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Spray-Drying, Solvent-Casting and Freeze-Drying Techniques: a Comparative Study on their Suitability for the Enhancement of Drug Dissolution Rates

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Abstract

Purpose

Solid dispersions (SDs) represent the most common formulation technique used to increase the dissolution rate of a drug. In this work, the three most common methods used to prepare SDs, namely spray-drying, solvent-casting and freeze-drying, have been compared in order to investigate their effect on increasing drug dissolution rate.

Methods

Three formulation strategies were used to prepare a polymer mixture of polyvinyl-alcohol (PVA) and maltodextrin (MDX) as SDs loaded with the following three model drugs, all of which possess a poor solubility: Olanzapine, Dexamethasone, and Triamcinolone acetonide. The SDs obtained were analysed and compared in terms of drug particle size, drug-loading capacity, surface homogeneity, and dissolution profile enhancement. Physical-chemical characterisation was conducted on pure drugs, as well as the formulations made, by way of thermal analysis and infrared spectroscopy.

Result

The polymers used were able to increase drug saturation solubility. The formulation strategies affected the drug particle size, with the solvent-casting method resulting in more homogenous particle size and distribution when compared to the other methods. The greatest enhancement in the drug dissolution rate was seen for all the samples prepared using the solvent-casting method.

Conclusion

All of the methods used were able to increase the dissolution rate of the pure drugs alone, however, the solvent-casting method produced SDs with a higher surface homogeneity, drug incorporation capability, and faster dissolution profile than the other techniques.

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Abbreviations

Δcp:

Heat capacity

APIs:

Active pharmaceutical ingredients

BCS:

Biopharmaceutical classification systems

DMSO:

Dimethyl sulfoxide

DSC:

Differential scanning calorimetry

Dsm:

Dexamethasone

DPBS:

Dulbecco buffer phosphate

FTIR:

Fourier transform infrared

HME:

Hot melt extrusion

HPMC:

Hydroxypropyl-methylcellulose

KBr:

Potassium bromide

MDX:

Maltodextrin

Olz:

Olanzapine

PVA:

Polyvinyl-alcohol

SD:

Solid dispersion

SEM:

Scanning electron microscopy analysis

Tg:

Glass transition

TGA:

Thermogravimetric analysis

Tm:

Melting point

Trm:

Triamcinolone acetonide

UV:

Ultraviolet

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Authors and Affiliations

  1. Dipartimento di Scienze per la promozione della Salute e Materno Infantile “Giuseppe D’Alessandro”, Palermo, Italy

    Laura Modica De Mohac

  2. Advanced Technologies Network Center (ATeN Center), University of Palermo, Viale Delle Scienze – Edificio, 18 – 90128, Palermo, Italy

    Roberto Caruana

  3. Laboratory of Biocompatible Polymers, Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università di Palermo, Via Archirafi, 32 - 90123, Palermo, Italy

    Gennara Cavallaro, Gaetano Giammona & Mariano Licciardi

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  1. Laura Modica De Mohac
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Correspondence to Mariano Licciardi.

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De Mohac, L.M., Caruana, R., Cavallaro, G. et al. Spray-Drying, Solvent-Casting and Freeze-Drying Techniques: a Comparative Study on their Suitability for the Enhancement of Drug Dissolution Rates. Pharm Res 37, 57 (2020). https://doi.org/10.1007/s11095-020-2778-1

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