The influence of chitosan and sodium alginate and formulation variables on the formation and drug release from pellets prepared by extrusion/spheronisation

Chatchawalsaisin, Jittima; Podczeck, Fridrun; Newton, JM

doi:10.1016/j.ijpharm.2004.01.025

Cited by 42 publications

(19 citation statements)

References 17 publications

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“…In addition, production of spherical pellets with maximum content of 16% chitosan (Seacure 252) and 50% MCC was also achieved by extrusion/spheronization with a ram extruder and using McIlvaine buffers (0.1 M citric acid and 0.2 M disodium phosphate) as the granulation liquid. 10 The pellets with chitosan from this system could disintegrate in simulated gastric fluid and addition of sodium alginate (1% to 3%) could suppress or extend disintegration of pellets. In pellet production by twin-screw extruder, chitosan (Chitoclear FG95) could be loaded to 50% when using water as the granulation liquid, and could be loaded to 100% when using diluted acetic acid as the granulation liquid.…”

Section: Introductionmentioning

confidence: 94%

“…29 It was reported that the proportion of added sodium alginate (0% to 4%) had an effect on formation, physical properties, and drug release of pellets prepared by a ram extruder. 10 Recently, formation of a polyelectrolyte complex between chitosan and sodium alginate during extrusion using twin-screw extruder and water as the granulation liquid was confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and solid state nuclear magnetic resonance spectroscopy. 16 Thus, the improved pelletization by sodium alginate in the chitosan-containing pellets was probably due to polyelectrolyte complex formation between sodium alginate and chitosan.…”

Section: E4mentioning

confidence: 99%

“…Similar results reported that the sphericity of pellets produced by ram extruder decreased with the addition of 16% wt/wt of chitosan. 9,10 Furthermore, chitosan HW produced pellets with less sphericity than chitosan LW (P G .05). Similar to the chitosan/Avicel RC-591 pellet systems, incorporation of higher viscosity grades of chitosan (Seacure 342 and Seacure 442) resulted in decrease of pellet sphericity and an increase in the surface roughness.…”

Section: Pellet Shapementioning

confidence: 99%

“…The MCC-based pellets are suitable for a controlled release dosage form as they do not disintegrate and prolong drug release, 4-6 which would be a disadvantage when fast release of drug is desired. This led to the study on modification of drug release from pellets by incorporating other excipients into the formulations such as chitosan, [7][8][9][10] alginate, 10,11 and carbopol. 12,13 Some investigations are also performed to find an alternative extrusion aid to MCC, such as chitosan, [14][15][16] pectin, 17 and κ-carragenan.…”

Section: Introductionmentioning

confidence: 99%

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Influence of chitosan type on the properties of extruded pellets with low amount of microcrystalline cellulose

2007

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The purpose of this research was to study the influence of type of chitosan with different molecular weights, ie, 190 and 419 kDa, on properties of pellets prepared by extrusion/ spheronization. The formulations, consisting of acetaminophen as model drug, chitosan, microcrystalline cellulose (MCC), and dibasic calcium phosphate dihydrate with/without sodium alginate, were extruded using a twin-screw extruder and water as the granulating liquid. With 30% wt/wt MCC and no added sodium alginate, spherical pellets were produced containing low and high molecular weight chitosan at a maximum amount of 60% and 40% wt/wt, respectively. With sodium alginate (2.5% wt/wt), pellets with either type of chitosan (60% wt/wt), MCC (17.5% wt/wt), and acetaminophen (20% wt/wt) could be produced indicating an improved pelletforming ability. Type and amount of chitosan and added sodium alginate affected physical properties of pellets including size, roundness, crushing force, and drug release. Low molecular weight chitosan produced pellets with higher mean diameter, sphericity, and crushing force. Additionally, the pellets made of low molecular weight chitosan and added sodium alginate showed faster drug release in 0.1 N HCl but had slower drug release in pH 7.4 phosphate buffer. This indicated that drug release from pellets could be modified by the molecular weight of chitosan. In conclusion, the molecular weight of chitosan had a major influence on formation, physical properties, and drug release from the obtained pellets.

