A novel core–shell chronotherapeutic system for the oral administration of ketoprofen

Cerciello, Andrea; Auriemma, Giulia; Gaudio, Pasquale Del; Sansone, Francesca; Aquino, Rita Patrizia; Russo, Paola

doi:10.1016/j.jddst.2015.07.017

Cited by 15 publications

(15 citation statements)

References 34 publications

(13 reference statements)

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“…A minimum of one hundred beads images were taken for each batch, in order to obtain particles diameter and relative standard deviation for at least three different prilling processes. Perimeter and projection surface ar-ea obtained by image analysis were used to calculate Sphericity Coefficient (SC) by the following equation [35].…”

Section: Beads Size and Morphologymentioning

confidence: 99%

“…The main technological approaches used to produce polysaccharides-based Drug Delivery Systems (DDS) include spray drying [28], spray-chilling [29], freeze-drying [30,31], coacervation [32], emulsification followed by evaporation or solvent extraction [33] and prilling [34,35]. Among them prilling, also known as laminar jet break-up, has been considered a proper tool in creating polymeric hydrophilic microparticles (gel-beads) as modified delivery devices [36].…”

Section: Introductionmentioning

confidence: 99%

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Pectin and Zinc Alginate: The Right Inner/Outer Polymer Combination for Core-Shell Drug Delivery Systems

et al. 2020

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Core-shell beads loaded with betamethasone were developed using co-axial prilling as production technique and pectin plus alginate as polymeric carriers. During this study, many operative conditions were intensively investigated to find the best ones necessary to produce uniform core-shell particle systems in a reproducible way. Particularly, feed solutions’ composition, polymers mass ratios and the effect of the main process parameters on particles production, micromeritics, inner structure, drug loading and drug-release/swelling profiles in simulated biological fluids were studied. The optimized core-shell formulation F5 produced with a pectin core concentration of 4.0% w/v and an alginate shell concentration of 2.0% w/v (2:1 core:shell ratio) acted as a sustained drug delivery system. It was able to reduce the early release of the drug in the upper part of the gastro-intestinal tract for the presence of the zinc-alginate gastro-resistant outer layer and to specifically deliver it in the colon, thanks to the selectivity of amidated low methoxy pectin core for this district. Therefore, these particles may be proposed as colon targeted drug delivery systems useful for inflammatory bowel disease (IBD) therapy.

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Section: Beads Size and Morphologymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Pectin and Zinc Alginate: The Right Inner/Outer Polymer Combination for Core-Shell Drug Delivery Systems

et al. 2020

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“…Prilling is a mild and scalable microencapsulation technique working essentially through two steps: the breaking apart of a laminar jet of alginate solution into a row of mono-sized drops through a vibrating nozzle and the successive drops' ionotropic gelling in a solution of cations acting as crosslinkers. In the last few years, a large variety of gel-beads has been produced, varying the types of polysaccharides (mainly alginate, pectin, chitosan, and so on) used alone or in combination [10,11]; the configuration of the prilling apparatus to obtain 'only core' or core-shell beads [12]; and the gelling conditions in terms of cross-linker, pH of the reticulation solution, and gelling time [13,14]. Moreover, calcium alginate has often been used in combination with different gas-generating agents such as sodium bicarbonate, calcium carbonate, and citric acid or tartaric acid to obtain low-density floating formulations [15][16][17].…”

Section: Introductionmentioning

confidence: 99%

Zinc and Calcium Cations Combination in the Production of Floating Alginate Beads as Prednisolone Delivery Systems

et al. 2020

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The aim of this research was to verify the application of alginate in combination with Ca2+ and Zn2+ ions to produce a floating and prolonged release system for the oral administration of prednisolone. Hollow and floating gel-beads were designed using prilling/ionotropic gelation as the microencapsulation technique, zinc acetate in the gelling solution as the alginate external crosslinker, and calcium carbonate in the feed as the internal crosslinking agent able to generate gas when in contact with the acidic zinc acetate solution. To achieve this goal, drug/alginate solutions were opportunely combined with different amounts of calcium carbonate. The effect of the addition of calcium carbonate into the feed solution on buoyancy, encapsulation efficiency, morphology, size distribution, as well as in vitro drug release profile of the alginate particles was studied. Moreover, the ability of the floating beads to modulate in vivo the anti-inflammatory response was assayed using the carrageenan-induced acute oedema in rat paw. The proposed strategy allowed obtaining alginate beads with extremely high encapsulation efficiency values (up to 94%) and a very porous inner matrix conferring buoyancy in vitro in simulated gastric fluid up to 5 h. Moreover, in vivo, the best formulation, F4, resulted in the ability to prolong the anti-inflammatory effect up to 15 h compared with raw prednisolone.

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“…Ketoprofen-loaded core particles based on Zn-pectinate matrix were produced by prilling technique using optimized operative conditions [53]. Beads micromeritics, solid state, and drug release properties were studied using established method (SEM, DSC, USP 36 Paddle Dissolution).…”

Section: Methodsmentioning

confidence: 99%

“…These preliminary results have been the starting point to further improve technological properties of gel-beads' formulations in terms of ketoprofen loading and release performances. Therefore, in the following study, we designed a more complex system based on core/shell particles (double-layered particles) consisting of a Zn-pectinate core loading NSAID and an enteric shell of Eudragit S100 (anionic copolymer of methacrylic acid and methyl methacrylate insoluble in acid pH) [53]. Among different commercially available pectins, we focused our attention on amidated low methoxy (ALM) pectin (esterification degree 24% and amidation degree 23%) that, showing high hydrophobic interactions between pectin chains and internal hydrogen bonding between amide groups, is able to stabilize the egg-box structure [54].…”

Section: Approach #2mentioning

confidence: 99%

NSAIDS: Design and Development of Innovative Oral Delivery Systems

Auriemma¹,

Cerciello²,

Aquino³

2017

Nonsteroidal Anti-Inflammatory Drugs

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Recently, different technologies have been used to transform active pharmaceutical ingredients (APIs) into new dosage forms. Engineered drug delivery systems may modify biopharmaceutical properties of the API achieving either immediate or delayed release according to specific therapeutic needs. Particularly, preprogrammed release of oral formulations delivering the drug at expected times may be useful in chronotherapy of early morning pathologies. The conventional approach when dealing with such diseases is to administer NSAIDs two to three times daily. This approach does not allow to fit drug release with symptoms onset resulting in inefficient therapy and poor patient compliance. NSAIDs may be very effective if administered at least 4-6 h before the pain reaches its peak in the early morning. The solution could be to design delayed drug delivery systems allowing one administration before going to sleep acting in the early morning. This chapter highlights new approaches in developing controlled delivery systems of NSAIDs potentially useful to treat both acute and chronic inflammation. The chapter illustrates the versatility of laminar jet break-up technology (prilling) to produce gel beads able to control rate and time of drug delivery. A special focus will be on particle-engineering strategies, i.e., prilling and prilling technique in tandem with microwave or supercritical fluid-assisted drying.

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A novel core–shell chronotherapeutic system for the oral administration of ketoprofen

Cited by 15 publications

References 34 publications

Pectin and Zinc Alginate: The Right Inner/Outer Polymer Combination for Core-Shell Drug Delivery Systems

Pectin and Zinc Alginate: The Right Inner/Outer Polymer Combination for Core-Shell Drug Delivery Systems

Zinc and Calcium Cations Combination in the Production of Floating Alginate Beads as Prednisolone Delivery Systems

NSAIDS: Design and Development of Innovative Oral Delivery Systems

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