In vitro and in vivo preclinical evaluation of a minisphere emulsion-based formulation (SmPill®) of salmon calcitonin

Aguirre, Tanira; Rosa, Mónica; Coulter, Ivan S.; Brayden, David J.

doi:10.1016/j.ejps.2015.09.001

Cited by 23 publications

(23 citation statements)

References 38 publications

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“…Salmon calcitonin (sCT, MW 3432), is a benchmark peptide to test any technology for oral delivery as it encompasses all five problems [2]. It is a second line anti-resorptive treatment for osteoporosis, as well as for Paget's disease and hypercalcemia, and is marketed in injectable and nasal formats [3].…”

Section: Introductionmentioning

confidence: 99%

“…Minispheres were kept in Miglyol 810 ® at 2-8°C for 30 min, separated with a sieve and allowed to dry at 2-8°C for 7 days. Additional minisphere prototypes loaded with sCT were prepared using a water-in-oil emulsion method [2]. The theoretical percentage of each component in four dried minisphere formulation prototypes is shown ( Table 1).…”

Section: Smpill ® Minisphere Preparation With Pesmentioning

confidence: 99%

“…Minispheres were prepared by the methods of [2,21], but using only an aqueous phase. Formulations were prepared at 65°C by mixing milliQ ® water, gelatin, sorbitol, followed by addition of an oral suspension of 1 g/ml BaSO 4 .…”

Section: Smpill ® Minisphere Preparation With Pesmentioning

confidence: 99%

“…and intra-colonic (i.c.) instillations [2]. The objectives of this work were firstly to develop suitable coatings for sCT-SmPill ® minispheres and then to use X-ray imaging to confirm delivery to rat jejunum and to rat colon following oral administration.…”

Section: Introductionmentioning

confidence: 99%

“…However, most peptides have unfavorable physicochemical properties for oral delivery including large molecular weight (MW), high hydrophilicity, a tendency to aggregate, susceptibility to pancreatic serine proteases, and low intestinal permeability [2].…”

Section: Introductionmentioning

confidence: 99%

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Coated minispheres of salmon calcitonin target rat intestinal regions to achieve systemic bioavailability: Comparison between intestinal instillation and oral gavage

Aguirre

Aversa

Rosa

et al. 2016

Journal of Controlled Release

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Achieving oral peptide delivery is an elusive challenge. Emulsion-based minispheres of salmon calcitonin (sCT) were synthesized using single multiple pill (SmPill ® ) technology incorporating the permeation enhancers (PEs): sodium taurodeoxycholate (NaTDC), sodium caprate (C 10 ), or coco-glucoside (CG), or the pH acidifier, citric acid (CA). Minispheres were coated with an outer layer of Eudragit ® L30 D-55 (designed for jejunal release) or Surelease ® /Pectin (designed for colonic release). The process was mild and in vitro biological activity of sCT was retained upon release from minispheres stored up to 4 months. In vitro release profiles suggested that sCT was released from minispheres by diffusion through coatings due to swelling of gelatin and the polymeric matrix upon contact with PBS at pH 6.8.X-ray analysis confirmed that coated minispheres dissolved at the intended intestinal region of rats following oral gavage. Uncoated minispheres at a dose of ~2000 I.U. sCT/kg were administered to rats by intra-jejunal (i.j.) or intra-colonic (i.c.) instillation and caused hypocalcaemia. Notable sCT absolute bioavailability (F) values were: 5.5% from minispheres containing NaTDC (i.j), 17.3% with CG (i.c.) and 18.2 % with C 10 (i.c.). Coated minispheres administered by oral gavage at threefold higher doses also induced hypocalcaemia. A highly competitive F value of 2.7% was obtained for orally-administered sCT-minispheres containing CG (45 μmol/kg) and coated with Eudragit ® . In conclusion, the SmPill ® technology is a potential dosage form for several peptides when formulated with PEs and coated for regional delivery. PK data from instillations over-estimates oral bioavailability and poorly predicts rank ordering of formulations .

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Section: Introductionmentioning

confidence: 99%

Section: Smpill ® Minisphere Preparation With Pesmentioning

confidence: 99%

Section: Smpill ® Minisphere Preparation With Pesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Coated minispheres of salmon calcitonin target rat intestinal regions to achieve systemic bioavailability: Comparison between intestinal instillation and oral gavage

Aguirre

Aversa

Rosa

et al. 2016

Journal of Controlled Release

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Application or function of citric acid in drug delivery platforms

Pooresmaeil

Javanbakht

Namazi

et al. 2021

Medicinal Research Reviews

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Nontoxic materials with natural origin are promising materials in the designing and preparation of the new drug delivery systems (DDSs). Today's, citric acid (CA) has attracted a great deal of attention because of its special features; green nature, biocompatibility, low price, biodegradability, and commercially available property. So, CA has been employed in the preparation of the various platforms to induce a suitable property on their structure. Recently, several research groups investigated the CA‐based platforms in different forms like tablets, dendrimers, hyperbranched polymers, (co)polymer, hydrogels, and nanoparticles as efficient DDSs. By considering an increasing amount of published articles in this field, for the first time, in this review, an overview of the published works regarding CA applications in the design of various DDSs is presented with a detailed and insightful discussion.

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Current status of selected oral peptide technologies in advanced preclinical development and in clinical trials

Aguirre

Teijeiro‐Osorio

Rosa

et al. 2016

Advanced Drug Delivery Reviews

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151

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Publication informationAdvanced Drug Delivery Reviews, 106 (Part B):Publisher Elsevier Item record/more information http://hdl.handle.net/10197/7801 Publisher's statementThis is the author's version of a work that was accepted for publication in Advanced Drug Delivery Reviews. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Advanced Drug Delivery Reviews (106, Part B, (2016)

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In vitro and in vivo preclinical evaluation of a minisphere emulsion-based formulation (SmPill®) of salmon calcitonin

Cited by 23 publications

References 38 publications

Coated minispheres of salmon calcitonin target rat intestinal regions to achieve systemic bioavailability: Comparison between intestinal instillation and oral gavage

Coated minispheres of salmon calcitonin target rat intestinal regions to achieve systemic bioavailability: Comparison between intestinal instillation and oral gavage

Application or function of citric acid in drug delivery platforms

Current status of selected oral peptide technologies in advanced preclinical development and in clinical trials

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