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Section: Introductionmentioning

confidence: 94%

Section: E4mentioning

confidence: 99%

Section: Pellet Shapementioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Influence of chitosan type on the properties of extruded pellets with low amount of microcrystalline cellulose

2007

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“…Chatchawalsaisin et al used a combination of two types of hydrophilic polymers, sodium alginate and chitosan in the formulation of pellets prepared by extrusionspheronization to assess their ability to produce suitable pellets. They reported negligible benefit in using a combination of the two polymers in comparison of sodium alginate alone for sustaining drug release (4). In another study three types of pectin including high methoxylated, low methoxylated, and amidated low methoxylated pectin and different concentrations of granulation liquids (i.e.…”

Section: Introductionmentioning

confidence: 99%

Combination of Pectin and Eudargit RS and Eudragit RL in the Matrix of Pellets Prepared by Extrusion - Spheronization for Possible Colonic Delivery of 5-Amino Salicylic Acid

Akhgari

Abbaspour

Moradkhanizadeh

2013

Jundishapur J Nat Pharm Prod

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Background: Different methods have been studied for targeting drugs to the colon, such as pH-based, time dependent and bacterially degradable systems. However, due to variations in physiological conditions of patients, one system alone could not be completely reliable on colonic drug delivery. Objectives: The aim of this study was preparation and evaluation of a novel colon-specific drug delivery system for 5-ASA (mesalazine) pellets using pectin as a microbially degradable polymeric carrier and Eudragit RS (ERS) and Eudragit RL (ERL) as time-dependent polymers. Materials and Methods: Formulations were constructed based on a multilevel full factorial design. Pellets were prepared via extrusion -spheronization and evaluated for physicochemical properties, image analysis, SEM, FT-IR, DSC and in vitro drug release studies in the simulated gastric fluid with pH = 1.2 (SGF), simulated intestinal fluid with pH = 6.8 (SIF) and simulated colonic fluid with pH = 6.8 in presence of pectinolytic enzyme (SCF). Results: It was shown that in the presence of pectin, formulations without ERL had a relative resistance to drug release in SGF. Pellets containing pectin and the least amount of ERS had the highest burst release effect in SCF. On the other hand, increasing in amount of ERS in the formulations caused a sustained drug release. Presence of pectin in formulations containing ERS and ERL caused sensitivity of formulations to pectinolytic enzyme which can suitable for a colon specific drug delivery system. Conclusions: It was shown that combination of pectin and eudragits can relatively control drug release in the upper GI. On the other hand, pectin degraded in the presence of pectinase and formulations were susceptible to the colonic media.

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Biomaterials as vaccine adjuvants

Jones

2008

Biotechnology Progress

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Biomaterials are promising candidate adjuvants to enhance vaccine efficacy. Through adjuvant design, we can broaden the use of vaccines to diseases such as AIDS, malaria, and cancer. This review addresses the fundamentals of vaccine and adjuvant function in order to determine guidelines for adjuvant design, including aspects of the vaccine such as disease target, antigen formulation, and delivery route. An ideal biomaterial adjuvant will perform three functions. (1) It will deliver the antigen selectively to dendritic cells. This has been accomplished through release of chemokines or cytokines, use of antidendritic cell antibodies, and even through particle size selection. (2) It will activate the dendritic cells, improving antigen presentation. Biomaterials themselves have been shown to activate innate immunity, but specific innate‐activating ligands have also been included in adjuvant formulations. Finally, (3) it will release the antigen appropriately into the dendritic cell. Tuning release to be pH sensitive and engineering endosomal release are strategies that have been used. There is a real opportunity to rationally design better biomaterial adjuvants that will significantly expand and improve vaccine function.

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The influence of chitosan and sodium alginate and formulation variables on the formation and drug release from pellets prepared by extrusion/spheronisation

Cited by 42 publications

References 17 publications

Influence of chitosan type on the properties of extruded pellets with low amount of microcrystalline cellulose

Influence of chitosan type on the properties of extruded pellets with low amount of microcrystalline cellulose

Combination of Pectin and Eudargit RS and Eudragit RL in the Matrix of Pellets Prepared by Extrusion - Spheronization for Possible Colonic Delivery of 5-Amino Salicylic Acid

Biomaterials as vaccine adjuvants

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