Novel co-axial prilling technique for the development of core–shell particles as delayed drug delivery systems

Gaudio, Pasquale Del; Auriemma, Giulia; Russo, Paola; Mencherini, Teresa; Campiglia, Pietro; Stigliani, Mariateresa; Aquino, Rita Patrizia

doi:10.1016/j.ejpb.2014.02.010

Cited by 34 publications

(17 citation statements)

References 47 publications

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“…During the process, the polymeric jet is broken-up by radiofrequency into uniform core-shell droplets that drip into a Zn 2+ gelling solution and "solidify". Polymeric feed solutions' composition were set according to our previous research experiences [40]. In detail, the main formulations (F3-F4-F5) were designed fixing pectin core composition (polymer concentration 4.0% w/v; B/pct mass ratio 1:20) and modifying alginate solution concentration from 1.0% to 2.0% w/v, that is, decreasing core/shell mass ratio from 4:1 to 2:1 ( Table 1).…”

Section: Core-shell Beads' Production and Characterizationmentioning

confidence: 99%

“…This technique essentially consists of two operations: the first is based on the breaking apart of a laminar jet of polymer solution into a row of mono-sized drops by means of a vibrating nozzle device, the second on their "solidification" through the ionotropic gelation method, exploiting the ability of polyelectrolyte polymers to cross-link in presence of counter ions [37][38][39]. Prilling technology offers different advantages; it is a mild and easy scalable microencapsulation technique that, if used in the co-axial configuration and in the proper operative conditions, could be used to obtain, in a single productive step, particles with multiple layers of different polymeric materials [40].The appropriate combination of two or more polysaccharides may be an effective way to prevent the early release of the drug in the upper part of the gastro-intestinal tract (GIT) that, as well known, represents the major drawback of oral formulations based on single polysaccharides [20,[41][42][43]. In addition, a multilayered system offers the possibility to release the drug in a specific district of the organism or in a precise moment of the day as required, for example, for the treatment of severe chronic mucosal inflammations such as IBD.…”

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: Core-shell Beads' Production and Characterizationmentioning

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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“…A minimum of 100 beads images were analyzed for each batch, and relative SD for at least three different prilling processes was calculated. Perimeter and projection surface area obtained by image analysis were used to calculate beads coefficient of sphericity (SC) by the following equation 14 :…”

Section: Beads Size Morphology and Inner Structurementioning

confidence: 99%

Design and In Vivo Anti-Inflammatory Effect of Ketoprofen Delayed Delivery Systems

Cerciello

Auriemma

Morello

et al. 2015

Journal of Pharmaceutical Sciences

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“…The process conditions strongly affect properties of the resultant dried microparticles such as size, morphology, and shape. In contrast to other techniques commonly used for enteric microsphere preparation, such as emulsion-solvent evaporation, prilling [17], and coacervation, spray drying is a one-step, continuous process that is highly reproducible and relatively easy to scale up [18].…”

Section: Introductionmentioning

confidence: 99%

Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design

et al. 2019

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Halimium halimifolium (Hh) is a shrub used in Algerian folk medicine to treat gastrointestinal pain. An UHPLC-PDA-ESI/MSn method was developed to identify the metabolic profile of the traditionally used infusion (Hh-A) from the aerial parts. The structures of flavanols were confirmed by NMR analysis after the isolation procedure from a hydrohalcolic extract (Hh-B) that also allowed for the identification of phenolic acids, an aryl butanol glucoside, and different derivatives of quercetin, myricetin, and kaempferol. Tiliroside isomers were the chemical markers of Hh-A and Hh-B (54.33 and 36.00 mg/g, respectively). Hh-A showed a significant scavenging activity both against the radicals 1,1-diphenyl-2-picrylhydrazyl and 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (EC50 = 10.49 µg/mL and TEAC value = 1.98 mM Trolox/mg infusion) and the lipopolysaccharide-induced reactive oxygen species release in A375 and HeLa cells. Moreover, the antihyperglycemic properties, by inhibiting the α-amylase and α-glucosidase enzymes (IC50 = 0.82 mg/mL and 25.01 µg/mL, respectively), were demonstrated. To upgrade the therapeutic effect, a microencapsulation process is proposed as a strategy to optimize stability, handling, and delivery of bioactive components, avoiding the degradation and loss of the biological efficacy after oral intake. Hh-loaded microparticles were designed using cellulose acetate phthalate as the enteric coating material and spray drying as a production process. The results showed a satisfactory process yield (67.9%), encapsulation efficiency (96.7%), and micrometric characteristics of microparticles (laser-scattering, fluorescent, and scanning electron microscopy). In vitro dissolution studies (USPII-pH change method) showed that Hh-loaded microparticles are able to prevent the release and degradation of the bioactive components in the gastric tract, releasing them into the intestinal environment.

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Novel co-axial prilling technique for the development of core–shell particles as delayed drug delivery systems

Cited by 34 publications

References 47 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

Design and In Vivo Anti-Inflammatory Effect of Ketoprofen Delayed Delivery Systems

Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design

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