Stabilisation and delivery of labile materials by amorphous carbohydrates and their derivatives

Hatley, Ross H.M.; Blair, J. A.

doi:10.1016/s1381-1177(99)00018-1

Cited by 41 publications

(22 citation statements)

References 27 publications

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“…They possess advantageous properties such as being readily available with high purity, low toxicity, good glass-formers and have high glass transition temperatures (T g ). 1,2 At temperatures below T g , in the so-called glassy state, molecular mobility is sharply reduced. High viscosity of the system slows the relaxation time down dramatically and the amorphous formulation gains physical stability.…”

Section: Introductionmentioning

confidence: 99%

“…High viscosity of the system slows the relaxation time down dramatically and the amorphous formulation gains physical stability. 1 The higher the T g value of an amorphous formulation the higher the temperature to which the physical stability can be extended. Thus, encased in a high T g amorphous carbohydrate, pharmaceutical products may be stored at room temperature and shipped without cooling.…”

Section: Introductionmentioning

confidence: 99%

“…For example, the disaccharide trehalose (Scheme 1) is widely used for this purpose due to its relatively high glass transition temperature and low tendency to crystallise. [1][2][3][4] 0008-6215/$ -see front matter Ó 2007 Elsevier Ltd. All In general, carbohydrates are hydrophilic and tend to strongly interact with water, which they may absorb either during the manufacturing process of a pharmaceutical formulation or from their surrounding after manufacture. Water can act as plasticizing agent changing the key mechanical properties and depressing the glass transition temperature of an amorphous carbohydrate.…”

Section: Introductionmentioning

confidence: 99%

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The glass transition temperatures of amorphous trehalose–water mixtures and the mobility of water: an experimental and in silico study

Simperler

Kornherr

Chopra

et al. 2007

Carbohydrate Research

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

The glass transition temperatures of amorphous trehalose–water mixtures and the mobility of water: an experimental and in silico study

Simperler

Kornherr

Chopra

et al. 2007

Carbohydrate Research

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“…49 In the case of carbohydrates, several parameters such as hygroscopicity and the formation of amorphous glasses during drying have to be taken into consideration. 50,51 Donnelly et al 52 reported hygroscopic properties of monosaccharides and disaccharides at 90% relative humidity. They found a higher hygroscopicity for glucose and sucrose compared to lactose, which correlates well with the observed re-swelling capacity of carbohydrate supplemented BNC.…”

Section: Discussionmentioning

confidence: 99%

Bacterial nanocellulose with a shape-memory effect as potential drug delivery system

et al. 2014

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In the steadily emerging field of applications for the natural biopolymer bacterial nanocellulose (BNC), the development of environmentally-friendly and cost-saving techniques to form xerogels by partial or complete dewatering is of great interest for convenient storage, handling and a reduced risk of microbial contamination. Air-dried BNC itself is not able to rehydrate after complete drying due to a structural collapse. In the present paper, it was supplemented with different hydrophilic, water-binding additives and characterized regarding morphology, re-swelling behavior, mechanical stability and potential as drug delivery system. A fast rehydration could be obtained by the addition of magnesium chloride > glucose > sucrose > sorbitol, with a maximum re-swelling percentage up to about 88% (magnesium chloride) of the initial wet weight. In contrast, poly(ethylene glycol) (8 kDa), lactose and trehalose reached only 12-30% whereas mannitol and sodium chloride only had a negligible effect. A high re-swelling value was found to be correlated with the preservation of the three-dimensional BNC network structure and mechanical characteristics such as compression and tensile strength. Confirming the relevance of these findings, the use of the hydrophilic model drug azorubine demonstrated the applicability of the shapememorized bacterial nanocellulose as drug delivery system with controllable release profiles.

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“…In order to satisfy these requirements, peptides and proteins are usually formulated as amorphous glasses. The principle is based on the addition of a glass-forming excipient (typically a carbohydrate, polymer or organic salts) to a solution of the pharmaceutically active material, followed by drying of the solution under conditions that result in the formation of an amorphous glassy matrix in which the pharmaceutically active material is protected from degradation (Hatley and Blair, 1999;Telko and Hickey, 2005). Franks et al (1991) described a possible mechanism of glassy immobilisation for protection of proteins: the formation of an amorphous glass during drying provides a rigid matrix around the protein molecules to restrict and stabilise their motion.…”

Section: Introductionmentioning

confidence: 99%

Formulation, stability and pharmacokinetics of sugar-based salmon calcitonin-loaded nanoporous/nanoparticulate microparticles (NPMPs) for inhalation

Amaro

Tewes

Gobbo

et al. 2015

International Journal of Pharmaceutics

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A challenge exists to produce dry powder inhaler (DPI) formulations with appropriate formulation stability, biological activity and suitable physicochemical and aerosolisation characteristics that provide a viable alternative to parenteral formulations. The present study aimed to produce sugar-based nanoporous/nanoparticulate microparticles (NPMPs) loaded with a therapeutic peptide - salmon calcitonin (sCT). The physicochemical properties of the powders and their suitability for pulmonary delivery of sCT were determined. Production of powders composed of sCT loaded into raffinose or trehalose with or without hydroxypropyl-β-cyclodextrin was carried out using a laboratory scale spray dryer. Spray dried microparticles were spherical, porous and of small geometric size (≤2 μm). Aerodynamic assessment showed that the fine particle fraction (FPF) less than 5 μm ranged from 45 to 86%, depending on the formulation. The mass median aerodynamic diameter (MMAD) varied between 1.9 and 4.7 μm. Compared to unprocessed sCT, sCT:raffinose composite systems presented a bioactivity of approximately 100% and sCT:trehalose composite systems between 70-90% after spray drying. Storage stability studies demonstrated composite systems with raffinose to be more stable than those containing trehalose. These sugar-based salmon calcitonin-loaded NPMPs retain reasonable sCT bioactivity and have micromeritic and physicochemical properties which indicate their suitability for pulmonary delivery. Formulations presented a similar pharmacokinetic profile to sCT solution. Hence the advantage of a dry powder formulation is its non-invasive delivery route and ease of administration of the sCT.

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Stabilisation and delivery of labile materials by amorphous carbohydrates and their derivatives

Cited by 41 publications

References 27 publications

The glass transition temperatures of amorphous trehalose–water mixtures and the mobility of water: an experimental and in silico study

The glass transition temperatures of amorphous trehalose–water mixtures and the mobility of water: an experimental and in silico study

Bacterial nanocellulose with a shape-memory effect as potential drug delivery system

Formulation, stability and pharmacokinetics of sugar-based salmon calcitonin-loaded nanoporous/nanoparticulate microparticles (NPMPs) for inhalation

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