypersensitivity Mouse Models

An Aliphatic Ester Diisopropyl Sebacate Exhibited an Adjuvant Effect on Fluorescein Isothiocyanate-Induced Contact Hypersensitivity Mouse Models

Preparation and Evaluation of Sustained-Release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding

Thermoplastic polyurethanes for the manufacturing of highly dosed oral sustained release matrices via hot melt extrusion and injection molding

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