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Amorphous Magnesium Carbonate Nanoparticles with Strong Stabilizing Capability for Amorphous Ibuprofen
Uppsala universitet, Teknisk-naturvetenskapliga vetenskapsområdet, Tekniska sektionen, Institutionen för teknikvetenskaper, Nanoteknologi och funktionella material.
Uppsala universitet, Medicinska och farmaceutiska vetenskapsområdet, Farmaceutiska fakulteten, Institutionen för farmaci.ORCID-id: 0000-0002-7781-4753
Uppsala universitet, Teknisk-naturvetenskapliga vetenskapsområdet, Tekniska sektionen, Institutionen för teknikvetenskaper, Tillämpad materialvetenskap.
Uppsala universitet, Medicinska och farmaceutiska vetenskapsområdet, Farmaceutiska fakulteten, Institutionen för farmaci.ORCID-id: 0000-0002-8917-2612
Visa övriga samt affilieringar
2018 (Engelska)Ingår i: International Journal of Pharmaceutics, ISSN 0378-5173, E-ISSN 1873-3476, Vol. 548, nr 1, s. 515-521Artikel i tidskrift (Refereegranskat) Published
Abstract [en]

Formulating active pharmaceutical ingredients (APIs) in the amorphous state can increase their apparent aqueous solubility and dissolution rate and consequently improve their bioavailability. This study demonstrates, for the first time, the ability to stabilize an API in the amorphous state using a solid dispersion of magnesium carbonate nanoparticles within the API. Specifically, high proportions of ibuprofen were able to be stabilized in the amorphous state using as little as 17% wt/wt amorphous magnesium carbonate nanoparticles, and drug release rates 83 times faster than from the crystalline state were achieved. Biocompatibility of the nanoparticles was demonstrated in vitro using human dermal fibroblasts and stability of the nanocomposite formulation was verified with a storage time of six months. The success of this novel formulation provides a promising approach for achieving improved apparent solubility and enhanced bioavailability of drugs.

Ort, förlag, år, upplaga, sidor
Elsevier, 2018. Vol. 548, nr 1, s. 515-521
Nyckelord [en]
Magnesium carbonate, Nanoparticles, Nanocomposite, Amorphous, Ibuprofen, Solubility, Dissolution
Nationell ämneskategori
Nanoteknik Farmaceutiska vetenskaper
Identifikatorer
URN: urn:nbn:se:uu:diva-354506DOI: 10.1016/j.ijpharm.2018.07.021ISI: 000440552100050PubMedID: 29981897OAI: oai:DiVA.org:uu-354506DiVA, id: diva2:1221565
Forskningsfinansiär
VetenskapsrådetTillgänglig från: 2018-06-20 Skapad: 2018-06-20 Senast uppdaterad: 2019-11-07Bibliografiskt granskad
Ingår i avhandling
1. Amorphous magnesium carbonate nanomaterials: Synthesis, characterization and applications
Öppna denna publikation i ny flik eller fönster >>Amorphous magnesium carbonate nanomaterials: Synthesis, characterization and applications
2018 (Engelska)Doktorsavhandling, sammanläggning (Övrigt vetenskapligt)
Abstract [en]

High surface-to-volume ratio materials, including nanoparticles and mesoporous materials, have a number of applications due to their large surface area and special structures. Traditional approaches for synthesizing high surface-to-volume ratio nanomaterials are often complicated, expensive or environmentally unfriendly. Considering aspects such as availability and safety in terms of environmental or biological contact, magnesium carbonate-based nanomaterials are an interesting and potentially valuable candidate for novel applications. The overall aim of this thesis was to develop novel high surface-to-volume ratio amorphous magnesium carbonate nanomaterials and investigating their possible applications.

Amorphous magnesium carbonate nanoparticles (AMN) were successfully synthesized via a simple and low-temperature pathway. The structure and resulting properties of the material can be tailored by changing the final steps in the synthesis process.

The ability of AMN to stabilize ibuprofen (IBU) in the amorphous state was investigated. Nanocomposites with IBU:AMN mass ratios as high as to 5:1 were shown to enhance the release rate of IBU in vitro by as much as 83 times compared to IBU in crystalline form. A related nanostructured material, mesoporous magnesium carbonate (MMC), was evaluated as a drug carrier for stabilizing amorphous drugs through the incorporation of the drug within its pores. In this study, MMC was used to release and sustain two poorly soluble drugs (tolfenamic acid and rimonabant) in the supersaturated state with the assistance of hydroxypropyl methylcellulose.

AMN was also used to synthesize a novel adhesive together with IBU without the addition of a polymer. This adhesive was transparent, self-healing, shapeable, stretchable and reusable. In addition, the adhesive was able to glue a variety of materials, including metals, glass, paper and plastics (even Teflon).

Finally, AMN was used to prepare flexible, transparent and UV-shielding films when incorporated into a PMMA matrix. These films exhibited both UV-shielding properties and moisture absorbance and retention abilities. In addition, the UV- and thermo-stability of these films were enhanced by the addition of AMN.

The work presented in this thesis show that the nanomaterials AMN and MMC possess great potential for an extremely broad range of applications, from pharmaceutical applications dealing with poorly soluble drugs to structural applications such as adhesives to applications in optics or electronics such as UV-shielding or moisture barrier films.

Ort, förlag, år, upplaga, sidor
Uppsala: Acta Universitatis Upsaliensis, 2018. s. 82
Serie
Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Science and Technology, ISSN 1651-6214 ; 1685
Nyckelord
high surface-to-volume ratio, nanoparticles, mesoporous, magnesium carbonate, amorphous drugs, supersaturated concentration, general adhesives, UV-shielding
Nationell ämneskategori
Nanoteknik
Identifikatorer
urn:nbn:se:uu:diva-354512 (URN)978-91-513-0370-3 (ISBN)
Disputation
2018-09-07, Häggsalen, Ångströmlaboratoriet, Lägerhyddsvägen 1, Uppsala, 13:25 (Engelska)
Opponent
Handledare
Tillgänglig från: 2018-08-15 Skapad: 2018-06-20 Senast uppdaterad: 2018-08-28

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Yang, JiaojiaoAlvebratt, CarolineLu, XiBergström, ChristelStrömme, MariaWelch, Ken

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Yang, JiaojiaoAlvebratt, CarolineLu, XiBergström, ChristelStrömme, MariaWelch, Ken
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Nanoteknologi och funktionella materialInstitutionen för farmaciTillämpad materialvetenskap
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International Journal of Pharmaceutics
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